Benzoxazinone or pyridoxine compounds, methods for their preparation, intermediate compounds, pharmaceutical composition having antibacterial activity, methods of treatment of bacterial infections |
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IPC classes for russian patent Benzoxazinone or pyridoxine compounds, methods for their preparation, intermediate compounds, pharmaceutical composition having antibacterial activity, methods of treatment of bacterial infections (RU 2191179):
                                                                                                                                                                                                  
 Tricyclic pyrazole derivatives, pharmaceutical composition / 2191176
The invention relates to new tricyclic pyrazole derivative or its pharmaceutically acceptable salt
 Derivatives of sulfonamides, the method of production thereof and pharmaceutical composition / 2168503
The invention relates to compounds of formula (I):
 < / BR>where -A= B-C= D - represents-CH=CH-CH=CH-group, in which 1 or 2 CH may be replaced by nitrogen; Ar denotes phenyl or naphthyl, unsubstituted or one-, two - or three-fold substituted with H, Gal, Q, alkenyl with the number of C-atoms up to 6, Ph, OPh, NO2, NR4R5, NHCOR4, CF3, OCF3CN, OR4, COOR4, (CH2)nCOOR4, (CH2)nNR4R5, -N=C=O or NHCONR4R5phenyl or naphthyl; R1, R2, R3each independently from each other, are absent or represent H, Gal, Q, CF3, NO2, NR4R5, CN, COOR4or CHCOR4; R4, R5each independently of one another denote H or Q, or together also denote-CH2-(CH2)N-CH2-; Q denotes alkyl with 1-6 C-atoms; Ph denotes phenyl; X denotes O or S; Gal denotes F, Cl, Br or I; "n" represents 1, 2 or 3; and their salts, except 4-methyl-N-(2,1,3-benzothiadiazole - 5-yl)benzosulfimide, 4-nitro-N-(2,1,3-benzothiadiazole-5-yl)- benzosulfimide and 4-amino-N-(2,1,3-benzothiadiazole-5-yl)- benzolsulfonat  Substituted tetracyclic derivatives of oxazepine and thiazepine, the method of production thereof, the composition having antipsychotic activity, and how you can get / 2161159
The invention relates to compounds of the formula I, their pharmaceutically acceptable salts and stereoisomeric forms, where R is hydrogen or C1-6-alkyl; R2is hydrogen; C1-6-alkyl; trihalomethanes; C1-6-alkyl, substituted carboxyla,1-6-alkylcarboxylic,1-6-allyloxycarbonyl, or R1and R2taken together with the nitrogen atom to which they are attached, may form a ring morpholinyl or optionally substituted heterocyclic radical; R3- R10each independently represents hydrogen; R8, R9independently represent hydrogen or halogen; R11and R12is hydrogen; n= 1, 2, 3, 4, 5 or 6; X Is O, S, S(=O)
 Derivatives (1,2,3-triazolyl)-1,2,5-oxadiazole, potentiating no-dependent activation of the soluble form of guanylate cyclase / 2158265
The invention relates to new chemical compounds, in particular derivatives (1,2,3-triazolyl)-1,2,5-oxadiazole General formula I, where R = NH2or
 < / BR>and, if R1= N, R2lowest hydroxyalkyl, or, if R1- lower alkyl, lower hydroxyalkyl, aryl, R2= N, the lower hydroxyalkyl or a radical of General formula-C(O)R3where R3= HE, NH2, lower alkyl or lower alkoxyl, potentiating NO-dependent activation of the soluble form of guanylate cyclase (RGC)  Derivative hinolan and naphthyridinone acid, mixture of isomers, or individual isomers in the form of a hydrate or salt with antibacterial activity, isoindole derivatives as intermediates for obtaining the derivatives of hinolan and naphthyridinone acid / 2145604
The invention relates to new chemical compounds with valuable biological properties, in particular to derive hinolan and naphthyridinone acids with antibacterial activity, as well as to the isoindole derivative as starting compounds for obtaining the derivatives hinolan and naphthyridinone acid
 Derivatives benzothiophene, benzofuran, indoltiazepinone, oxazepines and diazepinone, the pharmaceutical composition having inhibitory cell adhesion or hiv activity, the method of inhibition of leukocyte adhesion to endothelial cells in the treatment of diseases caused by it, the method of treating mammals infected with hiv / 2144033
The invention relates to new heterocyclic compounds with biological activity, more specifically, to the derivatives of benzothiophene, benzofuran, indoltiazepinone, oxazepines and diazepinone, the pharmaceutical composition having inhibitory cell adhesion or HIV activity, method of inhibition of leukocyte adhesion to endothelial cells in the treatment of diseases caused by it and the method of treating mammals infected with HIV
 Derivatives of guanidine, the retrieval method, the method of inhibition of na+/h+- metabolism in cells / 2141946
The invention relates to new derivatives of guanidine and their pharmaceutically acceptable salts, used as medicines
 The method of obtaining 2,5-dialkoxy-2,5-dihydrofuran / 2124508
The invention relates to the field of organic chemistry - getting hard-heterocyclic compounds in the range of 2.5-dialkoxybenzene, namely 2,5-dialkoxy-2,5-dihydrofuran, formula I, where R is alkyl and R1is a hydrogen atom or methyl, which are intermediates in the synthesis of chemicals and biologically active substances
![6-methyl-3,4-dioxo-1-(4-methoxybenzylidene)-furo[3,4-c] pyridine, manifesting stimulating germination of seeds of agricultural crops](http://img.russianpatents.com/img_data/8/84439-s.gif) 6-methyl-3,4-dioxo-1-(4-methoxybenzylidene)-furo[3,4-c] pyridine, manifesting stimulating germination of seeds of agricultural crops / 2117008
The invention relates to new biologically active chemical compound exhibiting the properties of activator germination of seeds of agricultural crops
 Bicyclic aromatic amino acids / 2187506
 Derivatives of colchicine, methods for their preparation and pharmaceutical compositions based on them / 2181354
The invention relates to the derivatives of colchicine formula (I), where R denotes methoxy or methylthiourea; R1means a linear or branched C1- C6alkyl, provided that when R is methoxy, R1cannot be methyl; and compounds of formula II, where R is methylthio; R1means a linear or branched C1- C6-alkyl
The way to prevent septic complications in the postoperative period / 2191014
The invention relates to medicine, in particular to surgery, and can be used for prophylaxis of septic complications in the postoperative period
 Salt of 5,5'-aileenpearlpiyali and 5,5'-arylidene(2 - thiobarbiturate) acid and 5,5'-arylidene(2 - thiobarbiturate) acid, which has antimicrobial, antiviral, immunomodulatory and antitumor activity / 2188195
The invention relates to new salts of 5,5'-aileenpearlpiyali and 5,5'-arylidene(2-thiobarbiturate) acid and 5,5' - arylidene(2-thiobarbiturate) acids of General formula I having antimicrobial, antiviral, immunomodulatory and antitumor activity
 The method of treatment of experimental leprosy infection / 2188003
The invention relates to medicine, to leprology, can be used to treat leprosy infection in the experiment
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(57) Abstract: The invention relates to new benzoxazine and piridokshinom compounds of formula I, where part of the Q - condensed phenyl, or condensed pyridyl; Z1is hydrogen, halogen, C1-C6alkyl, phenyl, nitro, sulfonylamino or trifluoromethyl; Z2is hydrogen or halogen; X is hydrogen or oxygen; And - C1-C6-alkyl, C1-C6-alkylaryl or C1-C6-Alkylglucoside, where aryl and heterocyclyl described in the claims, n = 0 to 3; Y is the portion described in the claims, and their pharmaceutically acceptable salts, esters and proletarienne forms. Also disclosed are methods for their preparation, intermediate compounds, pharmaceutical compositions based on them, which have antibacterial activity, and methods of treating bacterial infections. The invention can be used in medicine as an anti-infective funds. 10 C. and 22 C.p. f-crystals, 2 PL. The invention relates to benzoxazine and piridokshinom antibacterial compounds, to pharmaceutical compositions containing these compounds, and methods for their preparation and use. These compounds are effective when ingibiruet against a number of bacterial organisms, including organisms which are resistant to other antibiotics. Prokaryotes regulate the transcription of many genes in response to changes in the environment organisms (J. C. Stock, A. M. Stock, and J. M. Mottonen, Nature, 344, 395-400 (1990)). Such regulation is essential if the body must adapt to survive in a variable environment, and pathogenic bacteria use such systems of regulation, which enable them to survive in the host organism (J. F. Miller, J. J. Mekalanos, S. Falkow, Science, 243, 1059 (1989)). It can be assumed that the chemical compounds that inhibit the mechanisms of regulation are useful anti-infective medicines as they may interfere with the bacteria provide the necessary adaptive changes in patterns of gene expression. Virulence, chemotaxis and the production of toxin, sporulation and reproduction are examples of bacterial processes that are controlled by regulation and which could also be inhibited by such compounds. It is assumed that the inhibition of one or more of these processes leads to a decrease in virulence, to slow or stop bacterial growth and reproduction, and even to bacterial death is certain proteins in the control regulation and in response to the presence of intestinal epithelial cells, which allow them to attach to cells and to colonize these cells. Bacteria unable to synthesize these proteins, avirulent: they cannot cause infection in mice (C. C. Finlay, F. Heffron, S. Falkow, Science, 243, 940-943 (1989)). A similar effect could be expected if the genes encoding these proteins were intact, but remained ExpressionEngine. To perform adaptive responses to the environment bacteria use phosphoramidite mechanisms known in this area as the "two-switch". These switches have as a common effect the transfer of information from the environment to the cell nucleus, where this information appears in the answer by turn on or off the transcription of the corresponding genes. The first stage of this scheme pastoralisme mechanism is based on the action of various enzymes histidinemia (NRC). Most of these enzymes NRC are touch molecules and react to the stimulation of certain environmental signals by transferring phosphate from ATP to the residue histidine NRC protein. Some enzymes NRC stimulated by the presence of receptor proteins (described below), the concentration of which is modulated signals environment multiple acceptor proteins (the latter two components of the switch), who are the regulators of gene expression by binding to regulatory regions of DNA, or with a complex of RNA polymerase), or are themselves kinases to other acceptor molecules. These secondary acceptors, in turn, can be regulatory proteins or kinases for another protein. This cascade of transfer of phosphate from protein to protein in the end leads to the phosphorylation of one or more regulatory proteins, which then regulate gene expression. Mammalian cells do not use or at least at the present time it is unknown what they use NRC-managed system postoperati for the regulation of the gene. Thus, it cannot be expected that compounds that selectively inhibit or autophosphorylation RNA-protein or stage(s) phosphopentose, or both, have an undesirable effect on the host organism and are promising candidates for anti-infective drugs. The emergence of drug resistant pathogens that are resistant to one or more currently available medicines, created the need for new antibiotics that dyoni to meet this need. The presence of numerous RNA-managed systems (now known over fifty) in bacteria gives inhibitors NRC potential advantage compared with those in the present time, the antibiotics that it is unlikely that the mutation of the enzyme NRC will make the body resistant to the drug. Recently, researchers in this field have described a method for detecting bacterial genes "virulence", which is selectively expressed when bacteria infect the host (M. J. Mahan, J. M. Slauch and J. J. Mekalanos, Science, 259, 686-688 (1993)). Mentioned the possible use of this information in the development of new antibiotics, but the actual methods of reducing the expression of these genes have not been described. In a preliminary report of another group of researchers describes inhibitors of two-component switching, regulating gene activation of alginate in Pseudomonas aeruginosa in an in vitro system (S. Roychoudhury et al., Proc. Nat. Acad. Sci., 90, 965-969 (1993)), but not reported antibacterial activity of these compounds. The invention is compounds of General structure I< / BR> where part of the Q - condensed phenyl, or condensed pyridyl; Z1is hydrogen, halogen, C1-C6UB> is hydrogen or halogen; X is hydrogen or oxygen; A - C1-C6-alkyl, C1-C6-alkylaryl or C1-C6-Alkylglucoside, where aryl represents a biphenyl, naphthyl or phenyl and heterocyclyl represents a 5 - or 6-membered saturated or unsaturated heterocyclic group containing 1-4 nitrogen atom, oxygen atom or sulfur, where the aryl or heterocyclyl group optionally substituted C1-C6) alkyl, benzyl, oxybenzyl, phenoxy, hydroxy, alkoxy, halogen, two atoms of halogen, nitro, amino, carboxyla, Carbo(C1-C6)alkoxy or methylsulfonylamino; n = 0 - 3; Y choose from (a) other1R2N+R1R2R3, (b) < / BR> (in) CO2H, CHO; (g) SN(R6)CO2N, SN(R6)CO2CH3CH=CHR7CH=C(CO2H)2; (d) residue formula < / BR> (e) 5-tetrazolyl; where R1, R2and R3independently is hydrogen, C1-C6-alkyl or tert-butoxycarbonyl; R4and R5independently - tert-butoxycarbonyl or hydrogen, or R4and R5can be joined together with formation of the imidazoline ring, imidazoline or pyrimidine; R6is hydrogen, g is acceptable salt, esters and proletarienne form. This invention concerns a method of treating bacterial infections in mammals by introduction of a mammal suffering from such infection a therapeutically effective amount of compounds selected from compounds of the formula I that is effective in the inhibition of bacterial histidinemia. Compounds of the present invention inhibit autophosphorylation bacterial histidines; they also inhibit the transfer of phosphate from phosphorylated histidines to the remains of aspartyl protein-phosphate acceptors involved in the regulation of bacterial gene expression. The standard way, by measuring the minimum inhibitory concentrations (MIC values) found that the compounds of the present invention inhibit the growth of bacteria. Compounds useful as bacteriostatic and bactericidal funds and as anti-infective agents at treatment of infectious diseases. They can also be used to increase the susceptibility of bacteria to conventional antibiotics. Some compounds of formula I are preferred. Preferred implementations of the invention are the order C1-C5-alkyl, CH2-phenyl, CH2-thienyl, CH2-pyridyl, CH2-furyl or ethylpiperidine. Preferred groups for Y are (a) other1R2N+R1R2R3; (b) < / BR> (in) CO2N; (g) SN(R6)CO2N; (d) the balance equations < / BR> where R1, R2and R3independently is hydrogen, C1-C6-alkyl or tert-butoxycarbonyl, R4and R5independently - tert-butoxycarbonyl or hydrogen; R6is hydrogen or hydroxy, and their pharmaceutically acceptable salts, esters and proletarienne form. Most preferred are those compounds of formula I, where part of the Q - condensed phenyl; Z1is hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, phenyl, hydroxy, amino, nitro, sulfonylamino or trifluoromethyl; Z2is hydrogen or, when Z1- halogen, Z2also halogen; X is oxygen; A - C1-C5-alkyl, CH2-phenyl, CH2-thienyl, CH2-pyridyl, CH2-furyl or ethylpiperidine, where the phenyl, thienyl, pyridyl, furyl or piperidino part optionally substituted C1-C6) alkyl, benzyl, oxybenzyl, phenoxy, gidali, selected from (a) other1R2N+R1R2R3; (b) < / BR> (in) CO2N; (g) SN(R6)CO2N; (d) residue formula < / BR> where R1, R2and R3independently is hydrogen, C1-C6alkyl or tert-butoxycarbonyl; R4and R5independently - tert-butoxycarbonyl or hydrogen; R6is hydrogen or hydroxy, and their pharmaceutically acceptable salts, esters and proletarienne form. The present invention relates to certain new intermediate products for the production of the final compounds. Thus, the invention provides intermediates of the following formula < / BR> where part of Q is phenyl or pyridyl; Z1is hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, phenyl, hydroxy, amino, nitro, sulfonylamino or trifluoromethyl and Z2is hydrogen or halogen. Also includes intermediate products of General formula < / BR> where part of Q is phenyl or pyridyl and Z1represents hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, phenyl, hydroxy, amino, nitro, sulfonylamino or trifluoromethyl; Z2represents hydrogen or halogen, And pretty or phenyl and heterocyclyl represents a 5 - or 6-membered saturated or unsaturated heterocyclic group, containing 1-4 nitrogen atom, oxygen atom or sulfur, where the aryl or heterocyclyl group optionally substituted C1-C6)alkyl, benzyl, oxybenzyl, phenoxy, hydroxy, alkoxy, halogen, two atoms of halogen, nitro, amino, carboxyla, Carbo(C1-C4)alkoxy or methylsulfonylamino; and R8represents hydrogen or hydroxyamino group. Suitable hydroxyamine groups include any of the conventional protective groups for hydroxy groups, which are usually used by experts in the field, such as groups specified in T. Greene, "Protecting Groups in Organic Synthesis", J. Wiley and Sons, 1981. They include Silovye esters, aliphatic esters and aromatic esters, such as trimethylsilyl, tert-butyldimethylsilyl, acetyl, benzoyl and the like. Compounds of the present invention receive in accordance with the methods described below and illustrated in the following schemes. The first phase includes a new synthesis reaction accession and cyclization-bromo-butyrolactone, shown in figure 1 (see end of description), with appropriately substituted 2-nitro or 2-aminophenol. The reaction can be carried out in two separate stages, starting with the famous, Oba is retene. The solvent is typically DMF, and to complete the reaction requires basic (alkaline reagent, such as2CO3. Stage cyclization occurs during the restoration of the nitrogroup any systems of reagents, which are known to be suitable for this recovery, including catalyzed by palladium hydrogenation, Nickel and borohydride sodium and zelazowska acid. Alternatively, especially in cases when Z represents a nitro-group, or Q is condensed pyridyl, two stage, addition and cyclization can be carried out in one operation, using a base, such as2CO3or NaH in DMF with heating or without it. Having thus formed the system benzoxazinones heterocyclic ring, an intermediate alcohol 2 you can get a three-stage sequence of reactions. After the stage of protection of the alcohol group known protecting group such as tert-butyldimethylchlorosilane or its equivalent, followed by reaction at position 4, including nucleophilic substitution with alkyl - or helgaleena basic conditions: for example, very effective NaH in DMF. In the alternative case, the transformation of nitrogen in position 4 is the group of alcohol by any conventional reagents with fluoride anion or acid conditions gives compound 2. Obviously, scheme 1 depicts receiving benzoxazinone compounds, where the part "Q" represents a condensed phenyl. Pyridoxine connection part where "Q" represents a condensed pyridyl, can be obtained in accordance with the same method by replacing the phenolic starting material, shown in figure 1, on the appropriately substituted 2-nitro or 2-aminopyridine part. In other syntheses shown in the diagrams 2-10 below, benzoxazinone connections that are shown in the diagrams, the same way you replace pyridoxine connection. A key step in the synthesis is the reaction of a combination of alcohol 2 with substituted phenol via Mitsunobu reaction as shown in scheme 2 (see the end of the description). The Mitsunobu reaction may be one of several variants known in the field; the selection of the appropriate phosphine, azodicarbonamide reagent and solvent will be provided at the discretion of the researcher, based on the published precedents and on the empirical results with a certain combination of substrates, which need to be integrated. Guidance for this can be found in a review article D. L. Hughes in Organic Reactions, 42, 335-656 (1992), and in the following detailed examples. In Bo is whether, alternative, tributylphosphine (VI3P) and (azodicarbon)dipiperidino (ADDP). During the Mitsunobu reaction group Y in most cases should be in a protected form more reactive compounds or the same (for example, when the target compound is a heterocycle group Y must be prior functional group into the target heterocycle. Once formed the link between the two parts, the group Y turn, if necessary, in a preferred functional group, as shown in the diagrams at the end of the description. Suitable protective groups for guanidino and amines include, but are not limited to, TRIFLUOROACETYL, tert-butoxycarbonyl (Vos) and benzyloxycarbonyl. Suitable protective groups for carboxylic acids include, but are not limited to, lower alkalemia esters or benzyl esters; suitable preceding groups include olefin, nitrile or oxazolidin. Chemical processes represented in the diagram, in General, applicable to all definitions Y. To obtain those compounds where X=hydrogen, the reaction mix Mitsunobu conduct derived from the recovered compound 2. Recovery is very easily carried out with a protected precursor connection of reagent, such as a complex of borane-THF. After the reduction reaction of removing the protective groups as shown in scheme 1, gives the alcohol, which undergoes a Mitsunobu reaction as described previously. In figure 4 (see below) shows the reaction of 2 (4-hydroxyphenyl)ethylamine with diret-BUTYLCARBAMATE to obtain a protected phenolic combining component for the Mitsunobu reaction. Commercially available or are known various compounds (hydroxyphenyl)alkylamines followed; they can be synthesized by conventional means, such as reductive amination of benzaldehyde, hydrogenation of arylacetylenes or aryloxyacetic, restoring cynamide or cinnaminnamin etc. Ways to earn them choose, but are not limited to, from the examples presented here. In addition, figure 4 illustrates the receiving protected guanidine from the corresponding amine, again providing a phenolic component for combining Mitsunobu. Demonstrates the use of N,N'-bis(tert-butoxycarbonyl)-S-metalization-chevigny for this purpose is a known technique (R. J. Werdegar, J. S. McManis, J. Org. Chem., 52, 1700-1703 (1987)); in some cases it better by adding to the reaction mixture of the acetate of silver (see what edelenyi Ar, X, W and n. Alternatively, you can obtain 1 (see the description of the invention) with Y= NH2and then turn it the amino group in guanidinium above or other known methods (for example, M. S. Bernatowicz, Y. Wu, G. R. Matsueda, J. Org. Chem., 57, 2497-2502 (1992) and references therein). For compounds where Y represents a carboxylic acid (see definition), the original fooly with the appropriate substitution are known compounds and are commercially available compounds or carboxylic acids, or the corresponding alkanovykh esters. Acid to the combination of Mitsunobu reaction to first protect transformation in alcamovia esters in the usual manner, as shown in scheme 5 (see the end of the description). After the reaction combinations, NaOH saponification get the final products. When n is O and Y is Cho (scheme 6), the reaction with bromoform and CON with subsequent methylation of the crude product gives the hydroxyether 3. The hydrolysis of the thus formed ester gives the corresponding gidrokshikislotu 4. Acid 4 can be treated with reagents such as thionyl chloride, to form chlorinated and then reaction with thiourea to obtain thiazolidinedione, as shown in figure 6 (see the end of the description). For the tion in acidic conditions, for example trifluoroacetic acid or hydrochloric acid in isopropanol, gives amine salts and guanidine, respectively. In cases where a (see the description of the invention) represents a benzyl group, a substituted carboxylic acid, alcohol, shown in scheme 8, can be obtained by the method depicted in scheme 1, using the known benzyl halides having as Deputy ether carboxylic acid. The previously described transformation is carried out with ether in situ with subsequent hydrolysis of the ester to the formation of the acid, usually in the last stages of the reaction. The transformation shown in scheme 1, to obtain the alcohol 2 and the reaction mix described in scheme 2, can be performed with nitrosamine source materials to produce the products shown in scheme 9 (see at the end of the description). The restoration of the nitro-group reagents such as iron/acetic acid or catalyzed by palladium hydrogenation can be performed, for example, compounds derived from protected amino or guanidinopentanoic shown in scheme 2. In the alternative case, the recovery can be performed on unprotected connections provided that does not require further conversion. If taenia products shown in scheme 9. Similar conversions can be performed with compounds derived from compound 2 having nitroaniline Deputy, as shown in figure 10 (see the end of the description). The above reaction is carried out in a solvent suitable for these reagents and materials employed and suitable for implementation. Specialists in the field of organic synthesis should be understood that the various functional groups present in the molecule must be compatible with the alleged chemical transformations. This will depend on the order of the stages of synthesis, protection of reactive groups and the choice of reaction conditions. Reaction conditions compatible with your alternates, must be known to the person skilled in the art, as well as the choice of protective groups in cases where they are required. Of formula I it is obvious that some compounds of the invention in their structure can have one or more asymmetric carbon atoms. It is assumed that the present invention includes in its scope pure stereochemical isomeric forms of the compounds as well as their racemates. Stereochemical pure isomeric form can be obtained by known in this field is talisay and chromatographic methods and enantiomers can be divided from each other by the selective crystallization of the diastereomeric salts with optically active acids or bases or by chiral chromatography. Pure stereoisomers can also be obtained synthetically from appropriate stereochemical pure starting materials or by using stereospecific reactions. Suitable pharmaceutical salts are salts of inorganic or organic acids, such as chloride-hydrogen acid, Hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, acetic acid, succinic acid, oxalic acid, malic acid and the like. Suitable salts are salts of inorganic and organic bases, such as KOH, NaOH, CA(Oh)2, Al(Oh)3, piperidine, morpholine, ethylamine, triethylamine and the like. In the scope of the invention also include hydrated forms of the compounds, which contain various amounts of water, for example hydrated, palpitate and polutorakratnyj form. The ability of bacteria to respond quickly to changes in the environment is of paramount importance for their survival. Bacteria can quickly otec atory, light or environment of the host. These answers can be short, such as responses required for changes in mobility or for entry into the host cell. In the alternative case, the answers may require large changes in gene expression and cellular morphology, such as changes required for sporulation or for survival in the macrophage. The mechanism by which bacteria are able to sense stimuli from the physical environment (or from the cytoplasm) and convert these signals into appropriate responses, often including so-called "two-component" system. As stated above, the method of treatment according to the present invention is based on the inhibition of this system "two items". All bacteria use this mechanism for regulation of various adaptive/virulent factors to facilitate the establishment of bacterial populations in the environment (for example, a bacterial infection in the host). The system always consists of a sensor, which either activates the kinase, or is part of a kinase, which upon stimulation autophosphorylated. This phosphorylated molecule is a very active postdocoral that immediately transfers its phosphate in regulatory compo is Enos in cascade, which in the end end with the regulation of bacterial gene expression. Despite the fact that each of the kinases and regulators answers have a unique sequence (in fact, even functionally identical proteins have several different sequences in different species), they share homologous biochemical mechanism and possess significant homology in the active site. As indicated, the present invention provides compounds which exhibit antibiotic activity by inhibiting autophosphorylation bacterial histidines. They also inhibit the transfer of phosphate from phosphorylated histidines to the remains of aspartyl protein-phosphate acceptors involved in the regulation of bacterial gene expression. This invention is further a method of treating bacterial infections or enhancement or potentiation of the activity of other antibacterial agents in warm-blooded animals which consists in the introduction to the animals of the compounds according to the invention, separately or in mixture with another antibacterial agent in the form of a medicinal product according to the present invention. When the connection ispolnimymi media for example, solvents, diluents and the like, and can be administered orally in such forms as tablets, capsules, dispersible powders, granules, or suspensions containing, for example, from about 0.5 to 5% of suspending agent, syrups containing, for example, from about 10 to 50% of sugar, and elixirs containing, for example, from about 20 to 50% ethanol, and the like, or parenterally in the form of sterile injectable solutions or suspensions containing from about 0.5 to 5% suspending agent in an isotonic medium. These pharmaceutical preparations may contain, for example, from about 0.5 to about 90% of the active ingredient in combination with the carrier, more usually from 5 to 60% by mass. Compositions for topical application may take the form of liquids, creams or gels containing therapeutically effective concentrations of the compounds according to the invention in a mixture with a dermatologically acceptable carrier. Upon receipt of the compositions in oral dosage form can be applied with any conventional pharmaceutical environment. Solid carriers include starch, lactose, dicalcium phosphate, microcrystalline cellulose, sucrose and kaolin, while liquid carriers include sterile water, polite and sesame oil, when they are suitable for the nature of the active ingredient and the particular form of the desired injection. It may be useful to enable assistive devices, usually used in obtaining pharmaceutical compositions, such as corrigentov, coloring agents, preservatives and antioxidants, such as vitamin E, ascorbic acid, BHT and BHA. The preferred pharmaceutical compositions from the standpoint of the ease of obtaining and introduction are solid compositions, particularly tablets and filled with solid or liquid composition of the capsule. Preferably oral administration of the compounds. These active compounds can also enter parenteral or intraperitoneal means. Solutions or suspensions of these active compounds as free base or pharmacologically acceptable salts can be obtained in water suitably mixed with a surface-active substance, such as hydroxypropylcellulose. You can also obtain dispersions in glycerol, liquid polyethylene glycols and their mixtures in oils. During storage and use under normal conditions, these preparations may contain a preservative to prevent the growth of microorganisms. Pharmaceutical fornia powders for the preparation of sterile injectable solutions or dispersions for immediate admission. In all cases the form must be sterile and must be fluid to the extent that makes it easy to inject her with a syringe. It must be stable under the conditions of preparation and storage and must be preserved against the contaminating action of microorganisms, such as bacteria and fungi. The carrier can be a solvent or dispersion medium containing, for example, water, ethanol, polyol (e.g. glycerol, propylene glycol and liquid polyethylene glycol), suitable mixtures and vegetable oil. The effective dose of the applied active ingredient may vary depending on the specific compound, the route of administration and the severity of the condition, which are treated. However, in General satisfactory results are obtained when the compounds according to the invention is administered at a daily dosage of from about 0.1 to about 400 mg/kg animal body weight, preferably in divided doses, administered two to four times a day, or in the form with prolonged action. For most large mammals the total daily dosage is from about 0.07 to 7.0 g, preferably from about 100 to 1000 mg. Dosage forms suitable for internal use comprise from about 100 to 500 mg of active is to develop tools can be adjusted for optimal therapeutic susceptibility. For example, every day you can enter multiple divided doses or dose can be proportionally reduced, which is determined by the need of therapeutic situation. Obtaining the above-mentioned pharmaceutical compositions and pharmaceutical preparations carried out by any method known in this field, for example by mixing the active ingredient(s) with the diluent(s) to form a pharmaceutical composition (e.g., pellets) and then turning compositions in medicine (e.g., tablets). Compounds of the present invention possess antibacterial activity, as defined by the following tests. First, the compounds were tested for their ability to inhibit autophosphorylation kinase a and perestrelyany SpoOF, two proteins involved in one of the above described systems transduction of signals that regulate gene expression in bacteria. Presents compounds were then tested for antibacterial activity against selected organisms in a standard way MIC. The results are shown below. Table 1 lists examples of compounds of the invention together with their values IC50in the NRC analysis in vitro, described or which demonstrate the invention and are not intended in any way to limit the scope of the claims. In table 1 benzoxazinone connections are listed according to the formula < / BR> Table 2 lists the activity for piridokshinom compounds of the following formula, where Q is condensed pyridyl: < / BR> Obtained following the protocols of the above tests. 1. Analysis of autophosphorylated kinase a and perestrelyany SpoOF To study the effect of compounds of the present invention in the process of signal transduction in bacteria investigated the inhibitory effect of compounds on protein kinase a and SpoOF operon of sporulation. Specifically, inhibition of autophosphorylation kinase a and perestrelyany SpoOF was determined in the following analyses. Regulator response SpoOF is the main substrate for phosphorylation by protein kinase, Keene, participating in the process of sporulation in bacteria (see D. Burbulys, K. A. Trach, J. A. Hoch, Cell, 64, 545-552 (1991)). SpoOF and Keene were obtained from recombinant E. coli, sverkhekspressiya these proteins (J. Cavanagh et al., Amino Acids, 6, 131-140 (1994) and references therein). The following source reagents or received and immediately used, or kept at the same temperature: Salt 8X: 2 M KCl (5 ml), 1 M MgCl2(800 ml), 1 M CaCl2(100 ml), 10 mg/ml ASS="ptx2"> Downloadable dye 5X: 0.5 M Tris-HCl, pH 6.8 (7.5 ml), 10% sodium dodecyl sulphate (SDS) (2 ml), 0.1% of Antimicrobial activity of compounds in vitro was determined by the method of microrasbora broth by the method of testing National Committee for Laboratory Standards (NCCLS). This method is described in NCCLS Document M7-A2, Vol. 10, No 8 "Metods for Dilution Antimicrobial Susceptibility Test for Bacteria that Grow Aerobically - Second Edition. In this way the drug with twofold serial dilutions in b is spymania receive the regulation of the turbidity of the actively growing broth cultures so so that the final concentration of the organism for testing after it is added to the wells, was approximately 5x104colony forming units/well. After inoculation of the microplate to microrasbora their incubated at 35oC for 16-20 hours and then read. MIC is the lowest concentration of the test compound that completely inhibits growth of the organism for testing. The degree of growth in the wells containing the test compound compared with the level of growth in the wells with the control growth (without test compound) used in each microplate. As shown in tables 1 and 2, the compounds of the present invention was tested against a number of gram-positive and gram-negative bacteria, receiving a range of activity from 1 to > 128 µg/ml depending on the body for testing. In the analysis for the tests used the following organisms: Gram Bactria Enterococcus faecalis ATCC 29212 Enterococcus faecalis OS 3041 Enterococcus faecium OS 2993 methicillin-resistant Staphylococcus aureus OS 2089 methicillin-resistant Staphylococcus aureus OS 667 Staphylococcus aureus ATCC 29213 Staphylococcus aureus ATCC 6538 Staphylococcus epidermidis oc 2603 Gram-negative bacteria The following examples describe the chemical synthesis of the presented compounds of the present invention. Methods are only illustrations, and the invention should not be construed as limited chemical reactions and the conditions they represent. No attempt is made optimization of the yields obtained in these reactions, and the specialist of this field should be obvious that changes in reaction time, temperature, solvents and/or reagents can increase the outputs. Methods of obtaining examples of the compounds of the invention are presented below. These examples are intended to illustrate methods of synthesis and are in no way intended to limit the scope of the claims. Used abbreviations: DEAD - diethylazodicarboxylate; RH3P - triphenylphosphine; VI3R-three-n-butylphosphine; THF - tetrahydrofuran; DMF is N,N-dimethyl-formamide; ADDP - 1,1'-(azodicarbon)dipiperidino. Reference example 1 The intermediate product 9086-181-1 Dihydro-3-(2-nitrophenoxy)-2(3H) -furanone Method a: 2-NITROPHENOL (20.2 g, 1 EQ) was dissolved in DMF (250 ml) and was treated TO a2CO3(30 g, 1.3 EQ), then at room temperature under nitrogen atmosphere was added a-b is UB>CO3(5 g, 0.25 EQ). After a total reaction time of 48 h the reaction mixture was cooled in an ice bath was added acetic acid (13,7 ml of 1.65 EQ). The crude reaction mixture was poured into water and was extracted with ethyl acetate (EtOAc). The combined extract was concentrated in vacuum and was led from a mixture of ethanol/water, getting white needles (yield of 22.4 g, 70%), so pl. 112-113oC. IR (KBR) 2939, 1771, 1607, 1586, 1524, 1481, 1356, 1275, 1221, 1194, 1019, 745 cm-1;1H NMR (CDCl3) to 7.84 (DD, J=8,1, 1,6 Hz, 1H), 7,62-of 7.48 (m, 2H), 7,16 (m, 1H), 5,02 (apparent t, J=7,4 Hz, 1H), 4,62-to 4.52 (m, 1H), 4,45 is 4.35 (m, 1H), 2,83 is 2.55 (m, 3H). Analysis: Calculated for C10H9NO5: 53,82, N 4,06, N 6,28. Found: 53,65, N 3,84, N 6,05. Reference example 2 The intermediate product 10353-186-AND Dihydro-3-(4-methyl-2-nitrophenoxy)- 2(3H)-furanone Obtained from 4-methyl-2-NITROPHENOL by method And with the release of 33% in the form of a white solid product. MS (CI) 238 (MH+); IR (KBR) 3523, 3072, 3005, 1770, 1623, 1577, 1530, 1496, 1463, 1392, 1357, 1282, 1270, 1225, 1194, 1184, 1095, 1020, 992, 804 cm-1;1H NMR (Dl3) 7,66 (s, 1H), 7,38 (m, 2H), 4,93 (apparent t, J= 7,4 Hz, 1H), 4,59 (m, 1H), 4,39 (seemingly kV, J=7,3 Hz, 1H), 2,78-2,61 (m, 2H), of 2.38 (s, 3H). Analysis: Calculated for C11H11NO5: 55,70, N 4,67, N 5,90. Found: 55,62, N Of 4.66, N Of 5.82. Reference example is ethoxy-2-NITROPHENOL by method a in the form of yellow needles with a yield of 52%. MS (CI) 254 (MN+); IR (KBR) 3519, 3102, 3023, 2984, 1765, 1726, 1581, 1532, 1496, 1463, 1442, 1274, 1265, 1229, 1218, 1178, 1145, 1092, 1068, 1018, 992, 942, 859, 839, 806, 791, 755 cm-1;1H NMR (l3) 7,52 (d, J= 9.1 Hz, 1H), 7,39 (d, J=3.1 Hz, 1H), 7,31 (DD, J=9,1, 3.0 Hz, 1H), 4,87 (apparent t, J=7.5 Hz, 1H), 4,55 (m, 1H), 4,36 (m, 1H), a 3.87 (s, 3H), 2,82-2,69 (m, 1H), 2,68 of $ 2.53 (m, 1H). Analysis: Calculated for C11H11NO6: 52,18, N OF 4.38, N OF 5.53. Found: 52,19, N 4,50, N 5,43. Reference example 4 The intermediate product 11653-187 Dihydro-3-(5 - methoxy-2-nitrophenoxy) -2(3H)-furanone Obtained from 5-methoxy-2-NITROPHENOL by method a to yield 53%, so pl. 109-110oC; MS (CI) MH+254; IR (KBR) 3517, 3100, 3075, 2994, 2955, 2931, 2852, 1484, 1258, 1079, 714 cm-1;1H NMR (DMSO-d6) 7,98 (d, 1H, J=9.1 Hz), 7,02 (d, 1H, J= 2.5 Hz), 6,76 (DD, 1H, J=2.5 a, 9,2 Hz), 5,62 (t, 1H, J=8.7 Hz), 4,48 (dt, 1H, J=2,4, 8,8 Hz), 4,28 (m, 1H), 3,88 (s, 3H), 2,89-by 2.73 (m, 1H), 2,38-to 2.29 (m, 1H). Analysis: Calculated for C11H11NO6: 52,18, N OF 4.38, N OF 5.53. Found: 51,97, N 4,18, N Of 5.45. Reference example 5 The intermediate product 11578-25 Dihydro-3-(3-methyl-2-nitrophenoxy)-2(3H) -furanone Obtained from 3-methyl-2-NITROPHENOL by method a to yield 41%. Part of this material have led from a mixture of CH2CL2/ether, obtaining a white solid product, so pl. 82-84oC. IR (KBr) 2946, 1792, 1530, 12 1H), 4,96 (t, J=7,4 Hz, 1H), 6,97 (DD, J=7,1, 0.6 Hz, 1H), 7,24 and 7.36 (m, 2H); MN+at m/z=238. Analysis: Calculated for C11H11NO5: 55,70, N 4,67, N 5,90. Found: 55,61, N 4,62, N By 5.87. Reference example 6 The intermediate product 11578-61 Dihydro-3-(4 - chloro-2-nitrophenoxy)- 2(3H)-furanone Obtained from 4-chloro-2-NITROPHENOL by method And with the release of 60% and isolated in the form of a yellow solid product, so pl. 136-140oC; IR (KBr) 3110, 1786, 1771, 1608, 1527, 1488, 1359, 1276, 1193, 1180, 1020, 825, 734 cm-1;1H NMR (CDCl3) to 2.57-and 2.83 (m, 2H), 4,35 is 4.45 (m, 1H), 4,54-4,63 (m, 1H), to 4.98 (t, J=7,4 Hz, 1H), of 7.48-7,56 (m, 2H), a 7.85 (d, J=2.3 Hz, 1H); MH+at m/z=258. Analysis: Calculated for C10H8ClNO5: 46,62, N 3,13, N, 5,44. Found: 46,61, N 3,11, N 5,20. Reference example 7 The intermediate product 11578-62 Dihydro-3-(4 - carbomethoxy-2-nitrophenoxy)- 2(3H)-furanone Obtained from 4-carbomethoxy-2-NITROPHENOL by method a with 30% yield using equal parts of reagents. This material was isolated directly from the water treatment product in the form of a solid product, so pl. 99-101oC. IR (KBr) 2958, 1780, 1726, 1618, 1531, 1348, 1300, 1270, 1179, 1127, 756 cm-1;1H NMR (CDCl3) 2,62-to 2.85 (m, 2H), 3,95 (s, 3H), of 4.44 (dt, J=9,3, 7.2 Hz, 1H), 4,58 with 4.65 (m, 1H), 5,14 (t, J=7,3 Hz, 1H), 7,53 (d, J=8,8 Hz, 1H), 8,24 (DD, J=8,8, 2.1 Hz, 1H), ,29, N 4,08, N 4,89. Found: 50,03, N Of 3.85, N 4,68. Reference example 8 The intermediate product 11578-32 Dihydro-3 (4-benzyl-2-nitrophenoxy) -2(3H)-furanone Obtained from 4-benzyl-2-NITROPHENOL by method a to yield 54% in the form of a yellow crystalline solid product, so pl. 117-119oC. IR (KBR) 2931, 1785, 1625, 1535, 1346, 1334, 1279, 1261, 1156, 1022, 756 cm-1;1H NMR (CDCl3) 2,64-to 2.85 (m, 2H), 4,42 (kV, J=7,3 Hz, 1H), 4,57 with 4.65 (m, 1H), of 5.05 (t, J= 7,3 Hz, 1H), 7,40-to 7.59 (m, 6N), 7,78 (DD, J=8,7, 2.4 Hz, 1H), 8,07 (d, J=2.4 Hz, 1H). Analysis: Calculated for C16H13NO5: 64,21, N OF 4.38, N 4,68. Found By: PHP 64.00, N 4,20, N 4,59. Reference example 9 The intermediate product 11578-50 Dihydro-3-(4 - trifluoromethyl-2-nitrophenoxy) -2(3H)-furanone Obtained from 4-trifluoromethyl-2-NITROPHENOL by method a in 51% yield using equal parts of reagents. This material was isolated as a white solid product, so pl. 128-129oC. IR (KBR) 3100, 2995, 1782, 1626, 1537, 1358, 1329, 1283, 1159, 1131, 1098, 998, 822 cm-1;1H NMR (Dl3) 2,63-of 2.86 (m, 2H), 4,40-4,48 (m, 1H), 4,58 with 4.65 (m, 1H), 5,14 (t, J=7,4 Hz, 1H), 7,63 (d, J=8,8 Hz, 1H), 7,83 (DD, J=8,8, 1.9 Hz, 1H), 8,14 (d, J=1.9 Hz, 1H); MN+at m/z=292. Analysis: Calculated for C11H8F3NO5: 45,22, N 3,10, N 4,79. Found: 45,37, N 2,77, N 4,81. Reference 5-fluoro-2-NITROPHENOL by method And with the release of 65% using equal parts of reagents. This material was identified as not quite white solid product after crystallization from a mixture of CH2CL2/ether, so pl. 98-100oC; IR (KBR) 3055, 1773, 1619, 1591, 1508, 1350, 1284, 1024, 750 cm-1;1H NMR (CDCl3) 2,62-to 2.85 (m, 2H), to 4.38-to 4.46 (m, 1H), 4,57 with 4.65 (m, 1H), free 5.01 (t, J=7,3 Hz, 1H), 7.23 percent-7,27 (m, 1H plus l3), of 7.96 (DD, J=9,1, 5.8 Hz, 1H); MN+at m/z=242. Analysis: Calculated for C10H8FNO5: 49, 80MM, 3,34 N, N 5,81. Found: 49,85, N 3,24, N 5,78. Reference example 11 The intermediate product 11578-38 Dihydro-3-(5 - methyl-2-nitrophenoxy)-2(3H) -furanone Obtained from 5-methyl-2-NITROPHENOL by method And with the release of 22% using equal parts of reagents. This material was led from a mixture of CH2CL2/ether, obtaining a white solid product, so pl. 68-70oC; IR (KBR) 3003, 2950, 2928, 1774, 1516, 1355, 1189, 1023, 947 cm-1;1H NMR (CDCl3) 2,43 (s, 3H), 2,58-of 2.81 (m, 2H), 4,35-4,43 (m, 1H), 4,55-to 4.62 (m, 1H), 4,99 (t, J=7,4 Hz, 1H), 6,95 (d, J=8,4 Hz, 1H), 7,28 (s, 1H), 7,79 (d, J=8,3 Hz, 1H); MN+at m/z=238. Analysis: Calculated for C11H11NO5: 55,70, N 4,67, N 5,90. Found: 55,68, N 4,62, N 5,85. Reference example 12 The intermediate product 11578-22-predecessor Dihydro-3-(4,6-dichloro-2-nitrophenoxy) -2(3H)-furanone Obtained from 4,6-dichloro is I. IR (KBR) 3086, 1779, 1542, 1457, 1353, 1250, 1222, 1152, 1066, 995, 877 cm-1;1H NMR (Dl3) 2,62-of 2.81 (m, 2H), 4,35 was 4.42 (m, 1H), 4,59-of 4.66 (m, 1H), 5,02 (t, J=6,6 Hz, 1H), to 7.67 (d, J=2.6 Hz, 1H), 7,86 (d, J=2.6 Hz); MH+at m/z=292. Reference example 13 The intermediate product 9086-183-1 3,4-Dihydro-2-(2-hydroxyethyl)-3-oxo-2H-1,4-benzoxazin Method: Intermediate product 9086-181-1 (11.9 g, 1 EQ, reference example 1) was subjected to reaction with H2when 3,515 bar in the flask vibrator Parra, containing 10% Pd/C (1.8 g, 15% wt./wt.) in ethanol (200 ml) for 13 hours the Catalyst was removed by filtration and the filtrate was concentrated in vacuum. The crude product is triturated with hot diethyl ether, getting benzoxazine with the release of 87% in the form of a white powder, so pl. 65-69oC; IR (KBR) 3298, 3076, 2993, 2917, 1677, 1613, 1505, 1439, 1410, 1312, 1275, 1231, 1119, 1104, 1059, 805, 745, 689 cm-1;1H NMR (Dl3) 8,29 (Shir.s, 1H), 7,01-to 6.95 (m, 3H), PC 6.82 (m, 1H), amounts to 4.76 (DD, J=7,6, and 5.5 Hz, 1H), 3,91 (m, 2H), 2,35 and 2.13 (m, 3H). Analysis: Calculated for C10H11NO3: 62,17, N 5,74, N 7,25. Found: 62,01, N 5,48, N 6,95. Reference example 14 Intermediate 11653-A 3,4-Dihydro-2-(2-hydroxyethyl)-7-methoxy-3 - oxo-2H-1,4-benzoxazin Method: NaBH4(2.7 g, 6 EQ) was slowly added to stir the mixture split timing is SUP>C. the resulting dark reaction mixture was left for slow warming to room temperature. After 2 days the reaction mixture was carefully added 2 N. Hcl until gas evolution stops. The resulting mixture was diluted with water and extracted with ethyl acetate. The combined ethyl acetate layers were washed with saturated Panso3, then was concentrated in vacuum, obtaining a pale yellow solid product with a yield of 66%, so pl. 123-126o; MS (CI) MN+224; IR (KBr) 3475, 3307, 3188, 3066, 2931, 2892, 2835, 1769, 1664, 1450, 1327, 1258, 1224, 925 cm-1;1H NMR (DMSO-d6) 10,15 (Shir.s, 1H), 6,80 (d, 1H, J=8.5 Hz), of 6.52 (d, 1H, J=2.6 Hz), 6,46 (DD, 1H, J=2,6, 8.5 Hz), of 4.67 (DD, 1H, J=4,6, 8,8 Hz), of 4.05 (t, 1H, J=5.4 Hz), with 3.79 (m, 2H), 3,74 (s, 3H), of 2.16 (m, 1H), 2,01 (m, 1H). Analysis: Calculated for C11H13NO4: 59,19, N BY 5.87, N 6,27. Found: 58,87, N 5,80, N 6,09. Reference example 15 Intermediate 11653-29A 3,4-Dihydro-2-(2-hydroxyethyl)-7-nitro-3-oxo-2H - 1,4-benzoxazin Method D: 2-Amino-5-NITROPHENOL (13.5 g, of 87.6 mmol, 1 EQ) and a-bromo-butyrolactone (8.0 ml, 96.3 mmol, 1.1 EQ) was added to stir the mixture of DMF (80 ml) and potassium carbonate (12.1 g, of 87.6 mmol). After boiling under reflux for 5 hours and returned to room temperature, the reaction mixture was poured into an equal Obama at 65oWith getting the product with the release of 45%, so pl. 177-178oC. MS (FAB) MH+239; IR (KBr) 3541, 3204, 3095, 3037, 2929, 2888, 1699, 1599, 1508, 1480, 1417, 1389, 1342, 1299, 1136, 1034, 798, 617, 499 cm-1;1H NMR (DMSO-d6) 11,32 (Shir.s, 1H), to $ 7.91 (DD, 1H, J=2,4, and 8.7 Hz), 7,79 (s, 1H), 7,05 (d, 1H, J=8.7 Hz), 4,82 (DD, 1H, J=3,8, 9.0 Hz), 4,70 (Shir.s, 1H) and 3.59 (m, 2H), up to 1.98 (m, 1H), 1,90 (m, 1H). Analysis: Calculated for C10H10N2O5: 50,42, N TO 4.23, N 11,76. Found: 50,37, N 4,20, N 11,43. Reference example 16 The intermediate product 12168-6-1 3,4-Dihydro-2-(2-hydroxyethyl)-6-methoxy-3-oxo-2H-1,4-benzoxazin Obtained from intermediate 12168-2-1 (reference example 3) as a pale gray solid product with a yield of 76% of the way In, so pl. 111-113oC; MS (CI) 224 (MN+); IR (KBr) 3472, 3337, 3196, 3113, 3055, 2996, 2898, 2832, 1684, 1626, 1611, 1520, 1501, 1466, 1403, 1312, 1292, 1264, 1229, 1192, 1162, 1082, 796, 785 cm-1;1H NMR (CDCl3) 7,99 (Shir.s, 1H), 6,91 (d, J=8,8 Hz, 1H), of 6.52 (DD, J=8,8, 2.8 Hz, 1H), 6,37 (d, J=2,8 Hz, 1H), 4,70 (DD, J= 7,5, a 5.4 Hz, 1H), 3,90 (m, 2H), of 3.77 (s, 3H), of 2.21 (m, 2H). Analysis: Calculated for C11H13NO4: (MN+): 224,0922. Found: 224,0974. Reference example 17 The intermediate product 10353-189-1 3,4-Dihydro-2-(2-hydroxyethyl)-6-methyl-3-oxo-2H-1,4-benzoxazin Obtained by the method of intermediate product 10353-186 - 2919, 1681, 1609, 1523, 1498, 1409, 1365, 1232, 1058, 806 cm-1;1H NMR (CDCl3) of 7.96 (Shir.s, 1H), make 6.90 (d, J= 9.1 Hz, 1H), 6,80 (d, J=9.1 Hz, 1H), is 6.61 (s, 1H), 4.72 in (apparent t, J=7,3 Hz, 1H), 3,90 (seemingly kV, J=5.4 Hz, 2H), 2,32-of 2.15 (m, 3H), of 2.30 (s, 3H). Analysis: Calculated for C11H13NO3: 63,76, N 6,32, N 6,76. Found: 63,54, N 6,20, N 6,76. Reference example 18 The intermediate product 10353-184-IN 3,4-Dihydro-2-(2-hydroxyethyl)-3-oxo-6-trifluoromethyl-2H-1,4-benzoxazin Obtained from intermediate 11578-50 (reference example 9) In and isolated with yields of 54% in the form of a fluffy white solid, MS (CI) 262 (MN+); IR (KBr) 3468, 3202, 3113, 3044, 2962, 2888, 1696, 1622, 1496, 1402, 1336, 1215, 1159, 1124, 1111, 1058, 878, 827, 807 cm-1;1H NMR (CDCl3) 8,01 (Shir.s, 1H), 7,28 (m, 1H), to 7.09 (d, J=8,4 Hz, 1H), 7,05 (s, 1H), a 4.86 (DD, J=8,2, 5,2 Hz, 1H), 3,92 (apparent DD, J=12,7, 5.6 Hz, 2H), 2,38-2,17 (m, 1H), 1,92 (t, J=5.6 Hz, 1H). Analysis: Calculated for C11H10F3NO3: 50,58, N 3,86, N ARE 5.36. HRMS: Calculated for C11H10F3NO3: (MH+): 262,0691. Found: 262,0740. Found: 50,52, N 3,86, N 5,28. Reference example 19 The intermediate product 11578-28 3,4-Dihydro-2-(2 - hydroxyethyl)-5-methyl-3-oxo-2H-1,4-benzoxazin Obtained from intermediate 11578-25 (reference example 5) SPO is ether) to yield 39% in the form of a white solid product, so pl. 147-149oC; IR (KBR) 3221, 1683, 1502, 1480, 1266, 1225, 1099, 1057, 770, 723 cm-1; 1H NMR (Dl3) 2,14 of-2.32 (m, 3H), and 2.27 (s, 3H), 4,71 (kV, J= 5.3 Hz, 2H), 4,71 (DD, J=5,5, 7,4 Hz, 1H), 6,82-6,94 (m, 3H), 8,01 (Shir.s, 1H); MH+at m/z=208. Analysis: Calculated for C11H13NO3: 63,76, N 6,32, N 6,76. Found: 63,38, N 6,24, N 6,72. Reference example 20 The intermediate product 11578-68 6-Chloro-3,4-dihydro-2-(2-hydroxyethyl)-3-oxo-2H-1,4-benzoxazin Received by way of the intermediate product 11578-61 (reference example 6) using 3 EQ NiC26H2O and 6 EQ NaBH4. Allocated in the form of a white solid product with a yield of 66%, so pl. 135-138oC; IR (KBR) 3475, 2956, 1690, 1498, 1385, 1059, 809 cm-1;1H NMR (DMSO-d6) 1,95-of 2.08 (m, 1H), 2,12-of 2.23 (m, 1H), 3.33 and (Shir.s, 1H plus DHO), of 3.77-3,82 (m, 2H), 4,69 (DD, J=8,9, and 4.4 Hz, 1H), 6.87 in (s, 2H), 6,92 (s, 1H), 10,5 (Shir.s, 1H); MN+at m/z=228. Analysis: Calculated for C10H10lN3: 52,76, N 4,43, N 6,15. Found: 53,15, N 4,50, N 6,16. Reference example 21 The intermediate product 11578-72 6 Carbomethoxy-3,4-dihydro-2-(2-hydroxyethyl)-3 - oxo-2H-1,4-benzoxazin Obtained from intermediate 11578-62 (reference example 7) by the method With using 3 EQ NiCl26H2O and 6 EQ NaBH4and highlighted the 1400, 1305, 1214, 1049, 764 cm-1;1H NMR (DMSO-d6) 1,93-2,05 (m, 1H), 2,10-of 2.16 (m, 1H), 3,34 (PTS.Shir. s, 1H), 3.75 to of 3.78 (m, 2H), 3,86 (s, 3H), of 4.77 (DD, J=9,1, a 4.1 Hz, 1H), 7,00 (d, J=8,2 Hz, 1H), EUR 7.57 to 7.62 (m, 2H), 10,65 (Shir.s, 1H). Analysis: Calculated for C12H13NO50,2 H2ABOUT: 56,56, N. AND 5.30, N 5,50. Found: 56,71, N 5,18, N 5,35. Reference example 22 The intermediate product 11578-36 3,4-Dihydro-2-(2 - hydroxyethyl)-6-phenyl-3-oxo-2H-1,4-benzoxazin Obtained from intermediate 11578-32 (reference example 8) by the way with the release of 55% and isolated in the form of a white, crystalline solid product, so pl. 170-171oC; IR (KBR) 3428, 1682, 1605, 1489, 1403, 1237, 1030, 863, 762 cm-1; 1H NMR (DMSO-d6) 1,81-1,90 (m, 1H), 1,92 is 2.01 (m, 1H), 3,53-3,63 (m, 2H), 4,69 (DD, J=9,2, 3,9 Hz, 1H),? 7.04 baby mortality (d, J=8,3 Hz, 1H), 7,13 (d, J= 2.0 Hz, 1H), 7,21 (DD, J=8,4, and 2.1 Hz, 1H), 7,31 and 7.36 (m, 1H), 7,45 (t, J=7.5 Hz, 2H), 7,54 (d, J=7,3 Hz, 2H), 10,78 (s, 1H); MN+at m/z=270. Analysis: Calculated for C16H15NO3: 71,36, N 5,61, N 5,20. Found: 71,06, N Of 5.53, N 5,16. Reference example 23 The intermediate product 11578-42 3,4-Dihydro-7-fluoro-2-(2-hydroxyethyl)-3-oxo - 2H-1,4-benzoxazin Obtained from intermediate 11578-40 (reference example 10) and method C (reaction time 3 days with 43% in the form of a white, solid product, so pl. 136-138o<=5,2 Hz, 2H), 4,01 (t, J=5.4 Hz, 1H), 4,71 (DD, J=8,8, 4.5 Hz, 1H), 6,59-6,70 (m, 2H), 6,85 (DD, J=8,6, and 5.5 Hz, 1H), 10,34 (Shir.s, 1H); MN+at m/z=121. Analysis: Calculated for C10H10FNO3: 56,87, N 4,77, N 6,63. Found: 56,75, N 4,74, N 6,56. Reference example 24 The intermediate product 11578-45 3,4-Dihydro-2-(2 - hydroxyethyl)-7-methyl-3-oxo-2H-1,4-benzoxazin Obtained from intermediate 11578-38 (reference example 11) method and extracted as a white crystalline solid with a yield of 49% after crystallization from ethyl acetate, so pl. 143-144oC; IR (KBR) 3468, 3069, 1664, 1520, 1421, 1260, 1154, 1135, 1057, 931, 802 cm-1;1H NMR (DMSO-d6) 1,72 is 1.86 (m, 1H), 1,87 is 2.00 (m, 1H), of 2.21 (s, 3H), 3,54-of 3.60 (m, 2H), 4,59 (DD, J=9,4, 3,9 Hz, 1H) and 4.65 (t, J=5.3 Hz, 1H), 6,72-of 6.78 (m, 3H), of 10.58 (s, 1H); MH+ at m/z=208. Analysis: Calculated for C11H13NO3: 63,76, N 6,32, N 6,76. Found: 63,73, N 6,30, N 6,67. Reference example 25 The intermediate product 11578-22 6,8-Dichloro-3,4-dihydro-2-(2-hydroxyethyl)-3-oxo-2H-1,4-benzoxazin Obtained from dihydro-3-(3,5-dichloro-2-nitrophenoxy)-2(3H)-furanone method and selected and the form of a white solid product with a yield of 72%, so pl. 174-176oC; IR (KBR) 3056, 1702, 1598, 1478, 1386, 1227, 1055, 853 cm-1;1H NMR (DMSO-d6) 1,77-to 1.87 (m, 1H), 1,89-of 1.95 (m, 1H), 3,55-3,63 (Mr> Analysis: Calculated for C10H9Cl2NO3: 45,83, N OF 3.46, N 5,34. Found: 45,82, N 3,49, N Of 5.29. Reference example 26 Intermediate 11653-20A 3,4-Dihydro-2-(2 - hydroxyethyl)-6-nitro-3-oxo-2H-1,4-benzoxazin Obtained from 2-amino-4-NITROPHENOL by method D with the release of 35%, so pl. 173.5 metric-175oC; MS (FAB) MH+239; IR (KBr) 3401, 3092, 2932, 1595, 1536, 1499, 1323, 1213, 1144, 1100, 945, 474 cm-1;1H NMR (DMSO-d6) 11,06 (Shir.s, 1H), a 7.85 (DD, 1H, J=2,59, of 8.90 Hz), 7,74 (d, 1H, J=2,54 Hz), 7,17 (d, 1H, J=8,90 Hz), 4,88 (DD, 1H, J=3,88, of 8.90 Hz), 4,71 (m, 1H), of 3.56 (m, 2H), 2,03 (m, 1H), 1,90 (m, 1H). Analysis: Calculated for C10H10N2O5: 50,42, N TO 4.23, N 11,76. Found: 50,48, N Is 4.21, N 11,44. Reference example 27 The intermediate product 11653-156-AND 3,4-Dihydro-6-fluoro-2-(2-hydroxyethyl)-3-oxo-2H - 1,4-benzoxazin Obtained from 2-amino-4-terfenol method D to yield 22%, so pl. 126-129,5oC; MS (CI) MH+212; IR (KBr) 3349, 3199, 3109, 3054, 2981, 2893, 1621, 1517, 1500, 1364, 1105, 1009, 946 cm-1;1H NMR (DMSO-d6) 10,78 (Shir.s, 1H), 6,98 (DD, 1H, J=5,1, 8,8 Hz), 6,77 (d, 0.5 H, J=3.0 Hz), 6,74 (d, 0.5 H, J= 3.0 Hz), 6,70 (m, 0.5 H), to 6.67 (d, 0.5 H, J=3.0 Hz) and 4.65 (m, 2H) and 3.59 (m, 2H), 1,96 (m, 1H), 1,79 (m, 1H). Analysis: Calculated for C10H10FNO3: 56,87, N 4,77, N 6,63. Found: 56,55, N 4,91, N 6,54. Reference example 28 Method E: intermediate product 10353 189-1 (1.6 g, 1 EQ, reference example 17) was dissolved in DMF (4 ml) and treated sequentially chloro-tert-butyldimethylsilyl (1.4 g, 1.2 EQ) and imidazole (1.3 g, 2.5 EQ) under stirring in nitrogen atmosphere. After 18 h the reaction mixture was diluted with CH2Cl2and washed with water. The organic layer was concentrated and the product was isolated with a yield of 93% in the form of a white powder by crystallization from a mixture of Meon/water, MS (CI) 322 (MN+); IR (KBR) 2953, 2927, 2883, 2856, 1698, 1609, 1523, 1496, 1360, 1234, 1119, 1093, 842, 832, 811, 778 cm-1;1H NMR (CDCl3) of 8.27 (Shir. s, 1H), 6,86 (d, J=8,1 Hz, 1H), 6,76 (DD, J=8,1, 1.7 Hz, 1H), is 6.61 (d, J= 1.7 Hz, 1H), 4.72 in (DD, J=9,7, and 3.7 Hz, 1H), 3.95 to of 3.78 (m, 2H), 2,28 (s, 3H), of 2.20 (m, 1H), 2,00 (m, 1H), 0,90 (s, N), 0,70 (s, 3H). Analysis: Calculated for C17H27NO3Si: With 63,51, N Of 8.47, N 4,36. Found: 63,90, N 8,44, N 4,28. Reference example 29 The intermediate product 12168-8-1 3,4-Dihydro-2-(2-tert-butyldimethylsiloxy)-3-oxo-6-trifluoromethyl-2H - 1,4-benzoxazin Obtained from intermediate 10353-184-In (reference example 18) in the form of a white solid product with a yield of 90%, MS (CI) 376 (MN+); IR (KBR) 3027, 3076, 2956, 2931, 2883, 2859, 1698, 1615, 1495, 1390, 1335, 1257, 1222, 1164, 1125, 1095, 1069, 956, 833, 777 cm-1;1H NMR (CDCl3) 8,59 (Shir.s, 1H), 7,25 is Leno for C17H24F3NO3Si: 54,38, N 6,44, N Of 3.73. Found: 54,34, N 6,45, N Of 3.73. HRMS: Calculated for C17H24F3NO3Si (MH+): 376,1556. Found: 376,1570. Reference example 30 The intermediate product 10353-188-AND 3,4-Dihydro-2-(2-tert - butyldimethylsiloxy)-3-oxo-2H-pyrido[2,3-b] 1,4-oxazin Obtained from 3,4-dihydro-2-(2-hydroxyethyl)-3-oxo-2H-pyrido[2,3-b]-1,4-oxazine way F with the release of 91% as off-white flakes, MS (CI) 309 (MN+); IR (KBR) 3053, 2955, 2884, 2857, 1699, 1610, 1510, 1463, 1375, 1357, 1278, 1256, 1092, 836, 775 cm-1;1H NMR (CDCl3) the 10.40 (Shir.s, 1H), 8,04 (DD, J=5,4, and 1.4 Hz, 1H), 7,26 (d, J=7.7 Hz, 1H), 7,00 (DD, J=7,7, a 5.4 Hz, 1H), a 4.83 (DD, J=9,5, a 4.1 Hz, 1H), 3,84 (m, 2H), 2,25 (m, 1H), 2,03 (m, 1H), 0,89 (s, N), of 0.07 (s, 3H), 0,06 (s, 3H). HRMS Calculated for C15H24N2O3Si (MH+): 309,1634. Found: 309,1608. Reference example 31 The intermediate product 11653-23 2-(2-tert-Butyldimethylsiloxy) -3,4-dihydro-7-nitro-3 - oxo-2H-1,4-benzoxazin Obtained from intermediate 11653-29A (reference example 15) by method E and allocated by recrystallization from a mixture of diethyl ether/hexane, so pl. 152-157oC; MS (FAB) MH+353; IR (KBR) 3548, 3209, 3094, 2936, 2889, 1702, 1600, 1529, 1509, 1483, 1418, 1390, 1344, 1229, 1133, 1035 cm-1;1H NMR (CDCl3) 9,45 (Shir.s, 1H),, ,10 (s, 3H). Analysis: Calculated for C16H24N2O5Si: 54,52, N 6,86, N 7,95. Found: 54,14, N 6,64, N 8,18. Reference example 32 Intermediate 11653-33A 2-(2-tert-Butyldimethylsiloxy) -3,4-dihydro-6-nitro-3-oxo-2H-1,4-benzoxazin Obtained from intermediate 11653-20A (reference example 26) E yield 92%, so pl. 121,5-124,5oC; MS (FAB) MH+353; IR (KBr) 3190, 3125, 3055, 2952, 2884, 2426, 1921, 1623, 1446, 1296, 1281, 1209, 1004, 925, 682, 512 cm-1;1H NMR (CDCl3) 7,10 (DD, 1H, J=2,65, 8,79 Hz), of 7.75 (d, 1H, J= 2,56 Hz), of 6.96 (DD, 1H, J=4,99, 8,68 Hz), 4,80 (DD, 1H, J=3,88, of 9.30 Hz), of 3.78 (m, 2H), 2,18 (m, 1H), 1,95 (m, 1H), 0,82 (s, N), 0,01 (d, 6N, J=3,51 Hz). Analysis: Calculated for C16H24N2O5: 54,52, N 6,86, N 7,95. Found: 54,18, N 6,51, N 8,29. Reference example 33 The intermediate product 11653-163-A1 2-(2-tert - Butyldimethylsiloxy)-3,4 - dihydro-6-fluoro-3-oxo - 2H-1,4-benzoxazin Obtained from intermediate 11653-156-A (reference example 27) E exit 77%, so pl. 84-86oC; MS (CI) MN+326; IR (KBr) 3101, 3066, 2951, 2931, 2893, 2857, 1692, 1622, 1518, 1499, 1469, 1386, 1292, 1248, 1108, 1006, 812 cm-1;1H NMR (CDCl3) 8,86 (Shir.s, 1H), 6,92 (DD, 1H, J=4,9, 8,8 Hz), to 6.67 (m, 1H), 6,60 (DD, 1H, J=2,9, 8.5 Hz), to 4.73 (DD, 1H, J= 3,7, 9.5 Hz), 3,91-of 3.78 (m, 2H), and 2.26 (m, 1H), up to 1.98 (m, 1H), 0,89 (s, N), 0 the rate of 7.54, N 4,16. Reference example 34 The intermediate product 11578-31 2(2-tert - Butyldimethylsiloxy)-3,4-dihydro-5-methyl-3-oxo-2H-1,4-benzoxazin Obtained from intermediate 11578-28 (reference example 19) by method E and allocated directly from the reaction mixture with the release of 24% in the form of a white solid product by adding water and collecting the precipitate, so pl. 90-92oC; IR (KBR) 2953, 2927, 2855, 1693, 1502, 1482, 1390, 1360, 1250, 1119, 1093, 959, 837, 780, 769 cm-1;1H NMR (CDCl3) of 0.07 (s, 3H), and 0.08 (s, 3H), of 0.90 (s, N), 1,92-2,03 (m, 1H), 2,17-of 2.26 (m, 1H), and 2.26 (s, 3H), 3,78-3,93 (m, 2H), 4.72 in (DD, J=3,7, 9.7 Hz, 1H), for 6.81-6,92 (m, 3H), 8,04 (Shir.s, 1H). Analysis: Calculated for C17H27NO3Si: With 63,51, N Of 8.47, N 4,36. Found: 63,50, N 8,53 N 4,24. Reference example 35 The intermediate product 11578-70 2-(2-tert-Butyldimethylsiloxy) -6-chloro-3,4-dihydro-3-oxo-2H-1,4-benzoxazin Obtained from 11578-68 (reference example 20) by method E using 1 equiv of imidazole and tert-butyldimethylsilyl and isolated with yields of 44% in the form of a white solid after trituration with hexane, so pl. 86-89oC; MN+at m/z= 342; IR (KBR) 2955, 2928, 2881, 2857, 1700, 1496, 1400, 1360, 1231, 1124, 1094, 954, 834 cm-1;1H NMR (l3) of 0.07 (s, 3H), and 0.08 (s, 3H), 0,89 (s, N), 1,96-2,05 (m, 1H), 2,16-of 2.24 (m, 1H), 3,81-3,89 UB>24lN3Si: 56,21, N 7,08, N 4,10. Found: 56,59, N 7,17, N Of 4.04. Reference example 36 The intermediate product 11578-44 2-(2-tert - Butyldimethylsiloxy)-3,4-dihydro-7-fluoro-3-oxo - 2H-1,4-benzoxazin Obtained from 11578-42 (reference example 23) by method E and allocated directly from the reaction mixture with yields of 80% in the form of a white solid product by adding water and collecting the precipitate, so pl. 100-102oC; IR (KBR) 2958, 2928, 2888, 2854, 1697, 1667, 1517, 1428, 1367, 1252, 1150, 1112, 1084, 833, 779 cm-1; 1H NMR (CDCl3) of 0.07 (s, 3H), and 0.08 (s, 3H), of 0.90 (s, N), 1,96-2,05 (m, 1H), 2,16-of 2.27 (m, 1H), 3,80-3,91 (m, 2H), 4,77 (DD, J=9,5, 3.8 Hz), 6,64-to 6.80 (m, 3H), 9,05 (Shir.s, 1H). Analysis: Calculated for C16H24FNO3Si: 59,05, N 7,43, N 4,30. Found: 58,98, N 7,39, N 4,27. Reference example 37 The intermediate product 11578-30 2-(2-tert - Butyldimethylsiloxy)-6,8-dichloro-3,4-dihydro-3-oxo - 2H-1,4-benzoxazin Obtained from 11578-22 (reference example 25) by method E and allocated directly from the reaction mixture with the release of 90% in the form of a white solid product by adding water and collecting the precipitate, so pl. 118-120oC; IR (KBR) 2954, 2931, 2885, 2857, 1702, 1480, 1404, 1254, 1085, 838, 778 cm-1;1H NMR (l3) of 0.07 (s, 3H), and 0.08 (s, 3H), of 0.90 (s, N), 1,94-2,03 (m, 1H), 2,15-of 2.21 (m, 1H), of 3.77-to 3.89 (m, 1H), 3,93 (TD, J=9,7, 4,4 Hz, 1SUB>23Cl2NO3Si: 51,06, N 6,16, N 3,72. Found: 50,72, N By 5.87, N 3,82. Reference example 38 The intermediate product 11578-77-predecessor 2-(2-tert - Butyldimethylsiloxy)-6 - carbomethoxy-3,4-dihydro-3-oxo-2H-1,4-benzoxazin Obtained from intermediate 11578-72 (reference example 21) by way of E with yields of 80%. The crude product was used without further purification. MN+at m/z 366. Reference example 39 The intermediate product 12168-10-1 4-(3-Chlorobenzyl)-3,4-dihydro-2-(2-hydroxyethyl) -3-oxo-6-methyl-2H - 1,4-benzoxazin Obtained in two stages, starting with the intermediate product 12168-51 (reference example 28). Method F: Solution similarvideo alcohol (2.17 g, 1 EQ) in DMF (20 ml) was treated with NaH (60% oil dispersion, 0.27 mg, 1 EQ) in one portion and stirred at room temperature under nitrogen atmosphere for 20 min followed by the addition of a 3-chlorobenzylamino (0,89 ml, 1 EQ). After 14 h the crude reaction mixture was poured into cold water and extracted with ethyl acetate. The combined organic extract washed with brine and concentrated in vacuum. The crude product was used in the next stage without further purification. Method G: the Product of the ways the tion at room temperature for 8 h, the reaction mixture was concentrated in vacuum. The crude product was purified flash chromatography, elwira with ethyl acetate and further purified by rubbing with hot hexane, obtaining a product with a total yield of 93% in the form of a white solid substance, so pl. 75-78oC; MS (CI) 322 (MN+); IR (KBR) 3501, 3451, 3062, 1969, 2937, 2874, 1660, 1610, 1598, 1575, 1513, 1473, 1432, 1387, 1321, 1280, 1258, 1106, 1067, 1061, 934, 775, 698 cm-1;1H NMR (CDCl3) 7,27 (m, 3H), 7,17 (m, 1H), make 6.90 (d, J=8,1 Hz, 1H), 6,79 (d, J=7,0 Hz, 1H), 6,63 (s, 1H), 5,17 (d, J=16,3 Hz, 1H), 5,08 (d, J= 16,3 Hz, 1H), 4,80 (DD, J=7,6, and 5.5 Hz, 1H), 3,92 (seemingly kV, J=5.8 Hz, 2H), 2,29-2,17 (m, 3H), of 2.23 (s, 3H). HRMS: Calculated for C18H18ClNO3(MH+): 332,1053. Found: 332,1041. Reference example 40 The intermediate product 10353-191-1 4-(3-Chlorobenzyl) -3,4-dihydro-2-(2 - hydroxyethyl)-3-oxo-6-methyl-2H-pyrido[2,3-b] 1,4-oxazin Obtained from intermediate 10353-188-A (reference example 40) by methods F and G with the alkylation of 3-chlorobenzylamino with a total yield of 69% as not quite white powder, so pl. 80-81oC; MS (CI) 319 (MN+); IR (KBR) 3525, 3446, 2928, 2874, 1667, 1600, 1574, 1465, 1411, 1362, 1325, 1285, 1230, 1205, 1121, 1096, 1064, 797, 750 cm-1;1H NMR (CDCl3) of 8.04 (DD, J= 4,8, 1.5 Hz, 1H), 7,42 (s, 1H), 7,37-to 7.18 (m, 4H), of 6.96 (DD, J=7,9, and 4.8 Hz, 1H), 5,31 (s, 2H), around 4.85 (DD, J=7,5, a 5.4 Hz, 1H), 3,90 (m, 2H), 2,35-of 2.16 (m, 2H), 2,04 (t, 5.6 Hz, 1H). HRMS: Calculated for C16 4-(4-Chlorobenzyl)-3,4-dihydro-2-(2-hydroxyethyl) -3-oxo-2H - 1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H-1,4-benzoxazine by methods F and G by alkylation of 4-chlorobenzylchloride with a total yield of 63% in the form of a white solid product, so square 86-88oC; MS (CI) 300 (MN+-N2O); IR (KBR) 3496, 2977, 2890, 1656, 1607, 1501, 1466, 1401, 1297, 1250, 1088, 1061, 1018, 795, 747 cm-1;1H NMR (CDCl3) 7,28 (d, J=8.5 Hz, 2H), 7,18 (d, J=8.5 Hz, 2H), 7,05-6,87 (m, 3H), 6,83 (d, J=8.0 Hz, 1H), 5,12 (s, 2H), a 4.83 (DD, J=7,5, and 5.5 Hz, 1H), 3,92 (apparent t, J=5.7 Hz, 2H), 2,38-of 2.15 (m, 3H). Analysis: Calculated for C17H16ClNO3: 64,26, N 5,08, N TO 4.41. Found: 64,01, N 5,08, N 4,37. Reference example 42 The intermediate product 9086-189-1 4-(2-Chlorobenzyl)-3,4-dihydro-2-(2-hydroxyethyl)-3 - oxo-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H-1,4-benzoxazine by methods F and G by alkylation of 2-chlorobenzylchloride with a total yield of 65% in the form of a white powder, so pl. 90-91,5oC; MS (CI) 318 (MN+-N2O); IR (KBR) 3482, 2935, 2881, 1663, 1607, 1594, 1505, 1466, 1443, 1407, 1320, 1306, 1283, 1252, 1063, 749 cm-1;1H NMR (CDCl3) 7,42 (DD, J= 7,6, 1.5 Hz, 1H), 7,30-7,13 (m, 2H), 7,08-9,88 (m, 4H), of 6.73 (DD, J=7,9, 1.3 Hz, 1H), 5.25-inch (d, J=and 17.2 Hz, 1H), 5,23 (d, J=17.3 Hz, 1H), 4,88 (DD, J=7,5, and 5.5 Hz, 1H), 3,95 (formal is N 5,08, N to 4.41. Found: 64,41, N. 5,00, N 4,47. Reference example 43 The intermediate product 12168-25-1 4-(3-Chlorobenzyl)-3,4-dihydro-2-(2-hydroxyethyl)-3 - oxo-6-methoxy-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy)-3,4-dihydro-6-methoxy-3 - oxo-2H-1,4-benzoxazine by methods F and G with the alkylation of 3-chlorobenzylamino with a total yield of 80%. Selected by crystallization from a mixture of ethanol/water in the form of a white powder; MS (CI) 348 (MN+); IR (KBR) 3501, 3053, 3021, 2959, 2933, 2876, 2838, 1664, 1618, 1600, 1575, 1512, 1466, 1445, 1435, 1390, 1361, 1337, 1313, 1272, 1237, 1201, 1173, 1107, 1078, 1049, 1030 cm-1;1H NMR (CDCl3) 7,27-7,20 (m, 3H), 7,13 (m, 1H), 6,94 (d, J=8,8 Hz, 1H), of 6.52 (DD, J= 9,1, 2.7 Hz, 1H), 6,41 (d, J=2.7 Hz, 1H), 5,12 (d, J=16.2 Hz, 1H), 4,79 (DD, J=8,2, a 5.4 Hz, 1H), 3,92 (m, 2H), 3,68 (s, 3H), 3,39-of 2.16 (m, 2H), 2,17 (t, J=5,9 Hz, 1H). Analysis: Calculated for C18H18ClNO40,25 H2ABOUT: WITH 61,37, N OF 5.29, N 3,98. Found: 61,35, N 5,14, N 3,95. Reference example 44 The intermediate product 11578-41 4-(3-Chlorobenzyl)-3,4-dihydro-2-(2-hydroxyethyl)-3-oxo-6-phenyl-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-6-phenyl-2H-1,4-benzoxazine by methods F and G with the alkylation of 3-chlorobenzylamino and Veselin in the form of a white crystalline solid product with an overall yield of 27%, so pl. 119-121o is, J=7,6, and 5.5 Hz, 1H), 5,18 (ABq, JAB=17,1 Hz, 2H),? 7.04 baby mortality (d, J= 1.9 Hz, 1H), was 7.08 (d, J=8,3 Hz, 1H), 7,15-7,42 (m, 10H); MN+at m/z=394. Analysis: Calculated for C23H20lN3: 70,14, N 5,12, N OF 3.56. Found: 70,10, N 5,11, N 3,51. Reference example 45 The intermediate product 10508-24-AND 4-(3-Terbisil)-3,4-dihydro-2-(2-hydroxyethyl)-3-oxo-2H-1,4-benzoxazin Obtained from 2-(2-tert - butyldimethylsiloxy)-3,4-dihydro-3 - oxo-2H-1,4-benzoxazine by methods F and G with the alkylation of 3-formanilide with a total yield of 49% and isolated in the form of a resinous solid product; IR (KBR) 3425, 1683, 1501, 1401, 1252, 1061, 751 cm-1;1H NMR (Dl3) 2,16-of 2.38 (m, 3H), 3,92 (t, J= 5.8 Hz, 2H), around 4.85 (DD, J=7,6, and 5.5 Hz, 1H), 5,14 (s, 2H), 6,82-6,85 (m, 1H), 6.90 to-7,08 (m, 6N), 7,26-7,33 (m, 1H); MH+at m/z=302. Analysis: Calculated for C17H16FNO3: 67,76, N 5,35, N 4,65. Found: 67,48, N Of 5.34, N 4,57. Reference example 46 The intermediate product 10840-33 3,4-Dihydro-2-(2 - hydroxyethyl)-4-(4 - methylbenzyl)-3-oxo-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H-1,4-benzoxazine by methods F and G by alkylation of 4-methylbenzylamine with a total yield of 50%. This material was led from the air, getting a white solid product, so pl. 92-94o=7,4, 5.7 Hz, 1H), 5,12 (s, 2H), 6.90 to-7,00 (m, 4H), 7,13 (s, 4H); MH+at m/z=298. Analysis: Calculated for C18H19NO3: 72,71, N 6,44, N 4,71. Found: 72,71, N 6,48, N 4,65. Reference example 47 The intermediate product 10508-19 3,4-Dihydro-2-(2-hydroxyethyl) -4-(4-methoxybenzyl)-3-oxo-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H-1,4-benzoxazine by methods F and G by alkylation of 4-methoxybenzylamine with a total yield of 48% after flashmemory with elution with a mixture of ethyl acetate/hexane, so pl. 80-82oC; IR (KBR) 3496, 1660, 1515, 1501, 1412, 1250, 1057, 754 cm-1;1H NMR (CDCl3) 2,00 (PTS.Shir.s, 1H), 2,16-is 2.37 (m, 2H), of 3.77 (s, 3H), 3,91 (t, J=6,1 Hz, 2H), 4,82 (DD, J=7,5, and 5.6 Hz, 1H), 5,09 (s, 2H), 6,85 (d, J=8.7 Hz, 2H), 6,91-7,00 (m, 4H), 7,18 (d, J=8.7 Hz, 2H); MN+at m/z=314. Analysis: Calculated for C18H19NO4: 68,99, N 6,11, N 4,47. Found: 69,22, N 6,10, N 4,35. Reference example 48 The intermediate product 10005-181-1 4-(3,5-Dichlorobenzyl)-3,4-dihydro-2-(2-hydroxyethyl) -3-oxo-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H-1,4-benzoxazine by methods F and G with the alkylation of 3,5-dichlorobenzylchloride with a total yield of 89%. The sample was led from a mixture of CH2CL2H NMR (CDCl3) 1,92 (Shir.s, 1H), 2,17-is 2.37 (m, 2H), 3,93 (t, J=5.7 Hz, 2H), 4,87 (kV, J=5.4 Hz, 1H), 5,13 (ABq, JAB=16,3 Hz, 2H), 6,78 (d, J=7,3 Hz, 1H), 6,93-7,05 (m, 2H), 7,12 (Shir.d, J=1.7 Hz, 2H), 7,26-7,28 (m, 2H). Analysis: Calculated for C17H15Cl2NO3: 57,97, N 4,29, N 3,98. Found: 57,96, N 4,17, N A 3.87. Reference example 49 The intermediate product 11578-71 6-Chloro-4-(3-Chlorobenzyl) -3,4-dihydro-2-(2-hydroxyethyl) -3-oxo-2H-1,4-benzoxazin Obtained from intermediate 11578-70 (reference example 35) by methods F and G with the alkylation of 3-chlorobenzylamino and selected from a total yield of 43% in the form of a white solid product, so pl. 90-92oC; IR (KBR) 3499, 1663, 1601, 1497, 1433, 1386, 1324, 1267, 1091, 1050, 933, 783 cm-1;1H NMR (CDCl3) 2,05 (Shir.s, 1H), 2,18-of 2.30 (m, 2H), 3,89-of 3.97 (m, 2H), a 4.86 (DD, J=7,7, and 5.5 Hz, 1H), 5,1 (s, 2H), for 6.81 (s, 1H), of 6.96 (d, J=1.4 Hz, 2H), 7,12-7,30 (m, 4H); MN+at m/z=352. Analysis: Calculated for C17H15Cl2NO3: 57,95, H 4,29, N 3,98. Found: 58,26, H 4,32, 3,89 N. Reference example 50 The intermediate product 11578-56 0.2 Hydrate 4-(3-Chlorobenzyl)-6-trifluoromethyl-3,4-dihydro-2-(2-hydroxyethyl)-3 - oxo-2H-1,4-benzoxazine Obtained from intermediate 12168-8-1 (reference example 29) by methods F and G with the alkylation of 3-chlorobenzylamino with abs, 868, 712 cm-1;1H NMR (CDCl3) 2,20-2,40 (m, 2H), 3,92 (t, J=6.3 Hz, 2H), is 4.93 (t, J=7,6 Hz, 1H), 5,14 (s, 2H), 7,07-7,16 (m, 3H), 7.23 percent-7,30 (m, 4H); MH+at m/z=386. Analysis: Calculated for C18H15ClF3NO30,2 H2O: 55,52, H 3,99, N OF 3.60. Found: 55,49, H Of 3.77, N Of 3.53. Reference example 51 The intermediate product 11578-77 6 Carbomethoxy-4-(3 - Chlorobenzyl)-3,4-dihydro-2-(2-hydroxyethyl)-3-oxo-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy)-6-carbomethoxy-3,4-dihydro-3-oxo-2H-1,4-benzoxazine by methods F and G with the alkylation of 3-chlorobenzylamino and allocated in the form of a white solid after trituration with hexane with a total yield of 70%, IR (KBR) 3468, 2952, 1688, 1452, 1285, 1260, 765 cm-1;1H NMR (COCl3) 1,61 (Shir.s, 1H plus HDO), 2,17-2,39 (m, 2H), 3,86 (s, 3H), 3,93 (t, J=5.7 Hz, 2H), 4,94 (DD, J=7,6, and 5.5 Hz, 1H), 5,16 (s, 2H),? 7.04 baby mortality (d, J=8,4 Hz, 1H), 7,15-7,33 (m, 4H), to 7.59 (d, J=1.8 Hz, 1H), 7,71 (DD, J=8,4, 1.8 Hz, 1H); MH+at m/z=376. Analysis: Calculated for C19H18ClNO50,1 H2O: 60,44, H A 4.86, N 3,71. Found: 60,26, H 4,60, N To 3.58. Reference example 52 The intermediate product 11578-47 4-(3-Chlorobenzyl)-3,4-dihydro-7-fluoro-2-(2 - hydroxyethyl)-3-oxo - 2H-1,4-benzoxazin Obtained from intermediate 11578-44 (reference example 36) by methods F is ejogo product, so pl. 79-82oC; IR (KBR) 3487, 1662, 1508, 1412, 1320, 1155, 1115, 1053, 854, 799 cm-1;1H NMR (CDCl3) 2,10 (t, J=4.3 Hz, 1H), 2,18-to 2.40 (m, 2H), 3,92 (kV, J=6.0 Hz, 2H), 4,88 (t, J=5.5 Hz, 1H), 5,10 (ABq, JAB=to 15.4 Hz, 2H), only 6.64 (dt, J=7,9, 2.7 Hz, 1H), 6,72-6,79 (m, 2H), 7,11 (Shir.s, 1H), 7,22-7,28 (m, 3H plus Cl3); MH+at m/z=336. Analysis: Calculated for C17H15ClFNO3: 60,81, H 4,50, N 4,17. Found: 60,74, H 4,69, N 4,28. Reference example 53 The intermediate product 11578-113 7-Fluoro-3,4-dihydro-4-(3-terbisil)-2-(2 - hydroxyethyl)-3-oxo-2H-1,4-benzoxazin Obtained from intermediate 11578-44 (reference example 36) by methods F and G with the alkylation of 3-formanilide and allocated in the form of a white solid product with a yield of 67%, so pl. 78-79oC; IR (KBR) 3497, 1661, 1509, 1415, 1252, 1159, 1119, 1057, 937, 857, 801 cm-1;1H NMR (CDCl3) 2,11 (t, J= 5,1 Hz, 1H), 2,17-2,39 (m, 2H), 3,92 (kV, J=5.5 Hz, 2H), 4,87 (DD, J=7,6, and 5.5 Hz, 1H), 5,13 (s, 2H), only 6.64 (dt, J=8,0, 2.7 Hz, 1H), 6.73 x-6,79 (m, 2H), 6,94 (t, J=8.5 Hz, 2H), 7,01 (s, J=7.7 Hz, 1H), 7,27-7,35 (m, 1H); MN+at m/z=320. Analysis: Calculated for C17H15F2NO3: 63,95, H 4,74, N 4,39. Found: 63,91, H 4,70, N 4,30. Reference example 54 The intermediate product 11578-114 7-Fluoro-3,4-dihydro-2-(2 - hydroxyethyl)-4-(2 - nitrobenzyl)-3-oxo-2H-1,4-benzoxazin Obtained from Helen in the form of a white solid after column chromatography with elution with ether to yield 76%. Part of this material have led from hexane, so pl. 123-124oC; IR (KBR) 3510, 1655, 1527, 1509, 1357, 1157, 1127, 1063, 801 cm-1;1H NMR (CDCl3) a 2.01 (t, J=5,1 Hz, 1H), 2,22-of 2.38 (m, 2H), 3,93 (kV, J=5.6 Hz, 2H), 4.92 in (DD, J=7,54, 5,63 Hz, 1H), 5,23 (ABq, JAB=16.5 Hz, 2H), 6,63 to 6.75 (m, 2H), 6,80 (DD, J=8,7, and 2.6 Hz, 1H), 7,51-of 7.60 (m, 2H), 8,12 (s, 1H), 8,15 (d, J=7,1 Hz, 1H); MN+at m/z=347. Analysis: Calculated for C17H15FN2O5: 58,96, H 4,37, N 8,09. Found: 58,81, H 4,37, N 8,01. Reference example 55 The intermediate product 11578-52 4-(3-Chlorobenzyl)-3,4-dihydro-2-(2-hydroxyethyl)-7-methyl-3-oxo-2H - 1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-7-methyl-3-oxo-2H-1,4-benzoxazine by methods F and G with the alkylation of 3-chlorobenzylamino and isolated with yields of 76% in the form of a white solid product after crystallization from a mixture of ether/hexane, so pl. 72-74oC; IR (KBR) 3418, 1679, 1512, 1402, 1292, 1061, 763 cm-1;1H NMR (CDCl3) 2,20-of 2.36 (m, 3H), and 2.27 (s, 3H), 3,92 (kV, J=5.6 Hz, 2H), a 4.83 (DD, J=7,6, and 5.5 Hz, 1H), 5,10 (ABq, JAB= 17,0 Hz, 2H), 6,68 to 6.75 (m, 2H), at 6.84 (s, 1H), 7,10-7,14 (m, 1H), 7,22-7,29 (m, 3H); MN+at m/z=332. Analysis: Calculated for C18H18ClNO30,2 N2ABOUT: WITH 64,46, H OF 5.53, N 4,18. Found: 64,48, H 5,51, N 4,06. Reference example 56 The intermediate product 115 the exact product 11578-30 (reference example 37) by methods F and G with the alkylation of 3-chlorobenzylamino with yields of 80%. This material was isolated as a white foam after flash chromatography using a mixture of ether/CH2Cl2(1/4); IR (KBr) 3430, 1694, 1592, 1480, 1434, 1380, 1285, 1059, 933, 843, 755 cm-1;1H NMR (CDCl3) 2,00 (t, J=5.4 Hz, 1H), 2,15-to 2.40 (m, 2H), 3,92-a 4.03 (m, 2H), equal to 4.97 (DD, J=8,8, 4,7 Hz, 1H), 5,09 (s, 2H), 6,72 (d, J= 2.3 Hz, 1H), was 7.08 (d, J=2.2 Hz, 1H), 7,20 (s, 1H), 7,26-7,30 (m, 2H plus Cl3). Analysis: Calculated for C17H14Cl3NO3: 52,81, H 3,65, N 3,62. Found: 52,90, H Of 3.73, N 3.46 In. Reference example 57 The intermediate product 10840-18 3,4-Dihydro-2-(2 - hydroxyethyl)-3-oxo-4-(2-picolyl)-2H-1,4-benzoxazin 2-(2-tert-Butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H-1,4-benzoxazin alkilirovanie 2-chloromethylpyridine way F and the crude product is freed from the protective groups by way H without treatment. Method H: tert-Butyldimethylchlorosilane product was dissolved in methanol and an excess of 6 N. HCl. The solution was stirred at room temperature for 1 h and then concentrated in vacuum. The aqueous residue was extracted with dichloromethane and the combined extract was washed with saline and dried over Na2SO4. Removal of solvent gave the crude product, which was purified flash chromatography and was identified with the release of 42% in the form of be, 1070, 749 cm-1;1H NMR (CDCl3) 2,18-of 2.38 (m, 2H), 2,44 (Shir.s, 1H), 3,92 (Shir.d, J=3.8 Hz, 2H), a 4.86 (DD, J=7,2, 5.8 Hz, 1H), 5,27 (ABq, JAB=16,3 Hz, 2H), 6.89 in-7,03 (m, 4H), 7,17-7,24 (m, 2H), to 7.64 (TD, J=7,7, 1.7 Hz, 1H), 8,56 (Shir.d, J=4.3 Hz, 1H); MH+at m/z=285. Analysis: Calculated for C16H16N2O3: 67,59, H 5,67, N 9,85. Found: 67,55, H Of 5.83, N 9,83. Reference example 58 The intermediate product 10840-22 3,4-Dihydro-2-(2 - hydroxyethyl)-3-oxo-4-(4 - picolyl)-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H-1,4-benzoxazine ways F and H alkylation with 4-chloromethylpyridine with the release of 12% and isolated in the form of a solid product, so pl. 153-154oC; IR (KBR) 3204, 1679, 1505, 1407, 1283, 1256, 1077, 1065, 750 cm-1;1H NMR (Cl3) 2,18-of 2.38 (m, 3H), 3,93 (Shir.kV, J=3,9 Hz, 2H), 4,88 (DD, J=7,7, a 5.4 Hz, 1H), further 5.15 (s, 2H), 6.73 x (d, J=7,6 Hz, 1H), 6,92 (TD, J=6,7, and 3.2 Hz, 1H), 6,98-7,06 (m, 2H), 7,15 (d, J=5, 9 Hz, 2H), 8,56 (DD, J=4,5, 1.5 Hz, 2H); MH+at m/z=285. Analysis: Calculated for C16H16N2O3: 67,59, H 5,67, N 9,85. Found: 67, 67, H 5,78, N 9,79. Reference example 59 The intermediate product 11578-99 3,4-Dihydro-2-(2-hydroxyethyl) -4-(4-phenylbenzyl)-3-oxo - 2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H - 1,4-answerdave product, so pl. 110-113oC; IR (KBR) 3350, 1683, 1500, 1400, 1304, 1275, 1247, 1051, 908, 758 cm-1;1H NMR (CDCl3) 2,21-of 2.38 (m, 2H), 3,94 (kV, J=5,48 Hz, 2H), 4,87 (DD, J= 7,5, 5,61 Hz, 1H), 5,20 (ABq, JAB=17,1 Hz, 2H), 6,93? 7.04 baby mortality (m, 4H), 7,30-7,40 (m, 3H), 7,43 (t, J=7,0 Hz, 2H), 7,55 (d, J=8.1 Hz, 4H); MN+at m/z=360. Analysis: Calculated for C23H21NO3: 76.86 EUROS, H OF 5.89, N 3,90. Found: 76,61, H 5,88, N 3,74. 4-Phenylbenzophenone was obtained by treatment of a solution of the appropriate alcohol (1 EQ) in CH2Cl2methanesulfonanilide (1.1 EQ) and triethanolamine (TEA) (1.1 EQ) at 0oC. This solution was stirred for 16 h, and treated with 3 N. HCl and the organic layer was separated. After drying, the solvent evaporated, receiving 4-phenylbenzophenone with the release of 64%, MN+at m/z=202. Reference example 60 The intermediate product 10840-185 3,4-Dihydro-2-(2-hydroxyethyl) -3-oxo-4-pentyl-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H - 1,4-benzoxazine by methods F and G with the alkylation of 1-chloropentane with the release of 32% and isolated in the form of a colorless oil; IR (KBR) 3424, 2956, 2932, 1680, 1500, 1272, 1062, 749 cm-1; 1H NMR (CDCl3) of 0.91 (t, J=6.8 Hz, 3H), 1,31-to 1.38 (m, 4H), 1,66 (Shir.t, J=5.5 Hz, 2H), 2,08-to 2.29 (m, 2H), 2,59 (Shir.s, 1H), a 3.87-of 3.94 (m, 2H), 4,69 (DD, J=7,3, 5.8 Hz, 1H), 6,92-was 7.08 (m, 4H).>Reference example 61 The intermediate product 11653-180 3,4-Dihydro-2-(2 - hydroxyethyl)-4-(3 - nitrobenzyl)-3-oxo-2H-1,4-benzoxazin Intermediate silylamines alcohol was obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H-1,4-benzoxazine way F alkylation with 3-nitrobenzylamine. The removal of the protective group to obtain the specified product was performed by method I. Method I: TBDMS-Protected benzoxazin (3.1 mmol) was stirred in the milk mixture with the Asón (12 ml), THF (2 ml) and2O (5 ml). This mixture was stirred for 18 h, the light receiving solution. Addition of water gave a white solid precipitate, which was separated by filtration and dried in vacuum at 80oFrom: T. pl. 103-104oC; MS (CI) MH+329; IR (KBr) 3490, 3087, 2947, 2879, 1685, 1663, 1607, 1593, 1466, 1280, 1168, 976 cm-1;1H NMR (CDCl3) of 8.15 (s, 1H), 8,13 (s, 1H), 7,54 (m, 2H),? 7.04 baby mortality (m, 2H), 6,95 (m, 1H), 6,79 (d, 1H, J=7,6 Hz), 5,28 (d, 1H, J=16.5 Hz), to 5.21 (d, 1H, J=16.5 Hz), the 4.90 (DD, 1H, J=5,5 and 7.6 Hz), 3,93 (m, 2H), to 2.29 (m, 2H), 2,13 (t, 1H, J=5.6 Hz). Analysis: Calculated for C17H16N2O5: 62,19, H 4,91, N 8,53. Found: 61,99, H 4,91, N 8,43. Reference example 62 The intermediate product 12279-11 3,4-Dihydro-2-(2-hydroxyethyl) -7-nitro-4-(4-nitrobenzyl)-3-oxo-2H-1,4-benzoxazin The obtained product with a yield of 42%, so pl. 100-104oC; MS (CI) MH+374; IR (KBr) 3395, 3113, 3089, 2939, 1683, 1598, 1432, 1395, 1142, 991, 914, 800, 544, 455 cm-1;1H NMR (CDCl3) 8,23 (d, 2H, J=8,70 Hz), 7,92 (d, 1H, J=2,42 Hz), the 7.85 (DD, 1H, J=cent to 8.85, of 2.54 Hz), 7,41 (d, 2H, J=at 8.60 Hz), 6,85 (d, 1H, J=8,93 Hz), and 5.30 (d, 2H, J=4,56 Hz), free 5.01 (DD, 1H, J=7,76, 5,11 Hz), of 3.96 (t, 2H, J=6,45 Hz)that is 2.30 (m, 2H), 1,79 (Shir.s, 1H). Analysis: Calculated for C17H15N3O70,7 H2O: 52,91, H 4,28, N 10,89. Found: 53,17, H 4,36, N 10,53. Reference example 63 The intermediate product 12279-18-AND 3,4-Dihydro-2-(2 - hydroxyethyl)-7-methoxy-4-(3 - nitrobenzyl)-3-oxo - 2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-7-methoxy-3 - oxo-2H-1,4-benzoxazine by methods F and I by alkylation of 3-nitrobenzylamine with 30% yield, so pl. 116-118o; MS (CI) MH+359; IR (KBr) 3306, 3086, 2926, 2872, 1628, 1595, 1476, 1309, 1290, 1255, 1087, 999, 713, 458 cm-1;1H NMR (DMSO-d6) to 8.14 (s, 1H), 8,11 (s, 1H), 7,63 (m, 2H), 6,97 (d, 1H, J= 8,93 Hz), of 6.66 (d, 1H, J=2,42 Hz), 6,53 (d, 1H, J=8,87 Hz), of 5.26 (s, 2H), 4,87 (DD, 1H, J=8,98, of 3.78 Hz), 4.72 in (t, 1H, J=5,23 Hz), 3,68 (s, 3H), 3,61 (m, 2H), 2,01 (m, 1H), 1,90 (m, 1H). Analysis: Calculated for C18H18N2O6: 60,33, H IS 5.06, N OF 7.82. Found: 59,96, H 5,08, N 7,62. Reference example 64 The intermediate product 12279-21 3,4-Dihydro-6-fluoro-2-(2-hydroxyethyl)-4-(3 - nitrobenzyl alkylation with 3-nitrobenzylamine with the release of 35%, so pl. 110-112oC; MS (CI) MN+347; IR (KBR) 3483, 3077, 2945, 2872, 1620, 1603, 1453, 1297, 1210, 1098, 979, 791, 742, 685, 470 cm-1;1H NMR (DCl3) is 8.16 (d, 1H, J=6.87 in Hz), 8,10 (s, 1H), 7,54 (m, 2H), 6.90 to (DD, 1H, J=to 3.73, 5,12 Hz), of 6.71 (m, 1H), 6,51 (DD, 1H, J=9,35, 2.76 Hz), 5,20 (d, 2H, J=5,46 Hz), to 4.87 (DD, 1H, J=7,60, 5,41 Hz), 3,93 (t, 2H, J=5,78 Hz), to 2.29 (m, 2H), 2,00 (m, 1H). Analysis: Calculated for C17H15FN2O5: 58,96, H 4,37, N 8,09. Found: 58,57, H 4,43, N 7,89. Reference example 65 The intermediate product 12279-13-AND 4-(3-Aminobenzyl)-3,4-dihydro-2-(2-hydroxyethyl) -3-oxo-2H-1,4-benzoxazin Obtained by dissolving the intermediate 1 butyldimethylsilyl-oxycoedone example 11653-180 (1,58 g, reference example 61) in ethanol (25 ml). Under stirring was added Fe powder (1.3 g), then concentrated HCl (12 ml). The reaction mixture was stirred at room temperature for 16 hours. The reaction mixture was filtered directly into ice water and was extracted with ethyl acetate. The extract was washed with saline and concentrated in vacuum. The resulting brown oil was washed with ether. After decanting the ether-wall of the flask scratched for the conversion of the oil in a pale brown solid product with a yield of 50%, so pl. 79oWith (dark), 85-90o(Melts); MS (CI) MH+299; It 1H, J=7,70 Hz), 7,10-6,20 (PTS.Shir.s, 2H), 6,98 (m, 2H), 6,93 (m, 2H), 6,63 (d, 1H, J=7.8 Hz), 6,56 (d, 2H, J=8.6 Hz), 5,10 (d, 1H, J=16.0 Hz), 5,00 (d, 1H, J=16.0 Hz), a 4.83 (DD, 1H, J=5,61, was 7.45 Hz), 3,91 (q, 2H, J=5.4 Hz), 3,85-3,20 (PTS.Shir.s, 1H), 2,23 (m, 2H). Analysis: Calculated for C17H18N2O30.1 G2O: 68,03, H 6,11, N WAS 9.33. Found: 67,93, H 6,05, N 9,05. Reference example 66 The intermediate product 10488-22 4-(3-Chlorobenzyl)-3,4-dihydro-2-(2-hydroxyethyl) -3-oxo-2H-1,4-benzoxazin Obtained by methods F and G with the alkylation of 3-nitrobenzylamine with the release of 55%. The product was isolated in the form of oil, which could crystallize from a mixture of diethyl ether/hexane, so pl. 63-67oC; MS (CI) MH+318; IR (KBr) 3477, 2927, 2863, 1688, 1599, 1576, 1503, 1466, 1217, 1109, 931, 903 cm-1;1H NMR (DCl3) 7,26 (m, 3H), 7,12 (m, 1H), 7,01 (m, 2H), 6,94 (m, 1H), PC 6.82 (m, 1H), 5,15 (d, 1H, J=16,3 Hz) 5,08 (d, 1H, J=16.2 Hz), is 4.85 (DD, 1H, J=5,5 and 7.6 Hz), 3,92 (d, 2H, J=4,9 Hz), 2,39-2,14 (Shir.m, 3H). Analysis: Calculated for C17H16ClNO3: 64,26, H 5,08, N OF 4.44. Found: 63,89, H 5,00, N 4,13. Reference example 67 The intermediate product 11653-85-IN-1 3,4-Dihydro-2-(2-hydroxyethyl) -7-nitro-4-(3-nitrobenzyl) -3-oxo-2H-1,4-benzoxazin Obtained from intermediate 11653-23 (reference example 31) by methods F and G with the alkylation of 3-nitrobenzyl the>1;1H NMR (DMSO-d6) 8,17 (s, 1H), 8,13 (s, 1H), 7,86 (s, 1H), 7,83 (d, 1H, J=2.5 Hz), the 7.65 (d, 1H, J= 7.8 Hz), 7,58 (t, 1H, J=7.8 Hz), was 7.08 (d, 1H, J=9,2 Hz), of 5.40 (d, 1H, J=16.5 Hz), 5,31 (d, 1H, J=16.6 Hz), 5,07 (DD, 1H, J=4,0, 9.0 Hz), of 4.57 (t, 1H, J= 5,2 Hz), 3,80 (m, 2H), 2,23 (m, 1H), 2,10 (m, 1H). Analysis: Calculated for C17H15N3O7: 54,69, H OF 4.05, N OF 11.26. Found: 54,57, H Of 4.04, N 11,08. Reference example 68 Intermediate 11653-S 4-(3-Chlorobenzyl)-3,4 - dihydro-2-(2-hydroxyethyl)-6 - nitro-3-oxo-2H-1,4-benzoxazin Obtained from intermediate 11653-33A (reference example 32) by methods F and G with the alkylation of 3-chlorobenzylamino exit 77%, so pl. >38oC (decomposition); MS (CI) MH+363; IR (KBR) 3855, 3745, 3423, 1686, 1590, 1522, 1448, 1389, 1343, 1267, 1056, 875, 778, 680 cm-1;1H NMR (CDCl3) to 7.93 (DD, 1H, J=2.5 a, 8,8 Hz), 7,78 (d, 1H, J=2.5 Hz), 7,30 (m, 3H), 7,19 (m, 1H), 7,10 (d, 1H, J=8,8 Hz), 5,20 (d, 1H, J=16,3 Hz), 5,14 (d, 1H, J=16.2 Hz), to 5.03 (DD, 1H, J=5,3 and 7.6 Hz), 3,93 (t, 2H, J=6.2 Hz), 2,41-2,19 (m, 2H), 1,71 (Shir.s, 1H). Analysis: Calculated for C17H15ClN2O5: 56,29, H 4,17, N 7,72. Found: 56,19, H 4,22, N 7,55. Reference example 69 The intermediate product 11653-142 3,4-Dihydro-2-(2 - hydroxyethyl)-7-nitro-4-(2-nitrobenzyl)-3-oxo - 2H-1,4-benzoxazin Obtained from intermediate 11653-23 (reference example 31) str 3122, 3088, 2942, 2892, 1693, 1600, 1530, 1501, 1420, 1390, 1254, 1059, 888, 727 cm-1;1H NMR (DMSO-d6) 8,24 (DD, 1H, J=1,2, 8.0 Hz), of 7.90 (d, 1H, J=2.5 Hz), 7,83 (DD, 1H, J=2,6, a 8.9 Hz), a 7.62 (m, 2H), 7,20 (d, 2H, J=8,9 Hz), 5,59 (d, 1H, J=18.2 Hz), 5,49 (d, 1H, J= 18.2 Hz), 5,16 (DD, 1H, J=4,4, 8.5 Hz), rate 4.79 (t, 1H, J=5,2 Hz), 3,66 (m, 2H), 2.05 is (m, 2H). Analysis: Calculated for C17H15N3O7: 54,69, H OF 4.05, N OF 11.26. Found: 54,81, H Is 4.03, N 11,07. Reference example 70 Intermediate 11653-44A 4-(2-Chlorobenzyl)-3,4 - dihydro-2-(2-hydroxyethyl)-6 - nitro-3-oxo-2H-1,4-benzoxazin Obtained from intermediate 11653-33A (reference example 32) by methods F and G by alkylation of 2-chlorobenzylchloride with the release of 23%, so pl. 108-110oC; MS (CI) MH+363; IR (KBR) 3520, 3092, 2984, 2938, 2889, 1906, 1775, 1588, 1474, 1446, 1316, 1253, 1185, 1127, 1112, 926, 680 cm-1;1H NMR (DMSO-d6) 7,94 (DD, 1H, J=2.5 a, 8,8 Hz), a 7.62 (d, 1H, J=2.5 Hz), 7,56 (d, 1H, J=7,6 Hz), 7,31 (m, 3H), 7,15 (d, 1H, J=7,3 Hz in), 5.25 (s, 2H), 5,16 (DD, 1H, J=4.2, and an 8.5 Hz), 4,78 (t, 1H, J=5,2 Hz), 3,63 (m, 2H), of 2.09 (m, 2H). Analysis: Calculated for C17H15ClN2O5: 56,29, H 4,17, N 7,72. Found: 56,19, H 4,10, N 7,58. Reference example 71 The intermediate product 11653-173 3,4-Dihydro-2-(2-hydroxyethyl) -4-(4-nitrobenzyl)-3-oxo-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2+329; IR (KBR) 3498, 3076, 2930, 2863, 1656, 1605, 1500, 1466, 1302, 1279, 1184, 1126, 982, 613 cm-1;1H NMR (DCl3) to 8.20 (DD, 2H, J=2,0 and 6.9 Hz), 7,40 (d, 2H, J=8,8 Hz), 7,03 (m, 2H), 6,93 (m, 1H), 6.75 in (d, 1H, J=7,6 Hz in), 5.25 (s, 2H), 4,88 (DD, 1H, J= 5,4, and 7.6 Hz), 3,93 (m, 2H), 2,38-2,17 (m, 2H), 2,10 (m, 1H). Analysis: Calculated for C17H16N2O5: 62,19, H 4,91, N 8,54. Found: 62,05, H 4,87, N 8,39. Reference example 72 The intermediate product 11653-170-A2 4-Benzyl-3,4-dihydro-2-(2-hydroxyethyl)-7-nitro-3-oxo-2H-1,4-benzoxazin Obtained from intermediate 11653-23 (reference example 31) by methods F and G with the alkylation benzylbromide with the release of 98%, so pl. 102-105oC; MS (CI) MH+329; IR (KBR) 3561, 3086, 3062, 2970, 2932, 2873, 1698, 1598, 1500, 1452, 1075, 985 cm-1;1H NMR (Dl3) 7,88 (d, 1H, J=2.5 Hz), 7,82 (DD, 1H, J=2,5, and 8.9 Hz), 7,34 (m, 3H), of 7.23 (m, 2H), of 6.96 (d, 1H, J=8,9 Hz), 5,23 (d, 1H, J=16.4 Hz), to 5.17 (d, 1H, J=16.4 Hz), 4,80 (DD, 1H, J=5,1, 7.9 Hz), of 3.94 (m, 2H), of 2.34 (m, 1H), 2,28 (m, 1H), 1,98 (t, 1H, J=5,5 Hz). Analysis: Calculated for C17H16N2O5: 62,19, H 4,91, N 8,53. Found: 61,81, H 4,63, N At 8.36. Reference example 73 The intermediate product 11653-174-AND 3,4-Dihydro-2-(2-hydroxyethyl) -4-(3-nitrobenzyl)-3-oxo-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H-1,4-benzoxazine C0, 3495, 3074, 2974, 2949, 2896, 1658, 1605, 1576, 1515, 1503, 1468, 1426, 1362, 1218, 1163, 902 cm-1;1H NMR (DMSO-d6) to 8.20 (DD, 1H, J=1,3, 8.1 Hz), to 7.67 (t, 1H, J=7,6 Hz), 7,56 (t, 1H, J=7,0 Hz), to 7.15 (d, 1H, J=7,0 Hz), was 7.08 (d, 1H, J= 7,7 Hz), 6,99 (m, 1H), 6,92 (d, 2H, J=3,7 Hz), 5,49 (d, 1H, J=18.2 Hz), 5,42 (d, 1H, J=18,1 Hz), 4,94 (DD, 1H, J=4,1, 9.0 Hz), 4.72 in (t, 1H, J=5,2 Hz), 3,63 (m, 2H), 2,00 (m, 2H). Analysis: Calculated for C17H16N2O5: 62,19, H 4,91, N 8,53. Found: 61,85, H 4,89, N Of 8.37. Reference example 74 The intermediate product 10508-23-AND 4-Benzyl-3,4-dihydro-2-(2-hydroxyethyl)-3-oxo-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H - 1,4-benzoxazine by methods F and G with the alkylation benzylchloride with a total yield of 49% and crystallized from a mixture of ether/hexane with the formation of white solid product, so pl. 83-85,5oC; IR (KBR) 3213, 1680, 1505, 1399, 1250, 1050, 753 cm-1;1H NMR (DCl3) 2,17-of 2.38 (m, 3H), 3,92 (kV, J=5.7 Hz, 2H), 4,84 (DD, J=7,5, and 5.6 Hz, 1H), 5,16 (s, 2H), 6,86-7,03 (m, 4H), 7,21-7,37 (m, 5H); MH+at m/z=284. Analysis: Calculated for C17H17NO3: 72,07, H 6,05, N 4,94. Found: 72,08, H 6,20, N 4,87. Reference example 75 The intermediate product 10508-25-AND 3,4-Dihydro-2-(2 - hydroxyethyl)-4-(2-methoxybenzyl) -3-oxo-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsilyl kibesillah alcohol with a total yield of 47% in the form of a light yellow resinous product after flash chromatography with elution with a mixture of ethyl acetate/hexane, IR (net) 3436, 2941, 1583, 1683, 1501, 1466, 1403, 1281, 1246, 1113, 1052, 751 cm-1; 1H NMR (CDCl3) 2,18-of 2.36 (m, 2H), 2,39 (Shir.t, J= 6.0 Hz, 1H), 3,90 (s, 3H), 3,92 (Shir.kV, J=5.5 Hz, 2H), around 4.85 (DD, J=7,4, 5.7 Hz, 1H), further 5.15 (s, 2H), for 6.81-7,03 (m, 7H), 7.23 percent (TD, J=8,3, 1.7 Hz, 1H); MH+at m/z=314. Analysis: Calculated for C18H19NO40,2 H2O: 68,21, H 6,17, N 4,42. Found: 68,36, H 6,18, N 4,36. Reference example 76 The intermediate product 10508-22-AND 3,4-Dihydro-2-(2 - hydroxyethyl)-4-(3-methoxybenzyl) -3-oxo-2H-1,4-benzoxazin Obtained by methods F and G by alkylation of 2-methoxybenzylamine with a total yield of 49% in the form of a light viscous resin after flash chromatography with elution of 25-50% ethyl acetate in hexane), IR (net) 3433, 2941, 1683, 1583, 1501, 1466, 1403, 1262, 1152, 1052, 753 cm-1; 1H NMR (CDCl3) 2,17-is 2.37 (m, 3H), of 3.77 (s, 3H), 3,91 (Shir.kV, J=5.3 Hz, 2H), 4,84 (DD, J=7,5, and 5.6 Hz, 1H), 5,12 (ABq, JAB=17 Hz, 2H), 6,76-7,03 (m, 7H), from 7.24 (TD, J=7,6, and 0.98 Hz, 1H); MH+at m/z=314. Analysis: Calculated for C18H19NO4: 68,99, H 6,11, N 4,47. Found: 68,54, H 6,14, N 4,33. Reference example 77 The intermediate product 10508-82-AND 4-(3-Benzyloxybenzyl) -3,4-dihydro-2-(2-hydroxyethyl) -3-oxo-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H - 1,4-benzoxazin the form of a viscous liquid after flash chromatography with elution 30-100% ethyl acetate in hexane; IR (Cl3) 3434, 2933, 1681, 1500, 1401, 1256, 1054, 751 cm-1;1H NMR (CDCl3) 1.77 in (lat. s, 1H plus HDO), 2,20-of 2.34 (m, 2H), 3,91 (t, J=5.5 Hz, 2H), 4,82 (DD, J= 7,5, 5.7 Hz, 1H), 5,02 (s, 2H), 5,11 (ABq, JAB=16.0 Hz, 2H), 6,85-7,01 (m, 7H), 7,22-7,41 (m, 6N); MN+at m/z=390. Analysis: Calculated for C24H23NO4: 74,02, H 5,95, N OF 3.60. Found: 73,61, H 6,03, N 3,55. Reference example 78 The intermediate product 10508-84-A1 3,4-Dihydro-2-(2-hydroxyethyl) -4-(1-naphthylmethyl)-3-oxo-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy)-3,4-dihydro-3-oxo-2H-1,4-benzoxazine by methods F and G with the alkylation of 1-chloromethylation with a total yield of 42%. The crude product was led from a mixture of ether/ethyl acetate/hexane, obtaining a white solid product, so pl. 100-104oC; IR (KBR) 3435, 2896, 1668, 1504, 1414, 1253, 1132, 1068, 768, 758 cm-1;1H NMR (CDCl3) 1,92 (Shir.s, 1H plus HDO), and 2.26 is 2.44 (m, 2H), 3.96 points (t, J=5.6 Hz, 2H), 4,94 (DD, J=7,5, and 5.6 Hz, 1H), 5,62 (ABq, JAB=16,9 Hz, 2H), 6,72 (DD, J=8.0 a, 1,1 Hz, 1H), 6,84 (TD, J= 8,1, 1.5 Hz, 1H), of 6.96-7,11 (m, 3H), of 7.36 (t, J=7,4 Hz, 1H), 7,54-to 7.64 (m, 2H), 7,78 (d, J=8,2 Hz, 1H), 7,92 (d, J=7.8 Hz, 1H), 8,04 (d, J=8,1 Hz, 1H); MN+at m/z=334. Analysis: Calculated for C21H19NO3: 75,66, H 5,74, N 4,20. Found: 75,56, H 5,80, N 4,14 Reference example 79 The intermediate product 10508-80-1 3,4-Detil) -3,4-dihydro-3-oxo-2H-1,4-benzoxazine by methods F and G by alkylation of 2-chloromethylation with a total yield of 81%. The crude product was led from a mixture of ether/hexane, getting a white solid, so pl. 81-87oC; IR (KBR) 3459, 2940, 1665, 1500, 1403, 1277, 1242, 1066, 746 cm-1;1H NMR (CDCl3) of 2.23-2.40 a (m, 3H), of 3.95 (t, J= 5.4 Hz, 2H), 4,90 (DD, J=7,6, and 5.6 Hz, 1H), 5,32 (ABq, JAB=16.1 Hz, 2H), 6.87 in-7,03 (m, 4H), 7,38 (d, J=8.5 Hz, 1H), 7,43-of 7.48 (m, 2H), to 7.67 (s, 1H), 7,75-to 7.84 (m, 3H); MN+at m/z=334. Analysis: Calculated for C21H19NO3: 75,66, H 5,74, N 4,20. Found: 75,65, H 5,71, N Was 4.02. Reference example 80 The intermediate product 10508-79 4-(5-Chloro-2-thienylmethyl) -3,4-dihydro-2-(2-hydroxyethyl) -3-oxo-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H-1,4-benzoxazine by methods F and G with the alkylation of 5-chloro-2-(chloromethyl)thiophene and highlighted with a total yield of 83% in the form of a light yellow viscous oil after flash chromatography using 30-50% ethyl acetate in hexane; IR (Cl3) 3418, 2943, 1677, 1500, 1400, 1278, 1062, 750 cm-1;1H NMR (DCl3) 2,11 of-2.32 (m, 3H), 3,89 (kV, J=5.4 Hz, 2H), 4,78 (DD, J=7,6, and 5.5 Hz, 1H), further 5.15 (ABq, JAB= 16.0 Hz, 2H), 6,74 (d, J=3,7 Hz, 1H), at 6.84 (d, J=3,7 Hz, 1H), 7,01-was 7.08 (m, 4H); MN+at m/z=324. Analysis: Calculated for C15H14ClNO3S 0,25 H2O: 54,88, H OF 4.45, N 4,27, S 9,77. Found: 54,86, H To 4.41, N Of 4.04, S 9,87. Reference example is eventout From 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H-1,4-benzoxazine by methods F and G by alkylation of 4-(methoxycarbonyl)benzylchloride received alcohol in the form of a white solid product with a yield of 65%, so pl.=94-95o;1H NMR (Dl3) 8,00 (d, J=8,4 Hz, 2H), 7,30 (d, J=8,4 Hz, 2H), 6,95? 7.04 baby mortality (m, 2H), 6.89 in (dt, J=2,1, 8.0 Hz, 1H), 6,77 (DD, J=7,8, 1.5 Hz, 1H), 5,20 (s, 2H), a 4.86 (DD, J=5,4, and 7.7 Hz, 1H), 3,82-of 3.96 (m, 5H to 3H singlet at 3,89), 2,16-is 2.37 (m, 3H, one of which exchange).13With NMR (CDCl3) 166,8, 166,5, 144,1, 141,1, 130,1 (CH), 129,4, 128,4, 126,3 (SN), TO 124.2 (CH), 122,8 (CH), 117,3 (SN), THE 115.2 (CH), 75,1 (CH), 58,7 (CH2), 52,0 (CH3), 45,1 (CH2), 33,1 (CH2). IR 3450-3500 (W), 1719, 1660 cm-1. MS 342 (MN+), 324 (M-HE)+, 310 (M-OMe)+. Analysis: Calculated for C19H19NO5: 66,85, H 5,61, N 4,10. Found: 66,48, H 5,47, N 3,97. Reference example 82 The intermediate product 11758-93-2A Methyl-3-[3,4-dihydro-2 -(2-hydroxyethyl)-3-oxo - 2H-1,4-benzoxazin-4-yl]methylbenzoate Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H-1,4-benzoxazine by methods F and G with the alkylation of 3-(methoxycarbonyl)benzylchloride and allocated in the form of a white powder with a yield of 87%, so pl. 73-75o;1H NMR (CDCl3) 7,92-to 7.95 (m, 2H), 7,38-the 7.43 (m, 2H), of 6.96-7.03 is (m, 2H), 6,91 (dt, J=2,3, 7,3 Hz, 1H), for 6.81 (the Dean of metabolic hydrogen).13With NMR (CDCl3) 166,9, 166,7, 144,2, 136,5, 130,9 (CH), 130,7, 129,1 (CH), 128,7 (CH), 128,5, OF 127.7 (CH), 124,3 (CH), 122,9 (CH), 117,4 (CH), 115,4 (CH), 75,3 (SN), OF 58.9 (CH2), 52,2 (CH2), 45,1 (CH2), 33,3 (CH2). IR 3569, 2948, 1709, 1676, 1502 cm-1. MS 342 (MN+). Analysis: Calculated for C19H19NO5: 66,85, H 5,61, N 4,10. Found: 66,37, H 5,62, N 3,97. Reference example 83 The intermediate product 11758-82-2 Ethyl-2-[3,4-dihydro-2 -(2-hydroxyethyl)-3-oxo-2H-1,4-benzoxazin-4-yl]methylbenzoate Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H - 1,4-benzoxazine by methods F and G by alkylation of 2-(methoxycarbonyl)benzylchloride and allocated in the form of a white solid product with a total yield of 38%, so pl. 114-115,5oWith (ethyl acetate/hexane). 1H NMR (CDCl3) 8,08 (DD, J=1,4, and 7.8 Hz, 1H), 7,40 (dt, J=1,3, 7.5 Hz, 1H), 7,33 (Shir.t, J= 7,6 Hz, 1H), 6,97-7,06 (m, 3H), 6.89 in (dt, J=1,9, 7.5 Hz, 1H), 6,74 (d, J=8.0 Hz, 1H), 5,63 (d, J=18,0 Hz, 1H), 5,54 (d, J=18,0 Hz, 1H), 4,88 (DD, J=5,7, 7,4 Hz, 1H), to 4.41 (q, J=7,1 Hz, 2H), 3,90-3,95 (m, 2H), 2,23 to 2.35 (m, 2H), USD 1.43 (t, J=7,1 Hz, 3H). IR 3450-3550 (W), 1675, 1502 cm-1. MS 356 (MN+). Analysis: Calculated for C20H21NO5: 67,59, H 5,96, N 3,94. Found: 67,29, H 5,97, N 3,83. Reference example 84 The intermediate product 11758-190 4-(3-Chlorobenzyl)-3,4 - dihydro-2-(2-hydroxide the R. Gawinecki, Org. Prep. Proc. Int., 1985, 17, 409-423. A solution in ethanol of this nitropyridine (1 EQ) and NaOAc (1 EQ) was restored with 10% Pd/C (10% wt./wt.) in an atmosphere of hydrogen at 3,515 ATM (50 psig) within 4 h of Crude 3-amino-4-hydroxypyridine was dissolved in DMF (5 ml) and was treated with NaH (1.2 EQ). This mixture is then treated --bromo--butyrolactone (1.2 EQ) at room temperature under nitrogen atmosphere. After stirring at room temperature for 24 h, the solution in DMF) was treated with imidazole (1.2 EQ) and tert-butyldimethylsilyl (1.2 EQ). This solution was stirred for 16 h and then extinguished H2O. the Aqueous solution was extracted with ethyl acetate and the combined extract was washed H2O and dried over MgSO4. The solution in ethyl acetate was filtered through SiO2and concentrated in vacuum, obtaining the intermediate similarcanadian with the release of 14%. This material alkilirovanie method F 3-chlorobenzylamino and then processed triperoxonane acid (TFU) (20% vol. /about.) in l3for removal of the protective group receiving alcohol with a yield of 41% in the form of a white crystalline solid; IR (KBR) 3519, 1664, 1393, 1320, 1192, 1082, 1054, 868 cm-1;1H NMR (DMSO-d6)1,97-of 2.09 (m, 2H), to 3.58-3,62 (m, 2H), and 4.75 (t, J=5.0 Hz, 1H), 5,10 (DD, J=8,5, 4,2 Hz, 1H), total of 5.21 (s, 2H), 7,07 (d, J=R 85 The intermediate product 11721-108-1 3,4-Dihydro-2- (2-hydroxyethyl) - [4- (3-thienylmethyl)]-3-oxo-2H-1,4-benzoxazin Tributylphosphine (1.5 EQ) and 1,1'-(azodicarbon)piperidine (1.5 EQ) was added to a solution of 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H-benzoxazine (1 EQ) in CH2Cl2at room temperature. Was added dropwise 3-thiophenemethyl (1.5 EQ) and the mixture was stirred for 16 hours at room temperature. Added hexane and the mixture was filtered and concentrated in vacuum. The oily residue was purified column chromatography using 1-2% mixture of ethyl acetate/CH2CL2as eluent, getting alkilirovanny intermediate product as a yellow oil: MN+at m/z=404. Alkilirovanny intermediate product was treated according to method G, getting mentioned in the title compound in the form of a light oil. IR (net) 3427, 3101, 1681, 1500, 1060, 750 cm-1;1H NMR (CDCl3) of 2.1-2.4 (m, 2H), 3,8-4,0 (m, 2H), 4,15 (kV, 1H), 4,80 (t, 1H), total of 5.21 (s, 2H), 7,07 (m, 5H), and 7.1 (m, 1H), 7,25 of 7.3 (m, 1H); MH+at m/z=289. Reference example 86 Intermediate 11653-24A 4-(2-Chlorobenzyl)-3,4-dihydro-2-(2-hydroxyethyl)-3-oxo-7-nitro-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -th product; so pl. 106-108oC; MS (CI) 363 (MN+); IR (KBR) 3268, 3122, 3088, 3068, 2969, 2937, 2881, 1888, 1794, 1571, 1478, 1210, 1148, 1135, 1116, 972, 926, 864, 705, 626, 475 cm-1;1H NMR (CDCl3/TMS) of 7.90 (d, 1H, J=2,42 Hz), to 7.84 (DD, 1H, J=of 2.51, 8,91 Hz), was 7.45 (d, 1H, J=to 7.77 Hz), 7,20 (m, 2H), 6,95 (d, 1H, J=7,52 Hz), for 6.81 (d, 1H, J=8,90 Hz), from 5.29 (s, 2H), 5,00 (DD, 1H, J=5,13, of 7.90 Hz), of 3.95 (q, 2H, J=5,51 Hz), 2,30 (Shir.m, 2H), 1,86 (t, 1H, J=5,47 Hz). Analysis: Calculated for C17H15ClN2O5: 56,29, H 4,17, N 7,72. Found: 56,25, H 4,24, N 7,60. Reference example 87 Intermediate 11653-35V 4-(3-Chlorobenzyl)-3,4-dihydro-2-(2-hydroxyethyl)-3-oxo-7-nitro-2H-1,4-benzoxazin Obtained from 2-(2-tert-butyldimethylsiloxy) -3,4-dihydro-3-oxo-2H - 1,4-benzoxazine by methods F and G with the alkylation of 3-chlorobenzylamino in the form of a yellow solid product; so pl. 100-102,5oC; MS (CI) 363 (MN+); IR (KBR) 3512, 3090, 3058, 2980, 2939, 2886, 1888, 1600, 1518, 1498, 1475, 1443, 1431, 1278, 1204, 1107, 1080, 1020, 863, 681, 602, 452 cm-1;1H NMR (CDCl3/TMS) 7,89 (d, 1H, J=2,46 Hz), to 7.84 (DD, 1H, J=2,53, 8,84 Hz), 7,27 (m, 3H), 7,10 (m, 1H), 6.90 to (d, 1H, J=cent to 8.85 Hz) to 5.17 (s, 2H), 4,99 (DD, 1H, J= 5,13, the 7.85 Hz), of 3.94 (m, 2H), 2,35 (m, 1H), 2,24 (m, 1H), of 1.92 (t, 1H, J= 5,40 Hz). Analysis: Calculated for C17H15ClN2O5: 56,29, H 4,17, N 7,72. Found: 56,25, H 4.09 To, N 7,63. Reference example 88 The intermediate product 10840-117-1 knogo product 11653-23 (reference example 31) by methods F and G alkylation with methyl iodide. Analysis: Calculated for C11H13NO30,9 N2O: 62,14, H 6,41, N 6,59. Found: 62,21, H 6,27, N 6.42 Per. Connection 1 2-[2-[4-(tert-Butoxycarbonylamino) phenoxy]ethyl]-4-(3-Chlorobenzyl) -3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Method J: Intermediate product 10488-22 (of 7.65 g, 1 EQ, reference example 66) was dissolved in THF. Added triphenylphosphine (0.5 g, 1.1 EQ) and 4-(N-tert-butoxycarbonyl)aminomethylphenol (0,38 g, 1 EQ), then was added dropwise diethylazodicarboxylate (0,303 ml, 1.1 EQ). The reaction mixture was stirred at the boiling temperature for 48 h and concentrated in vacuum. The residue is triturated with diethyl ether and the precipitate was removed by filtration. The product was isolated from the filtrate flash chromatography, elwira a mixture of ethyl acetate/hexane. The fractions containing the product, was led from a mixture of ethyl acetate/hexane, obtaining a white powder with a yield of 50%, so pl. 99-100oC; IR (KBR) 3386, 2981, 1692, 1613, 1501, 1393, 1366, 1248, 1171, 1053, 862, 752, 388 cm-1;1H NMR (Dl3) 7,29 to 7.2 (m, 3H), 7,21 (d, J=8.6 Hz, 2H) 7,13 (m, 1H),? 7.04 baby mortality-6,91 (m, 3H), to 6.88 (d, J=8.6 Hz, 2H), PC 6.82 (DD, J=8 and 1.4 Hz), to 5.17 (d, J=16 Hz, 1H) 5,08 (d, J=16 Hz, 1H), 4,94 (DD, J=9,2, 4.0 Hz, 1H), 4,75 (Shir.s, 1H), 4,24 (m, 4H), of 2.56 (m, 1H), 2,34 (m, 1H), 1,46 (s, N). Analysis: Calculated for C29H31ClN2ABOUT5: 66,60-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> How To: Compound 1 was dissolved in isopropyl alcohol containing an excess of Hcl (gas) (0.2-0.3 g/ml) and was stirred at room temperature for 2 hours, the Reaction mixture was filtered and the solid product washed with diethyl ether, obtaining white solid with a yield of 87%, so pl. 194-200oC (decomposition); MS (CI) MH+422; IR (KBr) 2930, 1609, 1503, 1404, 1306, 1283, 1248, 1182, 1111, 1051, 833 cm-1;1H NMR (DMSO-d6) 8,45-8,24 (Shir.s, 2H), 7,42 (d, 2H, J=8.6 Hz), 7,35 (m, 2H), 7,22 (d, 1H, J= 6,8 Hz), 7,05 (m, 5H), 5,23 (d, 1H, J=16.5 Hz), 5,13 (d, 1H, J=16.5 Hz), 5,00 (DD, 1H, J=4.2, and 8.6 Hz), 4,22 (m, 2H), 3,94 (Shir.t, 2H, J=2,5 Hz), 3,39 (Shir.s, 2H), 2.40 a (m, 1H), 2,25 (m, 1H). Analysis: Calculated for C24H22lN2O3HCl: 62,89, H Is 5.06, N 6,11. Found: 62,49, H To 5.21, N 6,03. Connection 3 2-[2-[4-(tert-Butoxycarbonylamino) phenoxy] ethyl] -4-(4 - chlorbenzyl)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained by method J using intermediate product 10353-28-1 (reference example 41), modified by stirring at room temperature for 48 hours Product in the form of a white solid is obtained with a yield of 54%, so pl. 121-122,5oC; IR (KBR) 3400, 2977, 2931, 1690, 1613, 1516, 1503, 1468, 1436, 1395, 1366, 1301, 1277, 1248, 1171, 1094, 1053, 1014, 753 cm-1;1H NMR (CDCl3) 7,33-7,22 (m, (m, 1H), 1,47 (s, N). Analysis: Calculated for C29H31ClN2O5: 66,60, H 5,97, N ARE 5.36. Found: 66,48, H 5,86, N, 5,32. Connection 4 2-[2-[4-(Aminomethyl)phenoxy] ethyl]-4-(4-chlorbenzyl) -3,4-dihydro-3-oxo - 2H-1,4-benzoxazin < / BR> Obtained by the method For using the compound 3. Solution in a mixture of HCl/isopropanol evaporated in vacuum and the white solid product was isolated by crystallization from a mixture of CH2CL2/diethyl ether to yield 76%, so pl. 200-201oC; IR (KBR) 3480, 3360, 3235, 2910, 2878, 1681, 1609, 1519, 1503, 1465, 1401, 1281, 1243, 1183, 1110, 1023, 913, 830, 797, 749, 569, 529, 530 cm-1;1H NMR (DMSO-d6) 8,18 (Shir.s, 3H), 7,40 (m, 4H), 7,30 (d, J=8.6 Hz, 2H), 7,02 (m, 6N), to 5.21 (d, J=16,8 Hz, 1H), 5,12 (d, J=16,8 Hz, 1H), to 4.98 (DD, J= 9,2, 4,4 Hz, 1H), 4,23 (m, 2H), 3.96 points (m, 2H), 2,39 (m, 1H), 2,25 (m, 1H). Analysis: Calculated for C24H23ClN2O3HCl 0.5 H2O: 61,54, H 5,38, N 5,98. Found: 61,30, H 5,33, N 5,90. Connection 5 2-[2-[4-(2-(tert - Butoxycarbonylamino)ethyl) phenoxy]ethyl]-4-(4 - chlorbenzyl)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Method L: Intermediate alcohol 10353-28-1 (0.6 g, 1 EQ, reference example 41) was dissolved in dry benzene (6 ml) and treated with tributylphosphine (0.63 ml, 1.5 EQ) and BOC-protected 4-(2-amino-ethyl)phenol (0.66 g, 1.5 EQ). The resulting solution obliterating the mixture was heated to room temperature. After 20 h the reaction mixture was diluted with diethyl ether and the white precipitate was separated by filtration. The filtrate was washed 2 N. NaOH and concentrated. The product was isolated by flash chromatography, elwira a mixture of acetone/hexane. Recrystallization from a mixture of ethyl acetate/hexane gave the product as a white solid with a yield of 72%, so pl. 108-109oC; MS (CI) 537 (MN+); IR (KBR) 3378, 2979, 1798, 1609, 1515, 1500, 1395, 1368, 1246, 1171, 1061, 816, 749 cm-1; 1H NMR (CDCl3) 7,39 (d, J= 8.5 Hz, 2H), 7,18 (d, J=8.5 Hz, 2H), 7,11 (d, J=8.7 Hz, 2H),? 7.04 baby mortality-to 6.80 (m, 4H), 6,86 (d, J=8.7 Hz, 2H), 5,14 (d, J=16.4 Hz, 1H), 5,11 (d, J= 16.4 Hz, 1H), is 4.93 (DD, J=9,5, a 4.1 Hz, 1H), to 4.52 (Shir.s, 1H), 4,23 (m, 2H), 3,34 (m, 2H), 2,74 (apparent t, J=7,1 Hz, 2H), has 2.56 (m, 1H), 2,33 (m, 1H), 1,44 (s, N). Analysis: Calculated for C30H33lN2ABOUT5: 67,09, H IS 6.19, N 5,22. Found: 66,88, H 6,07, N 5,22. Connection 6 2-[2-[4-(2-Aminoethyl) phenoxy] ethyl] -4-(4-chlorbenzyl) -3,4-dihydro-3-oxo - 2H-1,4-benzoxazin < / BR> Obtained by the method For using the connection 5. After 18 h the solution in a mixture of HCl/isopropanol evaporated in vacuum and the product was isolated as a white solid by crystallization from a mixture of CH2CL2/diethyl ether with a yield of 43%, so pl. 174-176oC; IR (KBr) 3415, 2933, 1681, 1609, 1503, 1465, 1401, 1279, 1241, 1065, 824, 789, 488, 428, 415 cm-1;1<=a 16.8 Hz, 1H), 5,13 (d, J= 16,8 Hz, 1H), equal to 4.97 (DD, J=9,2, a 4.1 Hz, 1H), 4,19 (m, 2H), 2,99 (m, 2H), 2,80 (m, 2H), of 2.38 (m, 1H), 2,24 (m, 1H). Analysis: Calculated for C25H25ClN2O3HCl: 63,43, H 5,54, N Of 5.92. Found: 63,17, H 5,47, N Of 5.82. Connection 7 2-(2-[3-(2-tert - Butoxycarbonylamino)phenoxy] ethyl} -4-(4-chlorbenzyl) -3,4-Dihydro-3-oxo-2H - 1,4-benzoxazin < / BR> Obtained by method J using intermediate product 10353-28-1 (reference example 41), modified by stirring at room temperature for 20 hours, the Product obtained in the form of a white solid with a yield of 30%; so pl. 97-98,5oC; IR (KBr) 3368, 3066, 3050, 2981, 2940, 1680, 1602, 1594, 1522, 1503, 1466, 1447, 1399, 1364, 1267, 1175, 1113, 1052, 1013 cm-1;1H NMR (CDCl3) 7,32-7,16 (m, 5H), 7,05-6,89 (m, 3H), 6,86-of 6.73 (m, 4H), 5,16 (d, J= 17.6 Hz), 5,09 (d, J=17.6 Hz), is 4.93 (DD, J=6,7, 5.0 Hz), 4,55 (m, 1H), 4,23 (m, 2H), 3,38 (m, 2H), 2,78 (apparent t, J=7.2 Hz, 2H), 2,58 (m, 1H), 2,33 (m, 1H), USD 1.43 (s, N). Analysis: Calculated for C30H33lN2ABOUT5: 67,09, H IS 6.19, N 5,22. Found: 67,14, H 6,21, N 5,16. Compound 8 2-[2-[3-(2-Aminoethyl) phenoxy] ethyl] -4-(4-chlorbenzyl) -3,4-dihydro-3-oxo-2H - 1,4-benzoxazin < / BR> Obtained by the method For using the compound 7. Solution in a mixture of HCl/isopropanol evaporated in vacuum after 2.5 h and the product vyd is approximately 72%, so pl. 155-156oC; IR (KBR) 3400, 3052, 2940, 1683, 1605, 1501, 1399, 1301, 1248, 1162, 1094, 1053, 751 cm-1;1H NMR (DMSO-d6) 7,40 (d, J=8,4 Hz, 2H), 7,35-of 7.23 (m, 3H), 7,02 (m, 4H), 6,86 (m, 3H), and 5.2 (d, J=17,0 Hz, 1H), 5,14 (d, J=17 Hz, 1H), 5,15-3,30 (PTS.Shir.s, 4H), 4,22 (m, 2H), 3,05 (m, 2H), and 2.83 (m, 2H), 2.40 a (m, 1H), 2,25 (m, 1H). Analysis: Calculated for C25H25ClN2O3WITH2H2O40.75 H2O: FROM 60,00, H 5,32, N IS 5.18. Found: 60,11, H 5,08, N Is 5.06. Connection 9 2-[2-[3-(tert - Butoxycarbonylamino)phenoxy] ethyl]-4-(4-chlorbenzyl) -3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained by method J using intermediate product 10353-28-1 (reference example 41), modified by stirring at room temperature for 24 hours Product obtained with the yield of 50%. Rubbing with hot diethyl ether gave a white solid product, so pl. 114-116oC; IR (KBR) 3365, 2985, 1686, 1600, 1526, 1503, 1451, 1395, 1366, 1268, 1173, 1129, 1067, 1052, 843, 787, 760 cm-1;1H NMR (CDCl3) 7,29 (d, J=8,9 Hz, 2H), 7.23 percent (d, J=8,4 Hz, 1H), 7,19 (d, J=8,9 Hz, 2H), 7,15-of 6.78 (m, 7H), of 5.15 (d, J= 16,8 Hz, 1H), 5,1 (d, J=16,8 Hz, 1H), is 4.93 (DD, J=9,2, 4,2 Hz, 1H), 4,82 (Shir.s, 1H), 4,37 is 4.13 (m, 4H), 2.57 m (m, 1H), 2,34 (m, 1H), 1,46 (s, N). Analysis: Calculated for C29H31ClN2O5: 66,60, H 5,97, N ARE 5.36. Found: 66,62, H 5,90, N 5,33. Connection 10 2K using compound 9. Solution in a mixture of HCl/isopropanol evaporated in vacuum after 24 h and the product was isolated with a yield of 30% conversion to the oxalate salt, followed by rubbing with hot CH2Cl2so pl. 127-129oC; IR (KBR) 3446, 3053, 1501, 1466, 1401, 1248, 797, 747, 700, 486, 428 cm-1;1H NMR (DMSO-d6) 8,20 (Shir.s, 1H), 7,40 (d, J=8,4 Hz, 2H), was 7.36 (d, J=8.0 Hz, 1H), 7,31 (d, J=8,4 Hz, 2H), total of 5.21 (d, J=and 17.2 Hz, 1H), 5,13 (d, J=and 17.2 Hz, 1H), to 4.98 (DD, J=9,2, 4,2 Hz, 1H), 5,15-4,10 (PTS. Shir.s, 3H), 4,22 (m, 2H), 4,01 (s, 2H), 2,45 (m, 1H), and 2.27 (m, 1H). Analysis: Calculated for C24H23ClN2O3WITH2H2O41,5 H2O: 57,83, H 5,23, N 5,19. Found: 58,06, H Is 4.85, N 5,20. Connection 11 2-[2-[3-(tert - Butoxycarbonylamino)phenoxy] ethyl]-4-(2-Chlorobenzyl)-3,4-dihydro-3-oxo-2H - 1,4-benzoxazin < / BR> Obtained by method J using intermediate product 9086-189-1 (reference example 42), but without chromatography. The product was isolated by precipitation from aqueous methanol and podslushivaet by adding dropwise 2 N. NaOH and then recrystallize from a mixture of Meon/water, yield 84%, so pl. 115-116oC; MS (CI) 523 (MN+); IR (KBR) 3357, 2979, 1686, 1611, 1586, 1526, 1505, 1466, 1449, 1395, 1368, 1285, 1252, 1165, 1052, 749 cm-1;1H NMR (DCl3) the 7.43 (DD, J= 7,6, 1.7 Hz, 1H), 7,27-7,13 (m, 4H), 7,16-of 6.96 (m, 3H), 6,95-for 6.81 (m, 3H), of 6.73 (DD, J=8,4, 1.3 Hz, 1H), 5,28 (d, J=17, Calculated for C29H31ClN2O5: 66,60, H 5,97, N ARE 5.36. Found: 66,59, H By 5.87, N 5,30. Connection 12 2-[2-[3-(Aminomethyl) phenoxy] ethyl]-4-(2-Chlorobenzyl) -3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained by the method For using the compound (11). Solution in a mixture of HCl/isopropanol evaporated in vacuum after 24 h and the product was isolated by crystallization from CH2Cl2with the release of 50% in the form of a white powder, so pl. 191-193oC; MS (CI) 423 (MN+); IR (KBR) 3419, 2889, 2624, 1683, 1605, 1505, 1466, 1443, 1403, 1324, 1279, 1181, 1110, 1086, 1038, 951, 930, 893, 791, 749, 695, 627, 567, 452 cm-1; 1H NMR (DMSO-d6) 8,35 (Shir.s, 3H), 7,53 (DD, J=7,7, 1.2 Hz, 1H), 7,32 (m, 3H), 7,17 (s, 1H), 7,13-to 6.95 (m, 6N), 6,85 (DD, J=7,7, 1.2 Hz, 1H), 5,22 (d, J=17.3 Hz, 1H), 5,13 (d, J=17.3 Hz, 1H), 5,04 (DD, J=8,8, 4,2 Hz, 1H), 4,25 (m, 2H), 4,0 (s, 2H), 2,44 (m, 1H), 2,30 (m, 1H). Analysis: Calculated for C24H23lN2O3HCl 0.5 N2ABOUT: WITH 61,54, H 5,38, N 5,98. Found: 61,35, H 5,08, N By 5.87. Connection 13 2-[2-[4-(tert - Butoxycarbonylamino)phenoxy] ethyl]-4-(2-Chlorobenzyl)-3,4-dihydro-3-oxo-2H - 1,4-benzoxazin < / BR> Obtained by method J using intermediate product 9086-189-1 (reference example 42), with a yield of 50% in the form of a white solid product, so pl. 121-123oC; IR (KBR) 3345, 2979, 2925, 1683, 1611, 1503, 1466, 1401, 1248, 1171, 749 cm-1;1H NMR (CDCl 2-[2-[4-(Aminomethyl) phenoxy] ethyl] -4-(2 - Chlorobenzyl)-3,4-dihydro-3 - oxo-2H-1,4-benzoxazin < / BR> The obtained method from the connection 13. The isopropanol was removed under vacuum and the product was isolated by crystallization from a mixture of Cl3/ethyl acetate with a yield of 69% in the form of a white solid substance; so pl. 200-205oC; MS (CI) 423 (MN+); IR (KBR) 3430, 2960, 2890, 2600, 1690, 1611, 1517, 1501, 1468, 1401, 1279, 1250, 1183, 1050, 749, 407 cm-1; 1H NMR (DMSO-d6) by 8.22 (Shir. s, 3H), 7,53 (DD, J=7,6, 1.3 Hz, 1H), 7,40 (d, J=8.7 Hz, 2H), 7,37-of 7.23 (m, 3H), 7,12-to 6.95 (m, 4H), 7,02 (d, J=8.7 Hz, 2H), 6,83 (DD, J=7,9, and 1.6 Hz, 1H), and 5.2 (d, J=and 17.2 Hz, 1H), 5,13 (d, J=and 17.2 Hz, 1H), 5,04 (DD, of 8.4 and 4.2 Hz, 1H), 4,25 (m, 2H), 3,95 (s, 2H), 2,42 (m, 1H), 2,39 (m, 1H). 2-[2-[3-(2-(tert - Butoxycarbonylamino)ethyl) phenoxy]ethyl]-4- (2-Chlorobenzyl)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained by method J using intermediate product 9086-189-1 (reference example 42) with the release of 48% in the form of a white powder, 51 cm-1;1H NMR (DCl3) 7,42 (DD, J=7,6, 1.2 Hz, 1H), 7,35-7,13 (m, 3H), 7,08-6,87 (m, 4H), 6,85 of 6.68 (m, 4H), 5,28 (d, J=17, 6 Hz, 1H), total of 5.21 (d, J=1H), equal to 4.97 (DD, J=9,2, a 4.1 Hz, 1H), 4,54 (Shir.s, 1H), 4,25 (m, 2H), 3,37 (m, 2H), 2,66 (m, 2H), 2,59 (m, 1H), of 2.38 (m, 1H), 1,44 (s, N). 2-[2-[3-(2-Aminoethyl) phenoxy] ethyl]-4-(2 - Chlorobenzyl)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained by the method For using the connection 15. The isopropanol was removed under vacuum after 3 h and the product was isolated by crystallization from a mixture of CHCl3/ethyl acetate with a yield of 91% in the form of a white solid substance, so pl. 173-175oC; MS (CI) 437 (MN+); IR (KBR) 3420, 2932, 1687, 1603, 1501, 1466, 1445, 1401, 1326, 1252, 1160, 1050, 748, 695 cm-1;1H NMR (DMSO-d6) 7,94 (Shir.s, 3H), 7,53 (d, J=7.9 Hz, 1H), 7,37-of 7.23 (m, 3H), 7,15-to 6.95 (m, 5H), 6,86 (m, 3H), 5,22 (d, J=17.5 Hz, 1H), 5,13 (d, J=17.5 Hz, 1H), 5,04 (DD, J=9,2, 2.2 Hz, 1H), 4,23 (and 2H), 3.04 from (m, 2H), 2,35 (m, 2H), 2,4 (m, 1H), to 2.29 (m, 1H). 2-[2-[4-(2-(tert - Butoxycarbonylamino)ethyl) phenoxy]ethyl]-4- (2-Chlorobenzyl)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained by method J with SUP>o 2-[2-[4-(2-Aminoethyl)phenoxy] ethyl] -4-(2-Chlorobenzyl)- 3,4-dihydro-3-oxo - 2H-1,4-benzoxazin < / BR> Obtained by the method For using the connection 18. The isopropanol was removed in vacuo after 1 h and the product was isolated by rubbing with diethyl ether to yield 49% in the form of not quite white powder; so pl. 143-148oC; MS (CI) 437 (MH+-H2O); IR (KBr) 3365, 2930, 1686, 1609, 1515, 1503, 1468, 1445, 1401, 1252, 1111, 1050, 826, 747 cm-1;1H NMR (DMSO-d6) 7,97 (Shir.s, 3H), 7,54 (DD, J= 7,7, and 1.4 Hz, 1H), 7,37-7,22 (m, 2H), 7,19 (d, J=8.6 Hz, 2H), 7,12-to 6.95 (m, 4H), 6,94 (d, J=8.6 Hz, 2H), 6,83 (DD, J=7,6, 1.5 Hz, 1H), 5,20 (d, J=17.3 Hz, 1H), 5,13 (d, J=17.3 Hz, 1H), 5,04 (DD, J=9, 1, 4.0 Hz, 1H), 4,21 (m, 2H), 2,99 (m, 2H), 2,82 (m, 2H), 2.40 a (m, 1H), and 2.27 (m, 1H). Analysis: Calculated for C25H25ClN2O3HCl 0.5 N2O: 62,24, H 5,64, N 5,81. Found: 62,17, H 5,31, N 6,13. Soedinenie by method L using intermediate product 9086-189-1 (reference example 42) and N, N'-di-tert-butoxycarbonyl-(4-hydroxyphenyl)methylguanine and the way To with the following modifications. Bis-BOC-protected product combinations Mitsunobu were isolated by dissolving the residue, representing the crude product, in aqueous methanol and processing added dropwise 2 N. NaOH to achieve the basicity of the solution. The product was separated from the solution in the form of an oil layer. After removal of the solvent by decantation received a viscous oil, which was dried in vacuum and used without further purification. After the stage of removal of the protective group received the product, which was led in CH2Cl2getting a white powder with a total yield of 71%, so pl. 180-182oC; MS (CI) 465 (MN+); IR (KBR) 3320, 3162, 1685, 1665, 1611, 1515, 1503, 1468, 1447, 1401, 1333, 1302, 1281, 1243, 1181, 1113, 1048, 824, 749, 687, 565, 428, 401 cm-1;1H NMR (DMSO-d6) 8,07 (Shir.t, J=5,9 Hz, 1H), 7,53 (DD, J= 8.0 Hz, 1H), 7,8-6,7 (PTS.Shir.s, 4H), 7,35-to 7.15 (m, 3H), 7,26 (d, J= 9.0 Hz, 2H), 7,1-6,93 (m, 3H), of 6.99 (d, J=9.0 Hz, 2H), 5,22 (d, J=and 17.9 Hz, 1H), 5,11 (d, J=and 17.9 Hz, 1H), 5,04 (DD, J=8,8, 4,2 Hz, 1H), 4,3 (apparent d, J=6 Hz, 2H), to 4.23 (m, 2H), 2,41 (m, 1H), 2,28 (m, 1H). Analysis: Calculated for C25H25ClN4O3HCl: 59,89, H 5,23, N 11,17. Found: 59,57, H 5,13, N 10,99. The connection 20 4-(2-Chlorobenzyl)-2-[2-[4- (2-guanidinate)phenoxy] ethyl]-3,4-dihydro-3-ox is example 42) and N, N'-di-tert-butoxy-carbonyl-2-(4-hydroxyphenyl)ethylguanidine and the way To with the following modifications. Bis-BOC-protected product combinations Mitsunobu was isolated after flash chromatography and crystallization to yield 36%. The product with the remote protective group was allocated in the form of a carbonate salt (reddish-brown solid) with a yield of 88%; so pl. 90oWith (Razlog.); MS (CI) 479 (MN+); IR (KBR) 3600, 3350, 2939, 1688, 1515, 1501, 1401, 1243, 1111, 1050, 834, 749, 522 cm-1;1H NMR (DMSO-d6) 7,53 (DD, J= 7,8, and 1.6 Hz, 1H), 7,33 (DD, J=7,8, and 1.6 Hz, 1H), 7,29 (m, 1H), 7,25 (DD, 7,4, and 1.6 Hz, 1H), 7,18 (d, J=8,2 Hz, 2H), 7,12-6,93 (m, 4H), 6,9 (d, J= 8,2 Hz, 2H), PC 6.82 (DD, J=7,4, and 1.6 Hz, 1H), total of 5.21 (d, J=and 17.2 Hz, 1H), 5,11 (d, J= and 17.2 Hz, 1H) 5,2 (DD, J=8,5, a 4.1 Hz, 1H), 4,2 (m, 2H), 3,7-2,8 (Shir.s, 5H), 2,69 (m, 2H), 2,4 (m, 1H, in), 2.25 (m, 1H). Analysis: Calculated for C26H27N4O3Cl H2CO30,3 H2About: 59,35, H 5,46, N Of 10.25, Cl Of 6.49. Found: 59,37, H Of 5.29, N Of 10.25, Cl 6,86. Connection 21 4-(4-Chlorobenzyl)-2-[2- [4-(guanidinate)phenoxy] ethyl]-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained by method L using intermediate product 10353-28-1 (reference example 41) and N, N'-di-tert-butoxycarbonyl -(4-hydroxyphenyl)methylguanine and how To with the following modifications. Bis-BOC-protected product combinations Mitsunobu allocated R the pits 2 N. NaOH to achieve the basicity of the solution. The product was precipitated from solution, was collected by filtration. The resulting white solid product was air-dried and used without further purification. The product after removal of the protective group was allocated in the form of a carbonate salt (reddish-brown solid) with a total yield of 24%, so pl. 90oWith (Razlog.); MS (CI) 465 (MN+); IR (KBR) 3330, 2940, 1685, 1708, 1650, 1600, 1513, 1501, 1466, 1399, 1302, 1279, 1245, 1177, 1094, 1052, 799, 751 cm-1;1H NMR (DMSO-d6a ) 7.5 to 3.0 (PTS. Shir. s, 5H), 7,40 (d, J=8,4 Hz, 2H), 7,30 (d, J=8,4 Hz, 2H), 7,12 (d, J=8,8 Hz, 2H), 7,1-to 6.95 (m, 4H), 6,91 (d, J=8,8 Hz, 2H), total of 5.21 (d, J=17,4 Hz, 1H), 5,13 (d, J= 17,4 Hz, 1H), equal to 4.97 (DD, J=9,0, 4,2 Hz, 1H), to 4.28 (m, 2H), is 2.37 (m, 1H), 2,23 (m, 1H). Analysis: Calculated for C25H25ClN4O3CH2O30,3 H2O: 58,66, H 5,23, N 10,52. Found: 58,38, H A 4.86, N 10,61. Reference example 89 The intermediate product 10353-76 4-(2-Chlorobenzyl) -3,4-dihydro-2-(2 - hydroxyethyl)-2H-1,4-benzoxazin Method M: Intermediate product 9086-189-1 (1 g, 1 EQ, reference example 42) was dissolved in THF (5 ml) and treated with 1 m solution of borane/THF (6.3 ml, 3 EQ) and heated to boiling under reflux. After 3 h the reaction mixture was concentrated in vacuo and the residue was distributed between diethyl ether and 1 is SUB> and concentrated in vacuum. The product was isolated as a colourless oil flash chromatography, elwira a mixture of ethyl acetate/hexane, yield 96%. Reference example 90 The intermediate product 10353-82 4-(3-Chlorobenzyl)-3,4 - dihydro-2-(2-hydroxyethyl)-2H-1,4-benzoxazin Obtained by the method M of the intermediate product 10488-22 (reference example 66) and allocated with a yield of 99%. Reference example 91 The intermediate product 10353-83 4-(4-Chlorbenzyl)-3,4 - dihydro-2-(2-hydroxyethyl) -2H-1,4-benzoxazin Obtained by the method M of the intermediate product 10353-28-1 (reference example 41) and allocated with a quantitative yield as a colourless oil. Reference example 92 The intermediate product 10840-45 3,4-Dihydro-2-(2 - hydroxyethyl)-4-(4 - methylbenzyl)-2H - 1,4-benzoxazin Obtained by the method M of the intermediate product 10840-33 (reference example 46) with yields of 80% and isolated in the form of a green oil, IR (net) 3371, 2921, 1607, 1500, 1247, 1221, 1052, 743 cm-1;1H NMR (CDCl3) 1,77 is 2.00 (m, 3H), of 2.33 (s, 3H), 3,19 (DD, J=11.8 in, and 7.7 Hz, 1H), 3.27 to (DD, J=11,7, 2.6 Hz, 1H), 3,86-of 3.94 (m, 2H), 4,33-and 4.40 (m, 1H), and 4.40 (s, 2H), 6,60-of 6.71 (m, 2H), 6,76-6,84 (m, 2H), 7,15 (Shir.kV, JAB=8,2 Hz, 4H). Analysis: Calculated for C18H21NO20.6 N2ABOUT: WITH 73,49, H TO 7.61, N 4,76. On the oxyethyl)-4-(3 - methoxybenzyl)-2H-1,4-benzoxazin Obtained by the method M of the intermediate product 10508-22-A (reference example 76) with a quantitative yield and isolated in the form of a green oil, IR 3350, 2948, 1605, 1505, 1283, 1262, 1050, 743 cm-1;1H NMR (DCl3) 1,50-2,10 (PTS.Shir.s, 1H), 1,78 is 2.01 (m, 2H), 3,20 (DD, J=11,7, and 7.8 Hz, 1H), or 3.28 (DD, J=11,7, 2.6 Hz, 1H), of 3.78 (s, 3H), 3,88 (t, J=5.6 Hz, 2H), 4,34-4,43(m, 1H), and 4.40 (s, 2H), 6,62-6,79 (m, 2H), 6,76-6,89 (m, 5H), 7,24 (t, J=7.7 Hz, 1H); MN+at m/z=300. Analysis: Calculated for C18H21NO30,2 H2O: 71,36, H 7,12, N 4,62. Found: 71,25, H 7,00, N 4,62. Reference example 94 The intermediate product 10840-8 4-(2,4-Dichlorobenzyl) -3,4-dihydro-2-(2-hydroxyethyl) -2H-1,4-benzoxazin Obtained by the method M of the intermediate product 10005-181-1 (reference example 48) with the release of 87% and isolated in the form of a colorless oil. IR (net) 3348, 1607, 1501, 1247, 1221, 1046, 743 cm-1;1H NMR (DCl3) 1,80-2,03 (m, 3H), 3.27 to 3,37 (m, 2H), 3,85-3,98 (m, 2H), of 4.38 is 4.45 (m, 1H), of 4.45 (s, 2H), 6,44 (DD, J=8.0 a, and 1.4 Hz, 1H), 6,65 (TD, J=7,6, 1.5 Hz, 1H), 6,77 (TD, J=7,8, and 1.6 Hz, 1H), 6,83 (DD, J=7,8, and 1.6 Hz, 1H), 7,15-7,25 (m, 2H), 7,42 (d, J=1.8 Hz); MN+at m/z=338. Analysis: Calculated for C17H17Cl2NO2: 60,37, H 5,07, N 4,14. Found: 60,04, H To 4.98, N Of 4.05. The connection 22 4-(4-Chlorobenzyl)-2-[2- [4-(2-guanidinate)phenoxy] ethyl]-3,4-dihydro - 2H-1,4-benzoxazin < / BR>carbonyl-2-(4-hydroxyphenyl)ethylguanidine and the way To with the following modifications. Bis-BOC-protected product combinations Mitsunobu allocated with satisfactory purity flash chromatography (elution with a mixture of ethyl acetate/hexane) to yield 58%. The product with the remote protective group was identified as the carbonate salt with a yield of 50% in the form of a reddish-brown solid, which gave a single homogenous peak with HPLC (PDA detection) on a C18-column, 15 cm elution with a mixture of N2ABOUT (5% NH4OH, 5% HOAc)/CH3CN, 55/45; MS (CI) 466 (MH+); IR (KBr) 3475, 3321, 3064, 2931, 2875, 1698, 1638, 1608, 1581, 1513, 1502, 1467, 1696, 1358, 1303, 1288, 1244, 1178, 1116, 1047, 1013, 833, 743 cm-1;1H NMR (DMSO-d6) 8,30-7,50 (Shir.s, 2H), 7,40 (d, J=8,2 Hz, 2H), 7,35 (d, J=8,2 Hz, 2H), 7,19 (d, J=8,2 Hz, 2H), make 6.90 (d, J=8,2 Hz, 2H), 6,77-6,60 (m, 3H), 6,55 (m, 1H), 4,53 (d, J=16,8 Hz, 1H), 4,45 (d, J=16,8 Hz, 1H), 4,35 (m, 1H), 4,12 (Shir.d, J=11,4 Hz, 2H), 3,60-3,10 (Shir.s, 5H), 3,49 (m, 2H), by 2.73 (m, 2H), 2.05 is (m, 2H). The connection 23 4-(3-Chlorobenzyl)-2-[2-[4- (2-guanidinate)phenoxy] ethyl]-3,4-dihydro - 2H-1,4-benzoxazin < / BR> Obtained by method L using intermediate product 10353-82 (reference example 90) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine and the way To with the following modifications. Bis-BOC-protected product combinations Mitsunobu was isolated by flash chromatography (elution with a mixture of ethyl acetate/hexane) to yield 94%. P is ejogo substances, which gave a single homogenous peak with HPLC (PDA detection) on a C18-column, 15 cm elution with a mixture of N2O (5% NH4OH, 5% SPLA)/CH3JV, 55/45; MS (CI) 466 (MH+); IR (KBr) 3473, 3316, 3064, 2931, 2876, 1698, 1638, 1608, 1580, 1512, 1503, 1468, 1431, 1393, 1359, 1303, 1243, 1221, 1178, 833, 742 cm-1; 1H NMR (DMSO-d6) 8,50-7,60 (Shir.s, 2H), 7,42-7,20 (m, 4H), 7,19 (d, J=7.7 Hz, 2H), make 6.90 (d, J=7.7 Hz, 2H), 6,78-6,70 (m, 3H), return of 6.58 (m, 1H), 4,55 (d, J=17.3 Hz, 1H), 4,48 (d, J=17.3 Hz, 1H), 4,15 (m, 2H), 3,80-3,10 (Shir.s, 4H), 3,52 (Shir.d, J=11.8 Hz, 2H), 3,25 (m, 2H), by 2.73 (m, 2H), 2,08 (m, 2H). Connection 24 4-(3-Chlorobenzyl)-3,4-dihydro-2-[2-[4-(2-guanidinate) -phenoxy]ethyl] -6-methyl-3-oxo-2H-1,4-benzoxazin < / BR> Obtained by method L using intermediate product 12168-10-1 (reference example 39) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine and how To with the following modifications. Bis-BOC-protected product combinations Mitsunobu was isolated by flash chromatography (elution with a mixture of ethyl acetate/hexane) to yield about 70%. The product with the remote protective group triturated in diethyl ether, dissolved in CH2Cl2, and the solvent was removed in vacuum, obtaining a product with a yield of 92% as a pale-yellow solid; MS (CI) 493 (MN+); IR (KBR) 3148, 1666, 1610, 1511, 1433, 1384, 1302, 1244, 1178, 1112, 1052, 817, 772, 680, 527 cm-1, J=17.3 Hz, 1H), 5,12 (d, J= 17.3 Hz, 1H), 4,94 (DD, J=9,1, a 4.3 Hz, 1H), 4,18 (m, 2H), and 3.31 (m, 2H), rating of 2.72 (apparent t, J=7,3 Hz, 2H), is 2.37 (m, 1H), 2,30 and 2.13 (m, 1H), 2,19 (s, 3H). Analysis: Calculated for C27H29lN4ABOUT3HCl and 1.0 H2O: 59,23, H OF 5.89, N 10,23. Found: 59,47, H Ceiling Of 5.60, N 10,11. The connection 25 4-(3-Chlorobenzyl)-3,4-dihydro-2-[2-[4-(2-guanidinate)-phenoxy] ethyl] -3-oxo-2H-pyrido [3,2-b] 1,4-oxazin < / BR> Obtained by method L using intermediate product 10353-191-1 (reference example 40) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine and the way To with the following modifications. Bis-BOC-zawiszy product combinations Mitsunobu was isolated by flash chromatography (elution with a mixture of ethyl acetate/hexane) to yield 77%. The product with the remote protective group was provided with access to 50% after trituration with diethyl ether, T. pl. 47-54oWith (softened), 54-56oC; MS (CI) 480 (MN+); IR (KBR) 3326, 3150, 1666, 1599, 1513, 1459, 1398, 1331, 1278, 1229 cm-1;1H NMR (DMSO-d6) 8,0 (DD, J= 4,9, and 1.4 Hz, 1H), 7,53 (Shir.t, J=7,3 Hz, 1H), 7,47 (DD, J=7,9, 1.2 Hz, 1H), 7,37 (s, 1H), 7,35-7,22 (m, 2H), 7,17 (d, J=8.6 Hz, 2H), to 7.09 (DD, J= 7,9, and 4.8 Hz, 1H), 6.87 in (d, J=8.6 Hz, 2H), 5,24 (d, J=16,3, Hz, 1H), 5,23 (d, J= 16,3 Hz, 1H), 5,12 (DD, J=8,2, 4,2 Hz, 1H), 4,15 (m, 2H), 6,32 (m, 2H), 2,71 (m, 2H), 2,39 (m, 1H), to 2.29 (m, 1H). Analysis: Calculated for C25H26ClN5O < / BR> Obtained by method L using intermediate product 10353-191-1 (reference example 40) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine and the way To with the following modifications. Bis-BOC-protected product combinations Mitsunobu was isolated by dissolving the residue, representing the crude product, in aqueous methanol and processing added dropwise 2 N. NaOH to achieve the basicity of the solution. The residue was collected by filtration. The obtained product was dissolved in ether, washed sequentially 1 N. HCl, a saturated solution of NaHCO3and brine, dried over Na2SO4and concentrated in vacuo and used without further purification. The product with the remote protective group was identified as the carbonate salt with a yield of 22% in the form of a reddish-brown substance, which gave a single homogenous peak with HPLC (PDA detection) on a C18-column, 15 cm elution with a mixture of N2O (5% NH4OH, 5% SPLA)/CH3JV, 55/45; MS (CI) 451 (MH+); IR (KBr) 3314, 3036, 2923, 1682, 1608, 1581, 1511, 1468, 1443, 1392, 1352, 1302, 1244, 1223, 1175, 1046, 742 cm-1. The connection 26 4-(4-Chlorbenzyl)-3,4 - dihydro-2-[2-[4-(2- guanidinate)-phenoxy]ethyl]-3-oxo-2H-1,4-benzoxazin < / BR> Obtained by method L using premiato obom To with the following modifications. Bis-BOC-protected product combinations Mitsunobu was isolated by dissolving the residue, representing the crude product, in aqueous methanol and processing 2 N. NaOH to achieve the basicity of the solution. The product was precipitated from solution in the form of a resinous semi-solid substances. The solvent was removed by decantation, the product was air-dried and used without further purification. The product with the remote protective group was identified as the carbonate salt (reddish-brown solid) with a yield of 60%, which gave a single homogenous peak with HPLC (PDA detection) on a C18-column, 15 cm elution with a mixture of H2O (5% NH4OH, 5% SPLA)/CH3JV, 55/45; MS (CI) 479 (MN+); IR (KBR) 3337, 3050, 2930, 2875, 1683, 1609, 1512, 1500, 1466, 1439, 1397, 1327, 1301, 1278, 1242, 1177, 1093, 750 cm-1. Connection 27 4-Benzyl-2-{ 2-[4-[2-(N, N-bis-tert-butoxycarbonylamino-ethyl]phenoxy]ethyl}-3,4-dihydro-3-oxo-2H - 1,4-benzoxazin < / BR> Obtained by method L using intermediate product 10508-23-A (reference example 74) and allocated in the form of a white powder with a yield of 28% after column chromatography (10% ether in hexane); IR (KBR) 3334, 2978, 1638, 1616, 1330, 1132, 750 cm-1;1H NMR (CDCl3) to 1.48 (s, N) and 1.51 (s, N), 2,25-2,39 (m, 1H), 2,50 2.63 in (m, 1H), 2,81 (t, J=7.2 Hz, 2H), 3,63 (kV, J= 7.9 Hz, 2H), 4,18-4,2="ptx2"> Analysis: Calculated for C36H44N4O7: 67,06, H 6,88, N 8,69. Found: 66,80, H 6,90, N 8,63. The connection 280,7-Hydrate of the hydrochloride of 4-benzyl-3,4-dihydro- 2-{2-[4-[2-guanidinate] phenoxy] ethyl}-3-oxo-2H-1,4-benzoxazine < / BR> Obtained by the method For using the compounds 27 and allocated in the form of a white powder with a yield of 9.1%; IR (KBR) 3326, 3146, 1664, 1500, 1401, 1243, 827, 751 cm-1. Analysis: Calculated for C26H28N4O3HCl 0,7 N2O: 63,27, H 6,21, N 11,35. Found: 63,37, H 5,98, N 11,06. The connection 29 3,4-Dihydro-2-{ 2-[4-[2- guanidinate] phenoxy]ethyl} -4-(2-methoxybenzyl)-3 - oxo-2H-1,4-benzoxazin < / BR> Obtained from 2-{ 2-[4-[2-(N, N-bis - tert-butoxycarbonyl-guanidino)ethyl] phenoxy] ethyl}-3,4-dihydro-4-(2 - methoxybenzyl)-3-oxo-2H-1,4-benzoxazine ways L and K in the form of not-quite-white powder with a yield of 25%; IR (KBR) 3164, 1663, 1501, 1405, 1245, 751 cm-1;1H NMR (CDCl3) 2,20 is 2.33 (m, 1H), 2,37-2,52 (m, 1H), was 2.76 (Shir.s, 2H), 3.33 and (Shir.s, 2H), a 3.87 (s, 3H), 4,08-is 4.21 (m, 2H), 4,87 (DD, J=8,6, a 4.3 Hz, 1H), 5,09 (ABq, JAB=18,0 Hz, 2H), 6.73 x-7,25 (PTS. Shir. s, 4H), 6.73 x-6,99 (m, N), 7,11 (d, J=7.7 Hz, 2H), 7,21 (t, J=7.2 Hz, 1H), to 7.67 (Shir.with. 1H); MH+at m/z=475. Analysis: Calculated for C27H30N4O4HCl 0.75 H2O: 61,83, H 6,25, N IS 10.68. Found: 61,82, is ihydro-4-(3-terbisil)-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from 10508-24-A (reference example 45) by method L and isolated in the form of a white foam with a yield of 17% after chromatography using 20% ethyl acetate in hexane; IR (KBR) 3330, 2979, 1723, 1688, 1638, 1132, 1059, 751 cm-1;1H NMR (CDCl3) to 1.48 (s, N), 1,50 (s, N), 2,27-of 2.38 (m, 1H), 2,53-of 2.64 (m, 1H), 2,81 (t, J=7.2 Hz, 2H), 3,64 (kV, J=6,8 Hz, 2H), 4,15-the 4.29 (m, 2H), 4,94 (DD, J= 9,0, 4.0 Hz, 1H), further 5.15 (ABq, JAB=15.2 Hz, 2H), for 6.81? 7.04 baby mortality (m, 8H), 7,13 (d, J= 8.6 Hz, 2H), 7,28-a 7.92 (m, 2H), at 8.36 (t, J=4,8 Hz, 1H), 11,47 (s, 1H). Analysis: Calculated for C36H43FN4O7: 65,24, H IS 6.54, N 8,45. Found: 65,03, H To 6.43, N 8,31. The connection 31 3,4-Dihydro-4-(3 - terbisil)-2-{ 2-[4-(2- guanidinate)-phenoxy]ethyl} -3-oxo-2H-1,4-benzoxazin < / BR> Obtained from compound 30 by method K and isolated in the form of a white foam with a yield of 97%; IR (KBR) 3153, 1654, 1501, 753 cm-1;1H NMR (DCl3) 2,18 is 2.33 (m, 1H), 2,37-2,52 (m, 1H), 2,78 (Shir.s, 2H), 3,34 (PTS.Shir.s, 2H), 4,05-4,22 (m, 2H), a 4.86 (DD, J=8,7, 4,2 Hz, 1H), 5,07 (s, 2H), 's 6.75 to 7.25 (Shir.s, 4H), to 6.80 (d, J=7,6 Hz, 2H), 6,84-7,00 (m, 6N), 7,12 (d, J=7.7 Hz, 2H), 7,22-7,30 (m, 2H), 7,71 (Shir.s, 1H). Analysis: Calculated for C26H27FN4O3HCl H2O 0.1 C3H8O: 60,40, H 5,94, N 10,71. Found: 60,11, H 5,86, N 10,42. The connection 32 2-{2-[4-[2-(N,N-Bis-tert - butoxycarbonylamino) ethyl] -phenoxy]ethyl} -3,4-Digi the second example 76) by method L and isolated in the form of a white foam with 30% yield; IR (KBR) 3334, 2979, 1723, 1686, 1645, 1615, 1329, 1246, 1156, 1132, 1059, 751 cm-1;1H NMR (CDCl3) to 1.48 (s, N) and 1.51 (s, N), and 2.26-of 2.38 (m, 1H), of 2.51 2.63 in (m, 1H), 2,81 (t, J= 7.2 Hz, 2H), 3,64 (kV, J=6,79 Hz, 2H), of 3.77 (s, 3H), 4,15-the 4.29 (m, 2H), 4,94 (DD, J=9,2, 4.0 Hz, 1H), 5,13 (s, 2H), 6,76-7,02 (m, 8H), 7,12 (d, J=8.6 Hz, 2H), 7,21-7,26 (m, 2H), of 8.37 (t, J=4,8 Hz, 1H), 11,47 (s, 1H). Analysis: Calculated for C37H46N4O80.1 G2O: 65,68, H 6,88, N 8,28. Found: 65,40, H 6,83, N 8,10. The connection 33 3,4-Dihydro-2-{ 2-[4-(2-guanidinate)phenoxy] ethyl} -4-(3-methoxybenzyl)-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from compound 32 by method K and isolated in the form of soluble Cl3white foam with a yield of 21%; IR (net) 3020, 1671, 1513, 1501, 1407, 1217, 758 cm-1;1H NMR (DCl3) 2,15-of 2.28 (m, 1H), 2,35-2,48 (m, 1H), 2,70-2,87 (m, 3H), 3,34 (Shir.s, 2H), 3,71 (s, 3H), was 4.02-4,17 (m, 2H), around 4.85 (DD, J=8,8, 4.0 Hz, 1H), 5,03 (ABq, JAB=16,8 Hz, 2H), 6,72-of 7.23 (m, N), to 7.64 (Shir.s, 1H). Analysis: Calculated for C27H30N4O4HCl H2O: 61,30, H 6,29, N 10,59. Found: 61,20, H 6,04, N 10,45. The connection 34 4-(3-Benzyloxybenzyl) -2{ 2-[4-[2-(N,N-bis-tert-butoxycarbonylamino) ethyl]phenoxy]ethyl}-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from 10508-82-A (reference example 77) by method L and isolated in the form of a white foam with a yield of 35% after chromatography is R (CDCl3) to 1.48 (s, N) and 1.51 (s, N), 2,24-is 2.37 (m, 1H), 2,50 2.63 in (m, 1H), 2,81 (t, J=7.2 Hz, 2H), 3,63 (kV, J=7,1 Hz, 2H), 4,15-4,30 (m, 2H), 4.92 in (DD, J=9,4, 3,9 Hz, 1H), 5,02 (s, 2H), 5,12 (ABq, JAB= to 15.4 Hz, 2H), 6,84-7,00 (m, N), 7,12 (d, J=8.6 Hz, 2H), 7.23 percent-7,27 (m, 1H), 7,32-7,42 (m, 5H), of 8.37 (Shir.t, J=4.3 Hz, 1H), and 11.5 (s, 1H). Analysis: Calculated for C43H50N4ABOUT8: 68,78, H OF 6.71, N 7,46. Found: 68,50, H Is 6.78, N 7,41. The connection 35 4-(3-Benzyloxybenzyl) -3,4-dihydro-2-(2-[4-(2- guanidino-ethyl)phenoxy] ethyl}-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from compound 34 by method K and isolated in the form of a white foam with a yield of 53% after repeated rubbing with ether, so PL 100-105oC. IR (KBR) 3338, 3155, 1676, 1610, 1513, 1500, 1400, 1243, 751 cm-1;1H NMR (CDCl3) 2,10-of 2.23 (m, 1H), 2,30 is 2.44 (m, 1H), 2,74 (Shir.s, 2H), 3,32 (Shir.s, 2H), 3,97-to 4.15 (m, 2H), to 4.81 (DD, J=8,7, 4,1 Hz, 1H), 4,96 (s, 2H), free 5.01 (s, 2H), 6.75 in-7,33 (m, N), 7,63 (Shir.s, 1H). Analysis: Calculated for C33H34O4HCl H2ABOUT: 65,50, H 6,16, N 9,26. Found: 65,77, H 5,98, N 9,06. The connection 36 3,4-Dihydro-2-{ 2-[4-(2- guanidinate)phenoxy] ethyl}-4-(3-hydroxybenzyl) -3-oxo-2H-1,4-benzoxazin < / BR> Compound 35 (0.5 g, 0.83 mmol) was subjected to reaction with H2when 3,515 ATM in the vibrator Parra, containing 10% Pd/C (200 mg) in the Meon. After 2 h, the catalyst was removed and the filtrate koncentrirane is 2, 1500, 1242, 752 cm-1; 1H NMR (DMSO-d6plus DCl3) 2,28-of 2.38 (m, 1 H), 2,45-of 2.58 (m, 1H), 2,82 (t, J=7.4 Hz, 2H), 3,01 (s, HDO), 3,40 (kV, J= 6,8 Hz, 2H), 4,15-4,30 (m, 2H), 4,91 (DD, J=9,1, a 4.3 Hz, 1H), to 5.08 (s, 2H), 6,69 to 6.75 (m, 3H), 6.87 in-7,02 (m, 8H), 7,11-7,30 (m, 5H), 7,54 (Shir. t, J=5,1 Hz, 1H), 9,05 (s, 1H); MN+at m/z=461. Analysis: Calculated for C26H28N4O42HCl H2O: 56,63, H 5,85, N 10,16. Found: 56,46, H 5,61, N 9,85. The connection 37 3,4-Dihydro-2-{ 2-[4-(2- guanidinate)phenoxy] ethyl}-4- (4-methoxybenzyl)-3-oxo-2H-1,4-benzoxazin < / BR> Obtained as a white foam with a yield of 53% by method L using intermediate product 10508-19 (reference example 47) and N,N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)-ethylguanidine and how To: IR (KBR) 3411, 1654, 1617, 1515, 1501, 1248, 750 cm-1;1H NMR (CDCl3) of 2.20 (m, 1H), 2,31 is 2.44 (m, 1H), 2,72 (Shir.t, J=6.4 Hz, 2H), 3,29 (Shir.t, J=6.4 Hz, 2H), 3,68 (s, 3H), 3.96 points-of 4.12 (m, 2H), 4,79 (DD, J=8,8, 4.0 Hz, 1H), equal to 4.97 (s, 2H), 6,70-7,30 (PTS.Shir.s, 4H), of 6.71-6,93 (m, 8H), 7,05-7,13 (m, 4H), 7,70 (Shir.s, 1H); MH+at m/z=475. Analysis: Calculated for C27H30N4O4HCl H2O: 61,30, H 6,29, N 10,59. Found: 61,17, H 6,10, N Of 10.25. Compound 38 3,4-Dihydro-2-{ 2-[4-(2- guanidinate)phenoxy] ethyl} -3-oxo-4-(4-phenylbenzyl) -2H-1,4-benzoxazin < / BR> Obtained as a white PE-butoxycarbonyl-2-(4-hydroxyphenyl)-ethylguanidine and how To; IR (KBR) 3157, 1681, 1500, 1398, 1243, 759 cm-1;1H NMR (CDCl3) 2,20 is 2.33 (m, 1H), 2,38-of 2.54 (m, 1H), 2,73-2,82 (m, 2H), 3.27 to 3,39 (m, 2H), 4,05-4,22 (m, 2H), 4,88 (DD, J=8,9, and 4.4 Hz, 1H), 5,12 (s, 2H), 6,65-EUR 7.57 (PTS.Shir.s, 4H), to 6.80 (d, J=8,4 Hz, 2H), 6,88-6,97 (m, 3H), 7,11 (d, J=8,3 Hz, 2H), 7,25-to 7.32 (m, 4H), 7,39 (t, J=7,1 Hz, 2H), 7,51 (d, J=8.0 Hz, 4H), 7,71 (Shir.s, 1H); MH+ at m/z=521. Analysis: Calculated for C32H32N4ABOUT3HCl H2O: 66,83, H 6,13, N 9,74. Found: 67,01, H Of 5.99, N At 9.53. Connection 39 2-{ 2-[4-(2-Aminomethyl) phenoxy]ethyl}-4-(3,5 - dichlorobenzyl)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained in the form of a white solid product with a yield of 73% by method L using intermediate product 10005-181-1 (reference example 48) and N-tert-butoxycarbonyl-(4-hydroxyphenyl)benzylamine and how It directly from the reaction mixture; so pl. 228,5-230oC; IR (KBR) 2927, 1680, 1517, 1503, 1402, 1254, 752 cm-1;1H NMR (DMSO-d6) 2,20-2,31 (m, 1H), 2,36-2,48 (m, 1H), 3,94 (s, 2H), 4,20-to 4.28 (m, 2H), of 5.05 (DD, J=8,5, 3.8 Hz, 1H), 5,18 (ABq,AB=16,7 Hz, 2H), of 6.96-7,10 (m, 6N), 7,35 (d, J=1.8 Hz, 2H), 7,43 (d, J=8.6 Hz, 2H), 7,52 (t, J=1.8 Hz, 1H), of 8.37 (Shir.s, 3H). Analysis: Calculated for C24H22CL2N2O3HCl 0.5 N2O: 57,33, H TO 4.81, N 5,57. Found: 57,33, H 4,77, N Lower Than The 5.37. The connection 40 4-(3,5-Dichlorobenzyl)-3,4-dihydro-2-{ 2-[4-(2- goinig what about the product with an overall yield of 48% by method L using intermediate product 10005-181-1 (reference example 48) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine way To, so pl. of 115.5-117oC; IR (KBR) 3328, 1665, 1515, 1501, 1399, 1245, 751 cm-1;1H NMR (DMSO-d6) 2,17-of 2.30 (m, 1H), 2,33-2,47 (m, 1H), 2,72 (t, J= 7.2 Hz, 2H), 3,28-of 3.48 (m, 3H), 4,15, 4,24 (m, 2H), 5,02-of 5.06 (m, 1H), 5,18 (ABq, JAB=16,7 Hz, 2H), 6,8-7,6 (PTS.Shir.s, 4H), 6,91 (d, J=8.5 Hz, 1H), 6,99-7,10 (m, 4H), 7,20 (d, J=8.5 Hz, 2H), 7,35 (s, 2H), 7,52 (s, 1H), 7,66 (t, J=5.5 Hz, 1H). Analysis: Calculated for C26H26CL2N4O3HCl of 0.25 N2O: 56,33, H 5,00, N 10,11. Found: 56,18, H 5,26, N 9,90. The connection 41 2-{ 2-[4-[2-(N,N-Bis-tert - butoxycarbonylamino)ethyl]-phenoxy] ethyl} -3,4-dihydro-4-(3 - methoxybenzyl)-3-oxo-4- (4-picolyl)-2H-1,4-benzoxazin < / BR> Obtained in the form of not-quite-white powder with a yield of 20% by method L using intermediate product 10840-22 (reference example 58) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine; IR (KBR) 2979, 1723, 1690, 1638, 1501, 1416, 1368, 1333, 1246, 1158, 751 cm-1;1H NMR (CDCl3) to 1.48 (s, N), 1,50 (s, N), 2,28-to 2.40 (m, 1H), 2,53-of 2.64 (m, 1H), 2,81 (t, J=7.2 Hz, 2H), 3,63 (Shir.kV, J=7.2 Hz, 2H), 4,16-4,30 (m, 2H), 4,96 (DD, J=9,2, 4.0 Hz, 1H), 5,16 (ABq, JAB=14 Hz, 2H), 6.73 x (DD, J=8,4, 1.5 Hz, 1H), 6,85 (d, J= 8.6 Hz, 2H), 6,93 (TD, J=7,2, 2.0 Hz, 1H), 6,97-7,06 (m, 2H), 7,12-7,17 (m, 4H), at 8.36 (Shir.t, J=4,8 Hz, 1H), 8,56 (DD, J=4,5, and 1.6 Hz, 2H), 11,47 (s, 1H). Analysis: Calculated dlsite-2-{ 2-[4-(2- guanidinate)phenoxy]ethyl} -3-oxo-4-(4-picolyl) -2H-1,4-benzoxazin < / BR> Obtained from compound 41 by method K and isolated in the form of a white solid product with 30% yield after trituration with ether, so pl. 244-248oC; IR (KBR) 3184, 1673, 1640, 1499, 1403, 1248, 760 cm-1;1H NMR (DMSO-d6) of 2.20 to 2.35 (m, 1H), 2,35-2,48 (m, 1H), 2,72 (t, J=7.2 Hz, 2H), 3,32 (kV, J=6,6 Hz, 2H), 3,50-4,50 (PTS. Shir.s, 1H), 4,15-4.26 deaths (m, 2H), 5,07 (DD, J=8,8, 4,1 Hz, 1H), 5.40 to (ABq,AB= to 18.1 Hz, 2H), 6,80-7,55 (PTS.Shir.s, 4H), 6.87 in-7,13 (m, 6N), 7,21 (d, J=8.6 Hz, 2H), 7,66 (t, J=5.6 Hz, 1H), 7,78 (d, J=6.3 Hz, 2H), 8,78 (d, J=6,4 Hz, 2H); MN+at m/z=446. Analysis: Calculated for C25H27N5O32HCl 0.5 H2O: 56,93, H 5,73, N 13,28. Found: 56,87, H Ceiling Of 5.60, N 13,06. The connection 43 3,4-Dihydro-2-{ 2-[4-(2- guanidinate)phenoxy] ethyl} -4-(1-naphthylmethyl)-3-oxo-2H-1,4-benzoxazin < / BR> Obtained by method L using intermediate product 10508-84-A1 (reference example 78) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine and method For using triperoxonane acid present anisole instead of IPA/HC1. The crude product was treated with a mixture of CH2Cl2/ether, getting mentioned in the title compound as a cream solid product with a yield of 72%; so pl. 75-80oC; IR (KBR) 3360, 1671, 1501, 1405, 1204, 1136, 799, 723 cm-1;1H NMR (DMSO-d6) 2,29-is 2.37 (m, 1H), 2,37-of 2.50 (m, 1H), 2,72 (t, J.Shir.with, 4H), 6,86-7,06 (m, 4H), 7,11 (d, J= 8.1 Hz, 2H), 7,20 (d, J=8.6 Hz, 2H), 7,40 (t, J=7.7 Hz, 1H), of 7.48-of 7.55 (m, 1H), 7,58-to 7.68 (m, 2H), a 7.85 (d, J=8,2 Hz, 1H), 8,00 (d, J=9.1 Hz), 8,21 (d, J=8.1 Hz): MH+at m/z=495. Analysis: Calculated for C30H30N4O3C2HF3O2: 62,38, H IS 5.06, N 9,04. Found: 62,38, H Is 5.06, N 9,04. The connection 44 2-{ 2-[4-[2-(N,N-Bis-tert - butoxycarbonylamino)ethyl] -phenoxy]ethyl} -3,4-dihydro-4-(2-naphthylmethyl)-3-oxo-2H-1,4-benzoxazin < / BR> Obtained by method L using intermediate product 10508-80-1 (reference example 79) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine. The crude material was purified flash chromatography with elution with a mixture of ethyl acetate/hexane, receiving the product as a white foam with a yield of 24%; IR (KBR) 3330, 3053, 2977, 2931, 1722, 1638, 1614, 1512, 1501, 1366, 1330, 1244, 1156, 1131, 748 cm-1; 1H NMR (DCl3) to 1.48 (s, N) and 1.51 (s, N), 2,31 is 2.44 (m, 1H), 2,55 of 2.68 (m, 1H), 2,82 (t, J=7,1 Hz, 2H), 3,65 (kV, J= 6 Hz, 2H), 4,20-to 4.33 (m, 2H), 5,00 (DD, J=9,4, 3,4 Hz, 1H), 5,32 (ABq, AB= to 15.4 Hz, 2H), 6,84-of 6.96 (m, 5H), 7,00 (t, J=6,8 Hz, 1H), 7,14 (d, J=8.5 Hz, 2H), 7,38 (d, J=8,4 Hz, 1H), 7,45-of 7.48 (m, 2H), 7,68 (s, 1H), 7,75-7,83 (m, 3H), 8,20 (Shir.s, 1H), 11,48 (s, 1H). Analysis: Calculated for C40H46N4O7: 69,14, H 6,67, N 8,06. Found: 69,16, H 6,88, N 7,63. The connection 45 3,4-Dihydro-2-{ 2-[4-(2- gbom It and rubbing with ether. Specified in the title compound are obtained in the form of a white solid product with a yield of 80%, so pl. 173-178oC; IR (KBR) 3154, 1680, 1501, 1400, 1241, 752 cm-1;1H NMR (DMSO-d6) 2,22 to 2.35 (m, 1H), 2,38-2,48 (m, 1H), 2,72 (t, J=7,3 Hz, 2H), 3,28-to 3.38 (m, 2H), 4,17-4.26 deaths (m, 2H), of 5.05 (DD, J=8,7, 4.0 Hz, 1H), 5,34 (ABq, JAB= 16.2 Hz, 2H), 6,80-7,80 (PTS.Shir.s, 4H), 6,92-7,01 (m, 4H), was 7.08 (t, J=7,3 Hz, 2H), 7,20 (d, J=8,4 Hz, 2H), 7,43 (d, J=8,4 Hz, 1H), of 7.48-7,51 (m, 2H), to 7.59 (Shir.t, J=5,1 Hz, 1H), 7,78 (s, 1H), 7,83-to $ 7.91 (m, 3H); MN+at m/z=495. Analysis: Calculated for C30H30N4ABOUT3HCl 0,7 N2O: 66,28, H 6,01, N 10,31. Found: To 66.30, H 5,88, N 10,06. The connection 46 3,4-Dihydro-2-{ 2-[4-(2- guanidinate)phenoxy] ethyl} -3-oxo-2H-4-(3 - thienylmethyl)-1,4-benzoxazin < / BR> Obtained by method L using intermediate product 11721-108-1 (reference example 85) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine and method For using triperoxonane acid present anisole instead of IPA/HCl. The crude product was purified flash chromatography using a gradient from 1% Meon in CH2Cl2up to 6% of the Meon/1% NH4OH in CH2Cl2and provided with an outlet 48% in the form of a reddish-brown foam, so pl. 66-71oC; IR (KBR) 3364, 1655, 1500, 1246, 1203, 1136, 751 cm-1;1H NMR (DMSO-d6) 2,11-of 2.26 (m , ,99-7,04 (m, 5H), 7,12-7,22 (m, 2H), 7,19 (d, J= 8.6 Hz, 2H), 7,40 (d, J=2.3 Hz, 1H), 7,52 (DD, J=4,6, and 2.3 Hz, 1H), 7.62mm (t, J=5,75 Hz, 1H); MH+ at m/z=451. Analysis: Calculated for C24H26N4O3S2HF3O2: 51,61, H 4,39, N CENT TO 8.85. Found: 51,34, H 4,60, N Cent To 8.85. Connection 47 2-{ 2-[4-[2-(N,N-Bis-tert - butoxycarbonylamino)ethyl]-phenoxy] ethyl} -4-(2-chloro-4-thienylmethyl) -3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from 10508-79 (reference example 80) by method L using equal equivalents of reagents relative to the source material and extracted as a white foam with a yield of 24%; IR (KBR) 3330, 2978, 1722, 1686, 1638, 1615, 1500, 1413, 1331, 1247, 1130, 1058, 748 cm-1;1H NMR (CDCl3) to 1.48 (s, N) and 1.51 (s, N), 2,20 of-2.32 (m, 1H), 2,81 (t, J=7.2 Hz, 2H), 3,60-3,66 (m, 2H), 4,12-to 4.28 (m, 2H), 4,78 (DD, J=9,3, 4.0 Hz, 1H), 5,16 (ABq, JAB=to 15.8 Hz, 2H), 6.75 in (d, J=3.8 Hz, 1H), 6,82-6,85 (m, 3H), 7,00-was 7.08 (m, 4H), 7,12 (d, J=8.6 Hz, 2H), of 8.37 (t, J=3.5 Hz, 1H), 11,47 (s, 1H). Analysis: Calculated for C34H41ClN4O7S: 59,60, H 6,03, N 8,18. Found: 59,27, Of 6.02 H, N 8,01. The connection 48 4-(2-Chloro-4-thienylmethyl)- 3,4-dihydro-2-{2-[4-(2- guanidino-ethyl)phenoxy] ethyl}-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from compound 47 way To exit the crude product is 88%. This crude material was videlacele using etilize is UP>H NMR (CDCl3) 2,04-of 2.23 (m, 3H), 2,30-to 2.41 (m, 1H), 2,72-and 2.83 (m, 2H), 3,28 is 3.40 (m, 2H), 3,97-to 4.15 (m, 2H), 4,77 (DD, J=7,7, 3,4 Hz, 1H), is 5.06 (ABq, JAB=14,5 Hz, 2H), 6,69-7,20 (PTS.Shir.s, 4H), 6,69-to 6.80 (m, 3H), 6,92-7,06 (m, 5H), 7,11 (d, J=8.1 Hz, 2H), to 7.64 (Shir.s, 1H). Analysis: Calculated for C24H25ClN4OCS Hcl H2O: 53,43, H 5,23, N ACCOUNTED FOR 10.39. Found: 53,08, H 5,27, N 10,32. The connection 49 2-{ 2-[4-[2-(N,N-Bis-tert - butoxycarbonylamino)ethyl] -phenoxy]ethyl} -6-chloro-4-(3 - Chlorobenzyl)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from 11578-71 (reference example 49) method L using equal equivalents of reagents relative to the starting material and isolated in the form of a colourless oil with a yield of 34% after chromatography (elution CH2Cl2); IR (net) 3332, 2978, 1721, 1694, 1638, 1615, 1498, 1415, 1367, 1132, 811, 777 cm-1;1H NMR (CDCl3) to 1.48 (s, N) and 1.51 (s, N), 2,25-is 2.37 (m, 1H), 2,54-of 2.66 (m, 1H), 2,82 (t, J=7.2 Hz, 2H), 3,63 (kV, J=5.6 Hz, 2H), 4,16-of 4.25 (m, 2H), 4,94 (DD, J=9,3, 3,9 Hz, 1H), 5,09 (ABq,AB=16.1 Hz, 2H), 6,80 (s, 1H), 6,85 (d, J=8.5 Hz, 2H), 6,95 (s, 2H), 7,13 (d, J=8,5 Hz, 3H), 7.23 percent-7,31 (m, 3H), of 8.37 (Shir.t, J=2 Hz, 1H), 11,47 (s, 1H). Analysis: Calculated for C36H42CL2N4O7: 60,59, H 5,93, N OF 7.85. Found: 60,65, H 6,04, N 7,65. The connection 50 6-Chloro-4-(3-Chlorobenzyl) -2-{2-[4-(2-guanidinate) phenoxy]-ethyl} is de white foam of CH2Cl2with the release of 28%; IR (KBR) 3154, 1684, 1668, 1496, 1376, 1264, 1243, 1092 cm-1;1H NMR (CDCl3) 2,13-of 2.27 (m, 1H), 2,35-of 2.50 (m, 1H), 2,74 (Shir.s, 2H), 3,31 (Shir.s, 2H), 4,00-to 4.14 (m, 2H), 4,84 (DD, J=9,0, 4,2 Hz, 1H), to 4.98 (ABq, JAB=17.5 Hz, 2H), 6.73 x-7,29 (m, 15 NM), to 7.61 (Shir.s, 1H); MN+at m/z=513. Analysis: Calculated for C26H26CL2N4ABOUT3HCl 0,7 N2O: 55,61, H 5,26, N 9,75. Found: 55,83, H 5,01, N 9,51. The connection 51 2-{ 2-[4-[2-(N,N-Bis-tert - butoxycarbonylamino)ethyl] -phenoxy]ethyl} -4-(3-Chlorobenzyl) -3,4-dihydro-3-oxo-6-phenyl-2H-1,4-benzoxazin < / BR> Obtained from 11578-41 (reference example 44) method L and isolated in the form of an oil with a yield of 46%. This material was led from a mixture of ether/hexane, obtaining a white crystalline solid product, so pl. 115-116oC; IR (KBR) 2976, 2931, 1724, 1689, 1642, 1614, 1430, 1336, 1135, 766 cm-1;1H NMR (CDCl3) to 1.48 (s, N), 1,50 (s, N), 2,30 is 2.43 (m, 1H), 2,35 is 2.46 (m, 1H), 2,81 (t, J= 7,3 Hz, 2H), 3,63 (kV, J=7,1 Hz, 2H), 4,17-4,32 (m, 2H), 4,99 (DD, J= 9,3, 3,9 Hz, 1H), 5,18 (ABq, JAB=25,7 Hz, 2H), 6.87 in (d, J=8.5 Hz, 2H),? 7.04 baby mortality-7,40 (m, 14N), scored 8.38 (t, J=4.3 Hz, 1H), 11,47 (Shir.s, 1H). Analysis: Calculated for C42H47ClN4O7: 66,79, H 6,27, N 7,42. Found: 66,49, H 6,20, N 7,34. The connection 52 4-(3-Chlorobenzyl)-3,4-dihydro-2-{ 2-[4-(2-guanidinate) -phenoxy]ethyl}-3-oxo - 6-f the m 20%; IR (KBR) 3149, 1666, 1609, 1512, 1241, 1076, 1051, 761 cm-1;1H NMR (CD3OD) 2,31-to 2.40 (m, 1H), 2,43-of 2.54 (m, 1H), 2,81 (t, J=7.2 Hz, 2H), 3,41 (t, J= 7,0 Hz, 2H), 4,20-or 4.31 (m, 2H), 4,85 (s, 5H plus CD3HE, of 4.99 (DD, J=11,1, 4.5 Hz, 1H), 5,28 (s, 2H), 6,91 (d, J=8.6 Hz, 2H), was 7.08 (d, J= 8,3 Hz, 1H), 7,12-the 7.43 (m, 13H). Analysis: Calculated for C32H31ClN4O3HCl 1.4 N2O: 62,32, H 5,69, N REMAINING 9.08. Found: Of 61.95, H 5,51, N 9,27. The connection 53 2-{2-[4-[2-(N,N'-Bis-tert - butoxycarbonylamino)ethyl] -phenoxy]ethyl} -4-(3-Chlorobenzyl)-3,4-dihydro-3-oxo-6-trifluoromethyl-2H-1,4-benzoxazin < / BR> Obtained from 11578-56 (reference example 50) by method L using equal equivalents of reagents and isolated in the form of a colourless oil with a yield of 18% after column chromatography on SiO2(CH2Cl2); IR (KBR) 3333, 2979, 1723, 1696, 1639, 1617, 1453, 1330, 1303, 1165, 1129, 824 cm-1: 1H NMR (DCl3) to 1.48 (s, N) and 1.51 (s, N), and 2.26-2.40 a (m, 1H), 2,55-to 2.67 (m, 1H), 2,82 (t, J= 7,1 Hz, 2H), 3,63 (kV, J=5.4 Hz, 2H), 4,06-4,27 (m, 2H), 5,02 (DD, J= 9,2, 3,9 Hz, 1H), 5,14 (ABq, JAB=16.1 Hz, 2H), at 6.84 (d, J=8.5 Hz, 2H), 7,05-7,17 (m, 3H), 7,13 (d, J=8.5 Hz, 2H), 7.23 percent-7,30 (m, 4H), of 8.37 (Shir.t, J=4.3 Hz, 1H), 11,48 (s, 1H). Analysis: Calculated for C37H42ClF3N4O3: 59,48, H 5,67, N 7,50. Found: 59,60, H 5,67, N 7,39. The connection 54 4-(3-Chlorobenzyl)-3,4-dihydro-2-{ 2-[4-(2- se the m K and extracted as a white foam with a yield of 27%; IR (KBR) 3336, 3159, 1667, 1453, 1304, 827 cm-1;1H NMR (DCl3) 2,20-2,39 (m, 1H), 2,48 (Shir.s, 3H), 2,77 (Shir.s, 2H), 3,35 (Shir.s, 2H), 4,08 (Shir.s, 2H), is 4.93 (DD, J=8,6, 4.0 Hz, 1H), is 5.06 (ABq, JAB=16,8 Hz, 2H), 6.75 in-7,30 (PTS. Shir. s, 4H), 6,77 (d, J=7.7 Hz, 2H), 7,01-7,26 (m, 7H), 7,25 (d, J=7,1 Hz, 2H), to 7.64 (PTS.Shir.s, 1H); MN+at m/z=547. Analysis: Calculated for C27H26ClF3N4ABOUT3HCl 0,7 N2O: 54,41, H 4,80, N 9,40. Found: 54,49, H 4,74, N To 9.32. The connection 55 4-(3-Chlorobenzyl)-3,4-dihydro-7-fluoro-2-{2[4-(2- guanidinate)-phenoxy] ethyl}-3-oxo-2H - 1,4-benzoxazin < / BR> Obtained from 11578-47 (reference example 52) and N,N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine by method L using equal equivalents of reagents and method K. the Product was isolated as a white foam with a total yield 17%; IR (KBR) 2877, 1664, 1509, 1405, 1243, 1154, 852 cm-1;1H NMR (CD3OD) and 2.26-is 2.37 (m, 1H), 2,42 of $ 2.53 (m, 1H), and 2.83 (t, J=6,8 Hz, 2H), 3,42 (t, J=6,8 Hz, 2H), 4,17-the 4.29 (m, 2H), 4,84 (s, 6.4 N plus CD3IT), to 4.98 (DD, J= 8,4, 4,4 Hz, 1H), 5,18 (s, 2H), 6.73 x (TD, J=8,8, 2.6 Hz, 1H), 6,83 (DD, J= 9,2, 2.8 Hz, 1H), 6,92 (d, J=8.0 Hz, 2H), 6,97 (DD, J=8,8, 5,2 Hz, 1H), 7,17 (d, J= 8 Hz, 2H), 7,17-7,22 (m, 1H), 7,25-7,35 (m, 3H); MH+at m/z=497. Analysis: Calculated for C26H26ClFN4O3HCl 0,7 H2O: 57,19, H 5,24, N 10,26. Found: 56,81, H Are 5.36, N 10,26. C4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from 11578-33 (reference example 56) and N,N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine by method L using equal equivalents of reagents relative to the starting material and isolated in the form of a white solid product with a yield of 27% after column chromatography on SiO2with elution CH2Cl2so pl. 115-117oC; IR (KBR) 2977, 1699, 1639, 1615, 1593, 1367, 1131, 1058, 810, 776 cm-1:1H NMR (CDCl3) to 1.48 (s, N) and 1.51 (s, N), 2,25-is 2.37 (m, 1H), 2,52-to 2.67 (m, 1H), 2,82 (t, J=7.2 Hz, 2H), 3,63 (kV, J= 7,1 Hz, 2H), 4,13-4,24 (m, 1H), 4,27 is 4.35 (m, 1H), of 5.05 (DD, J=9,7, 3.5 Hz, 1H), 5,10 (s, 2H), of 6.71 (d, J=2.2 Hz, 1H), 6,86 (d, J=8.6 Hz, 2H), 7,05 (d, J=2.2 Hz, 1H), 7,13 (d, J=8.6 Hz, 2H), 7,13 (s, 1H), 7,26-7,29 (m, 3H), of 8.37 (t, J=2,6 Hz, 1H), 11,48 (s, 1H). Analysis: Calculated for C36H41Cl3N4O7: 57,80, H 5,52, N 7,49. Found: 57,64, H 5,39, N To 7.77. Connection 57 4-(3-Chlorobenzyl)-6,8-dichloro-2-{2-[4-(2-guanidinate) -phenoxy]ethyl}-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from compound 56 way To and allocated in the form of a white foam with a yield of 75%; IR (KBR) 3150, 1666, 1591, 1479, 1242, 743 cm-1;1H NMR (DMSO-d6) 2,23-is 2.37 (m, 1H), 2,50-2,61 (m, 1H), 2,84 (t, J=7,1 Hz, 2H), 3,39 (kV, J= 5,9 Hz, 2H), 4,15-to 4.23 (m, 1H), 4,25 is 4.35 (m, 1H), 5,04 (DD, J=9,8, and 3.8 Hz, 1H), 5,11 (ABq, JAB=16,3 Hz, 2H), 6.75 in (d, J=2.2 Hz, 1H), 6.87 in (d, J=8,4 Hz, 2H), 7,07-7,21 SUB>3H4O3HCl 0,7 N2O: 52,31, H 4,63, N 9,39. Found: 52,37, H 4,59, N 9,37. The connection 58 4-(3-Chlorobenzyl)-2-{ 2-[4-(2- guanidinate)phenoxy] ethyl}-3,4-dihydro-7-methyl-3-oxo-2H-1,4-benzoxazin < / BR> Obtained by method L using intermediate product 11578-52 (reference example 55) and N, N'-di-tert-butoxy-carbonyl-2-(4-hydroxyphenyl)ethylguanidine and way in the form of a white foam with a total yield of 2.5%; IR (KBR) 3340, 3161, 1668, 1402, 1244, 1178, 1146, 1107, 1056 cm-1;1H NMR (DCl3) 2,15-of 2.28 (m, 1H), measuring 2.20 (s, 3H), 2,34-2,47 (m, 3H), was 2.76 (t, J=6.4 Hz, 2H), 3,30 is 3.40 (m, 2H), 4,00-4,18 (m, 2H), a 4.83 (DD, J=8,9, a 4.3 Hz, 1H), free 5.01 (s, 2H), 6,63-7,27 (PTS.Shir.s, 4H), 6,63-6,70 (m, 2H), 6.75 in-6,83 (m, 2H), 7.03 is-of 7.23 (m, 7H), 7,63 (Shir.s, 1H); MH+ at m/z=493. Analysis: Calculated for C27H29Cl3N4O3HCl H2O: 59,23, H OF 5.89, N 10,23. Found: 58,84, H Ceiling Of 5.60, N 10,07. Connection 59 2-{2-[4-[2-(N,N'-Bis-tert - butoxycarbonylamino)ethyl]-phenoxy] ethyl} -3,4-dihydro-4-methyl-3 - oxo-2H-1,4-benzoxazin < / BR> Obtained from 10840-117-1 (reference example 88) by method L and isolated in the form of a white foam with a yield of 13%; IR (KBr) 3334, 2978, 2933, 1722, 1686, 1639, 1614, 1513, 1504, 1417, 1131, 750 cm-1:1H NMR (CDCl3) to 1.48 (s, N), 1,50 (s, N), 2,19-2,31 (m, 1H), 2,45-of 2.56 (m, 1H), 2,81 (t, J=7.2 Hz, 2H), 3,38 (s, 3H), 3,63 (kV, J=5.3 Hz, 2H), 4,10-4.26 deaths (m, 2H), a 4.83 (DD, J=8,8, 4,for C30H40N4ABOUT70,2 H2O: 62,96, H 7,12, N 9,79. Found: 62,88, H 7,20, N 9,71. The connection 60 3, 4-Dihydro-2-{ 2-[4-(2- guanidinate)phenoxy] ethyl}-4-methyl-3-oxo - 2H-1,4-benzoxazin < / BR> Obtained by dissolving compound 59 in CH2Cl2and processing triperoxonane acid (TFU). The solvent was removed and the residue was purified by chromatography on SiO2(26% Meon in CH2Cl2) followed by crystallization from a mixture of Meon/CH2Cl2/ether, obtaining a product with the release of 82% in the form of a cream solid, so pl. 80o(Compressed), 82-85oC; IR (KBR) 3339, 3176, 1682, 1515, 1505, 1383, 1249, 1137, 755 cm-1;1H NMR (DMSO-d6) 2,08-of 2.16 (m, 1H), 2,27 is 2.33 (m, 1H), 2,71 (t, J=7.5 Hz, 2H), 3.27 to the 3.35 (m, 2H), 3,30 (s, 3H), 4,10-4,18 (m, 2H), to 4.81 (DD, J=8,8, 4,2 Hz, 1H), 6,83-7,50 (PTS.Shir.s, 4H), of 6.90 (d, J= 8.6 Hz, 2H), 7,00 for 7.12 (m, 4H), 7,18 (d, J=8.7 Hz, 2H), 7,56 (Shir.t, J=5.7 Hz, 1H); MN+at m/z=369. The connection 61 3,4-Dihydro-2-{ 2-[4-(2- guanidinate)phenoxy] ethyl} -3-oxo-4-pentyl - 2H-1,4-benzoxazin < / BR> Obtained from intermediate 10840-185 (reference example 60) way To and allocated in the form of a colorless glassy product with a yield of 98%; IR (KBR) 3154, 1661, 1513, 1500, 1244, 751 cm-1;1H NMR (CDCl3) to 0.88 (t, J= 6.5 Hz, 3H), 1,19 (d, isopropanol), of 1.25 to 1.37 (m, 4H), 1 J= 8,7, 4.0 Hz, 1H), 6,70-7,17 (PTS. Shir.s, 4H), 6,78 (d, J=7.5 Hz, 2H), 6,93-7,07 (m, 4H), 7,13 (d, J=7,4, 2H), to 7.67 (Shir.d, 1H); MN+at m/z=425. Analysis: Calculated for C24H32N4O3HCl 0.1 s3H8ABOUT 0.6 N2ABOUT: 61,00, H 7,38, N 11,73. Found: 61,04, H 7,27, N 11,67. The connection 62 4-(3-Chlorobenzyl)-3,4-dihydro-2-[2-[4-(2-guanidinate) phenoxy] ethyl] -3-oxo-2H-pyrido [4,3-b]-1, 4-oxazin < / BR> Obtained by method L using intermediate product 11578-190 (reference example 84) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine and the way To as not quite white foam with a yield of 35%; IR (KBR) 3134, 1701, 1669, 1642, 1508, 1240, 1178, 1161, 1055, 824 cm-1;1H NMR (DMSO-d6) of 2.50 (m, 1H plus DMSO-d5), a 2.71 (t, J=7.5 Hz, 2H), 3,28-to 3.35 (m, 3H), 4,17 (t, J=5.6 Hz, 2H), 5.25-inch (ABq, JAB=16.5 Hz, 2H), 5,52 (t, J=6,9, 1H), 6,70-7,60 (PTS. Shir.s, 5H), 6,83 (d, J=8,4 Hz, 2H), 7,18 (d, J=8,4 Hz, 2H), 7,28-7,40 (m, 3H), of 7.48 (s, 1H), 7,50 (s, 1 H), to 7.67 (t, J=5.4 Hz, 1H), 8,39 (s, 1H), 8,40 (s, 1H); MN+at m/z=480. Analysis: Calculated for C25H26ClN5O32HCl 1,5 H2O: 51,78, H 5,39, N 12,08. Found: 51,78, H 5,39, N 12,08. Connection 63 2-{ 2-[3-[2-(N,N-Bis-tert - butoxycarbonylamino)ethyl]-phenoxy] ethyl} -4-(3,5-dichlorobenzyl)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from 10005-181-1 (reference Prime,5 to 10% ethyl acetate in CH2Cl2and crystallization from a mixture of CH2CL2/ether/hexane, so pl. 116-118oC; IR (KBR) 3359, 1688, 1505, 1256, 1171, 752 cm-1;1H NMR (CDCl3) of 1.44 (s, N), 2,28-2,39 (m, 1H), 2,52-2,62 (m, 1H), 2,77 (t, J=9 Hz, 2H), 3.33 and-to 3.41 (m, 2H), 4,16-4,30 (m, 2H), 4,54 (Shir. s, 1H), 4,94 (DD, J=10,5, 3 Hz, 1H), 5,09 (ABq, JAB=18 Hz, 2H), 6.75 in-6,83 (m, 4H), 6,93-7,06 (m, 3H), 7,13 (d, J=1.8 Hz, 2H), 7,20-7,27 (m, 2H). Analysis: Calculated for C30H32Cl2N2O5: 63,05, H 5,64, N 4,90. Found: 63,24, H Ceiling Of 5.60, N 4,71. The connection 64 2-{ 2-[3-(2-Aminoethyl) phenoxy] ethyl}-4-(3,5 - dichlorobenzyl)-3,4-dihydro-3-oxo-2H-benzoxazin < / BR> Obtained by method J using intermediate product 10005-181-1 (reference example 48) and 4-[2-(N-tert - butoxycarbonylamino)ethyl]phenol, as well as way because the Product is obtained in the form of a white solid with a yield of 58%, so pl. 173.5 metric-176oC; IR (KBR) 2942, 1684, 1592, 1501, 1399, 1265, 752 cm-1;1H NMR (DMSO-d6) 2,19 of-2.32 (m, 1H), 2,35-2,47 (m, 1H), 3,84-to 3.89 (m, 2H), 3,01-of 3.06 (m, 2H), 4,19-4,24 (m, 2H), 5,03-5,08 (m, 1H), 5,18 (ABq, JAB= 16.1 Hz, 2H), 6,83-6,87 (m, 3H), 6,99-to 7.09 (m, 4H), 7,25 (t, J=7,6 Hz, 1H), 7,35 (d, J=1.8 Hz, 2H), 7,52 (t, J=1.8 Hz, 1H), 8,06 (Shir.s, 3H). Analysis: Calculated for C25H24Cl2N2O3HCl 0,25 H2O: 58,61, H 5,02, N 5,47. Found: 58,47, H 4,88, N 5,33. The connection 65 2-{BR> < / BR> The intermediate product 10840-45 (1 EQ, reference example 92) was dissolved in 7 ml of a mixture of CH2CL2/ether (3/1) in the atmosphere of nitrogen and treated with triethylamine (1.2 EQ), then methanesulfonanilide (1.2 EQ). The mixture was stirred for 0.5 h and filtered. The filtrate was concentrated in vacuo and the residue was again dissolved in ether and washed with N2O and dried over MgSO4. After removal of the ether was received target methansulfonate product. This crude material (1 EQ) was dissolved in DMSO (1.7 ml) and was treated with the appropriate phenol (1 EQ) plus pellets of NaOH (3 EQ). This solution was stirred at 50oC for 24 h in nitrogen atmosphere and then was diluted with water. The solution of the precipitate in a mixture of CH2Cl2/ethyl acetate washed with water and dried over MgSO4. After removal of the solvent was obtained crude material which was purified flash chromatography, obtaining a product with a total yield of 16% in the form of a white powder; IR (KBR) 2979, 1723, 1650, 1625, 1513, 1246, 1156, 1133, 743 cm-1;1H NMR (CDCl3) to 1.47 (s, N), 1,50 (s, N), 2,03-2,17 (m, 2H), 2,33 (s, 3H), of 2.81 (t, J=7.2 Hz, 2H), 3,18 (DD, J=11,9, 7.2 Hz, 1H), 3,34 (DD, J=11,9, 2.5 Hz, 1H), 3,63 (kV, J= 6,8 Hz, 2H), 4,08-to 4.23 (m, 2H), of 4.38 is 4.45 (m, 3H), 6,62 (dt, J=7,5, 1.5 Hz, 1H), 6,69 (DD, J=7,5, 1.5 Hz, 1H), 6.75 in-6,84 (m, 2H), PC 6.82 (d, J=8.7 Hz, 2H), 7,12 (d, J=8.7 Hz, 2H), 7,16 (Shir.kV, JAB=2, H 7,50, N 8,69. Found: 68,65, H 7,24, N 8,56. Compound 66 3,4-Dihydro-2-{ 2-[4-[2- guanidinate] phenoxy] ethyl} -4-(4-methylbenzyl)-2H-1,4-benzoxazin < / BR> Obtained from compound 65 way To exit 3% and isolated in the form of a green powder after trituration with Cl3; IR (KBR) 3157, 1663, 1611, 1513, 1300, 1241, 743 cm-1;1H NMR (CD3OD) 2,04 with 2.14 (m, 2H), 2,30 (s, 3H), of 2.81 (t, J=7.2 Hz, 2H), 3,18 (DD, J=12,0, 8.0 Hz, 1H), 3,36-to 3.49 (m, 3H), 4,07-4,2 (m, 2H), 4,37-to 4.46 (m, 1H), 4,50 (s, 2H), 6,70-to 6.95 (m, 7H), 7,05-7,40 (m, N). Analysis: Calculated for C27H32N4O2HCl 1,75 H2O: 63,37, H 7,31, N OF 11.26. Found: 63,40, H 7,14, N 11,21. Connection 67 2-{2-[4-[2-(N,N'-Bis-tert - butoxycarbonylamino)ethyl]-phenoxy] ethyl} -4-(2,4-dichlorobenzyl) -3,4-dihydro-2H-1,4-benzoxazin < / BR> Obtained from 10840-8 (reference example 94) method L with a yield of 20% and extracted as a white foam; IR (KBR) 3336, 2979, 2932, 1723, 1640, 1617, 1366, 1133 cm-1;1H NMR (CDCl3) to 1.48 (s, N), 1,50 (s, N), 2,08-of 2.20 (m, 2H), of 2.81 (t, J= 7.2 Hz, 2H), and 3.31 (DD, J=11,7, 7.5 Hz, 1H), 3,41 (DD, J= 11,6, and 2.6 Hz, 1H), 3,64 (kV, J=6,5 Hz, 2H), 4,10-4,27 (m, 2H), of 4.44-4.53-in (m, 1H), 4,46 (s, 2H), of 6.45 (DD, J=8,0, 1.3 Hz, 1H), 6,65 (TD, J=7,6, and 1.4 Hz, 1H), 6,76 (TD, J= 7,8, and 1.6 Hz, 1H), 6,80-6,87 (m, 3H), 7,10-7,24 (m, 4H), 7,42 (d, J=1.9 Hz, 1H), 8,35 (t, J=4,1 Hz, 1H), 11,46 (s, 1H). Analysis: Calculated for C36H44Cl2N4 < / BR> Obtained from compound 67 way To with the release of 4.5% and highlighted in green glassy product; IR (net) 3334, 3166, 1665, 1611, 1513, 1246, 1219, 1046, 830 cm-1;1H NMR (DCl3) 1,74 (Shir.s, 2H), 1,94-of 2.15 (m, 2H), 2,80 (Shir. t, J= 5.6 Hz, 2H), 3,20-to 3.38 (m, 4H), was 4.02-4,18 (m, 2H), 4,32-4,47 (m, 1H), 4,42 (s, 2H), 6,35-7,40 (PTS.Shir.s, 4H), 6,41 (DD, J=8.0 a, 1,1 Hz, 1H), 6,61 (TD, J=7,6, 1.2 Hz, 1H), 6.73 x (TD, J=7,9, 1.5 Hz, 1H), 6,80 (d, J= 7.9 Hz, 2H), 7,10-7,20 (m, 5H), 7,39 (d, J=1.8 Hz, 1H), 7,80 (Shir.s, 1H); MH+ at m/z=499. Analysis: Calculated for C26H28Cl2N4O2HCl H2O: 56,38, H 5,64, N 10,11. Found: 56,68, H 5,41, N Becomes 9.97. Connection 69 2-{ 2-[3-(2-(tert - Butoxycarbonylamino)ethyl)phenoxy] ethyl}-4-(3-Chlorobenzyl) -3,4-dihydro-3-oxo-2H - 1,4-benzoxazin < / BR> Obtained from intermediate 10488-22 (reference example 66) and 3-[2-(N-tert-butoxycarbonylamino) ethyl]phenol method J. the Product was isolated with a yield of 82% after chromatography in the form of oil, which crystallized upon standing, so pl. 107-108oC; MS (CI) MN+the peak is not found; IR (KBR) 3319, 2986, 1597, 1532, 1505, 1468, 1445, 1402, 1368, 1323, 1271, 1171, 1061, 787, 752 cm-1; 1H NMR (DCl3) of 7.23 (m, 5H), 7,13 (m, 1H), 7,00 (m, 2H), 6,94 (m, 1H), 6,78 (m, 3H), by 5.18 (d, 1H, J=16.0 Hz), to 5.08 (d, 1H, J=16.0 Hz), 4,94 (DD, 1H, J=3,9, 9,2 Hz), 4,55 (Shir.s, 1H), 4,24 (m, 2H), 3,38 (m, 2H), was 2.76 (t, 2H, J=6.9 Hz), 2,58 (m, 1H), 2,34 (M5. Found: 66,28, H 6,13, N 5,02. The connection 70 2-{ 2-[3-(2-Aminoethyl) phenoxy]ethyl}-4-(3 - Chlorobenzyl)-3,4-dihydro-3-oxo-2H-benzoxazin < / BR> Obtained from compound 69 the way To with quantitative yield, so pl. 163oWith (dark), 169-171o(Melts); MS (CI) MH+437; IR (KBr) 2948, 1678, 1599, 1503, 1468, 1447, 1402, 1321, 1265, 1171, 1115, 1051, 939, 866 cm-1;1H NMR (DMSO-d6) 8,80-8,00 (PTS.Shir.s, 2H), 7,22 (m, 4H), 7,10 (m, 1H), 6,95 (m, 3H), to 6.80 (m, 4H), 5,13 (d, 1H, J=16,3 Hz), of 5.05 (d, 1H, J=16,3 Hz), 4,89 (DD, 1H, J= 3,8, 8,8 Hz), 4,19 (m, 2H), 3,28 (Shir.s, 2H), is 3.08 (Shir.s, 2H), 2.49 USD (m, 1H), and 2.27 (m, 1H), 2,52-1,50 (PTS.Shir.s, 1H). Analysis: Calculated for C25H25ClN2O3HCl: 63,43, H 5,54, N Of 5.92. Found: 63,16, H 5.40, Is N 5,73. Connection 71 2-{ 2-[4-[2-(N,N'-Bis-tert - butoxycarbonylamino)ethyl]-phenoxy]ethyl} -4-(3-Chlorobenzyl)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from 10488-22 (reference example 66) and N,N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine way J to yield 31%; so pl. 74-78oC; MS (FAB) MH+679; IR (KBr) 3332, 2979, 1723, 1688, 1501, 1414, 1368, 1329, 1246, 1132, 1059, 750 cm-1;1H NMR (DCl3) 11,47 (Shir.s, 1H), at 8.36 (Shir. t, 1H), 7,25 (s, 2H), 7,14 (d, 2H, J=3,7 Hz), 7,06 (m, 2H), 6,92 (m, 4H), at 6.84 (m, 2H), 5,19 (d, 1H, J=16.0 Hz), to 5.08 (d, 1H, J=16.0 Hz), 4,94 (DD, 1H, J=3,9, and 9.3 Hz), 4,22 (m, 2H), 3,63 (m, 2H), of 2.81 (t, 2H, J=7,2 Hz), 2,58 (m, 1H), 2,2,99, H TO 6.43, N 8,16. Found: 62,96, H 6,37, N 8,09. The connection 72 4-(3-Chlorobenzyl)-3,4-dihydro-2-{ 2-[4-(2-guanidinate)-phenoxy] ethyl} -2H-1,4-benzoxazin < / BR> Obtained from compound 71 way To exit 34%, so pl. 90-101oC; IR (KBR) 3355, 1501, 1468, 1402, 1244, 750 cm-1;1H NMR (DMSO-d6) to 7.68 (Shir. t, 1H), 7,50-6,80 (PTS.Shir.s, 1H), 7,35 (d, 1H, J=7,3 Hz), 7,20 (m, 4H), 7,03 (m, 4H), 6,92 (d, 2H, J=8,4 Hz), with 5.22 (d, 1H, J=16.5 Hz), 5,13 (d, 1H, J= 16.5 Hz), 5,00 (DD, 1H, J=4.2, and 8.7 Hz), is 4.21 (m, 2H), 2,72 (Shir.t, 2H), of 2.51 (m, 2H), 2,38 (Shir.s, 1H), 2,24 (Shir.s, 1H). Analysis: Calculated for C26H27lN4ABOUT32,5 HCl: 54,77, H 5,22, N 9,83. Found: From 54.99, H Of 5.34, N 9,79. Connection 73 2-{2-[3-(tert-Butoxycarbonylamino) phenoxy]ethyl}-4-(3-Chlorobenzyl)- 3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from 10488-22 (reference example 66) J with the release of 48%, so pl. 98-100oC; MS (CI) M+522 there is one Cl; IR (KBR) 3351, 2927, 1599, 1530, 1505, 1447, 1402, 1279, 1175, 1111, 1055, 939, 864 cm-1;1H NMR (CDCl3) of 7.24 (m, 5H), 7,13 (m, 1H), 7,00 (m, 2H), 6,92 (m, 1H), 6,83 (m, 3H), by 5.18 (d, 1H, J=16.0 Hz), 5,07 (d, 1H, J=16.0 Hz), is 4.93 (DD, 1H, J=3,9, 9,2 Hz), a 4.83 (Shir. s, 1H), 4,37-4,14 (Shir.m, 4H), 2,58 (m, 1H), 2,34 (m, 1H), 1,46 (s, N). Analysis: Calculated for C29H31ClN2O50,3 H2O: 65,92, H 6,03, N AND 5.30. Found: 65,95, H Of 5.99, N 5,22. Sweden from compound 73 way To with quantitative yield, so pl. 124-129oC; MS (CI) MH+423; IR (KBR) 2886, 1599, 1501, 1402, 1265, 1171, 1080, 1051, 885, 470 cm-1;1H NMR (DMSO-d6) 7,27 (m, 5H), 7,13 (m, 1H), 7,00 (m, 2H), 6,95 (m, 2H), 6.90 to (m, 2H), 6,83 (m, 2H), 5,17 (d, 1H, J=16.2 Hz), to 5.08 (d, 1H, J=16.2 Hz), 4,94 (DD, 1H, J=4.0 a, 9,2 Hz), 4.26 deaths (m, 2H), 3,82 (s, 2H), 2,59 (m, 1H), 2,34 (m, 1H). Analysis: Calculated for C24H23ClN2O3HCl 0,4 H2ABOUT: WITH 61,78, H ARE 5.36, N 6,00. Found: 61,78, H Are 5.36, N Of 5.83. Connection 75 2-{ 2-[4-(3-(tert - Butoxycarbonylamino)propyl] phenoxy] ethyl} -4-(3 - Chlorobenzyl)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from 10488-22 (reference example 66) and 4-[3-(N-tert-butoxycarbonylamino)propyl] phenol method L with a yield of 58%, so pl. 75-81oC; MS (FAB) MH+551; 3365, 2979, 2934, 1611, 1512, 1503, 1468, 1398, 1366, 1302, 1279, 1242, 1022, 997, 922 cm-1:1H NMR (CDCl3) of 7.24 (d, 4H, J=6.4 Hz), 7,12 (m, 2H), was 7.08 (d, 1H, J=8.6 Hz), 7,00 (m, 2H), 6,92 (m, 1 H), at 6.84 (m, 2H), 5,17 (d, 1H, J=16.0 Hz), to 5.08 (d, 1H, J=16.0 Hz), 4,94 (DD, 1H, J=3,9, 9,2 Hz), is 4.21 (m, 2H), as 3.14 (m, 2H), 2,59 (m, 2H), 2,32 (m, 1H), 1,78 (m, 2H), 1,44 (s, N). Analysis: Calculated for C30H33ClN2O5: 67,09, H IS 6.19, N 5,22. Found: 67,46, H Is 6.54, N Is 4.93. The connection 76 2-{ 2-[4-(3-Aminopropyl) phenoxy]ethyl}-4-(3 - Chlorobenzyl)-3, 4-dihydro-3-oxo-2H-benzoxazin < / BR> Obtained from compound 75 way To, so pl. 109-111oC; MS (CI) MH Analysis: Calculated for C26H27ClN2O3HCl H2O: 61,78, H 5,98, N, 5,54. Found: 61,91, H 6,07, N 5,62. Connection 77 2-{ 2-[4-[(N,N'-Bis-tert - butoxycarbonyl)guanidine] -phenoxy]ethyl} -4-(3 - Chlorobenzyl)-3,4-dihydro-3 - oxo-2H-1,4-benzoxazin < / BR> Obtained by method L using intermediate product 10488-22 (reference example 66) and N, N-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)methylguanine with the release of 52%, so pl. 74o(Compressed), 89-95o(Melts); MS (FAB) MH+665; IR (KBR) 3334, 2979, 1723, 1690, 1501, 1396, 1368, 1325, 1248, 1057, 810 cm-1; 1H NMR (CDCl3) to 11.52 (s, 1H), 8,49 (Shir. t, 1H), 7,24 (m, 4H), 7,13 (m, 1H), 6,99 (m, 3H), 6,92 (m, 2H), 6.89 in (d, 1H, J= 8.5 Hz), PC 6.82 (d, 1H, J=7.5 Hz), 5,18 (d, 1H, J=16.0 Hz), to 5.08 (d, 1H, J= 16.0 Hz), is 4.93 (DD, 1H, J=3,9, and 9.3 Hz), of 4.54 (d, 2H, J=4,9 Hz), 4,25 (m, 2H), 2,59 (m, 1H), 2,34 (m, 1H), 1,52 (s, N), 1,47 (s, N). Analysis: Calculated for C35H41ClN4O7H2O: 61,53, H 6,34, N 8,20. Found: 61,50, H 6,26, N 8,03. The connection 78 4-(3-Chlorobenzyl)-3,4-dihydro-2-{ 2-[4-(guanidinylation) -phenoxy]ethyl} -2H-1,4-benzoxazin < / BR> Retrieved from, 501, 1398, 1246, 1051, 750 cm-1;1H NMR (DMSO-d6) 8,03 (Shir.t, 1H, J=5,9 Hz), 7,35 (m, 5H), of 7.23 (m, 5H), 7,02 (m, 6N), 5,23 (d, 1H, J=16.5 Hz), 5,12 (d, 1H, J= 16.5 Hz), 5,00 (DD, 1H, J=4.2, and 8.7 Hz), the 4.29 (d, 2H, J=5,9 Hz), 4,22 (m, 2H), 2.40 a (m, 1H), 2,25 (m, 1H). Analysis: Calculated for C25H25lN4O3HCl H2O 0.1 C6H14: 58,23, H 5,61, N 10,61. Found: 58,51, H 5.40, Is N 10,81. Connection 79 2-{ 2-[4-(2-Aminoethyl)phenoxy] ethyl} -4-(3-Chlorobenzyl)-3,4-dihydro-3-oxo-2H-benzoxazin < / BR> Obtained from 10488-22 (reference example 66) and 4-[2-(N-tert-butoxycarbonylamino)ethyl]phenol method J and then the way To with quantitative yield, so to 140.5 square-143oC; MS (CI) MH+437; IR (KBr) 2930, 1885, 1591, 1503, 1466, 1437, 1398, 1323, 1182, 1138, 991, 879 cm-1;1NMR (DMSO-d6) 8,00 (Shir.s, 3H), 7,35 (m, 3H), 7,20 (m, 3H), 7,03 (m, 4H), 6,92 (d, 2H, J=8.6 Hz), 5,23 (d, 1H, J=16.5 Hz), 5,13 (d, 1H, J=16.4 Hz), 5,00 (DD, 1H, J=4.2, and 8.7 Hz), 4,19 (m, 2H), 2,98 (m, 2H), 2,82 (m, 2H), 2,39 (m, 1H), 2,22 (m, 1H). Analysis: Calculated for C25H25ClN2O3HCl: 63,43, H 5,54, N Of 5.92. Found: 63,26, H 5,46, N 5,86. The connection 80 2-{2-[4-(2- (N,N'-Bis-tert-butoxycarbonylamino) ethyl] phenoxy]ethyl} -4-(3-Chlorobenzyl)-3,4-dihydro-7-nitro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from intermediate 11653-35V (reference example 87) and N, N'-di-tert-+ 724; IR (KBr) 3329, 3119, 3090, 2977, 2933, 2420, 2287, 1575, 1475, 1080, 1057, 927, 855, 701, 576, 490 cm-1;1H NMR (CDCl3) 11,50 (Shir.s, 1H), of 8.37 (Shir.s, 1H), 7,88 (d, 1H, J= 2.4 Hz), 7,82 (DD, 1H, J=2,6, 8,8 Hz), 7,28 (d, 2H, J=5,1 Hz), 7,22 (s, 1H), 7,12 (m, 3H), 6.90 to (d, 1H, J=8,8 Hz), at 6.84 (d, 2H, J=8.5 Hz), 5,23 (d, 1H, J=16.4 Hz), 5,13 (d, 1H, J=16,3 Hz), is 5.06 (DD, 1H, J=3,4, and 9.1 Hz), to 4.23 (m, 2H), 3,63 (q, 2H, J=5.4 Hz), 2,82 (t, 2H, J=7,2 Hz), 2,65 (m, 1H), 2,37 (m, 1H), 1,50 (s, N), to 1.48 (s, N). Analysis: Calculated for C36H42ClN5O90.5 H2O: 58,97, H 5,91, N OF 9.55. Found: 58,97, H 6,00, 9,25 N. Connection 81 2-{ 2-[4-[2-(tert - Butoxycarbonylamino)ethyl] phenoxy] ethyl}-4-(3-Chlorobenzyl)-3,4 - dihydro-7-nitro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from intermediate 11653-35V (reference example 87) and N, N'-di-tert-butoxycarbonyl-2- (4-hydroxyphenyl)-ethylguanidine way J with a yield of 20%, so pl. 82-85oC; MS (CI) MN+582; IR (KBr) 3366, 3085, 2975, 2935, 1882, 1695, 1600, 1526, 1512, 1477, 1442, 1389, 1365, 1301, 1114, 999, 853, 665 cm-1;1H NMR (CDCl3) 7,88 (d, 1H, J=2,42 Hz), to 7.84 (DD, 1H, J= 8,82, 2.55 Hz), 7,28 (m, 4H), 7,22 (s, 1H), 7,12 (d, 2H, J=to 8.57 Hz), 6.90 to (d, 1H, J=8,84 Hz), 6,85 (d, 1H, J=at 8.60 Hz), 5,23 (d, 1H, J=16.2 Hz), 5,13 (d, 1H, J=16,3 Hz)that is 5.06 (DD, 1H, J=9,03, 3,94 Hz), 4.53-in (lat.s, 1H), 4,24 (m, 2H), 3.33 and (m, 2H), 2,74 (t, 2H, J=6,86 Hz), 2,62 (m, 1H), 2,37 (m, 1H), 1,44 (s, N). Analysis: Calculated for C30H34ClN3O7: 61,91, H 5,54, N 7,22. Nagel)- 3,4-dihydro-7-nitro-3 - oxo-2H-benzoxazine < / BR> Obtained from compound 81 way To exit 46%, so pl. 79o(Compressed), 92-96o(Melts); MS (CI) MH+482; IR (KBR) 3392, 2933, 2021, 1474, 1441, 1146, 1118, 928, 852, 701, 528 cm-1;1H NMR (DMSO-d6) 7,95 (Shir. s, 2H), 7,92 (d, 1H, J=2.5 Hz), 7,87 (m, 1H), 7,42 (s, 1H), was 7.36 (m, 2H), 7,24 (d, 2H, J=8,8 Hz), 7,16 (d, 2H, J=8.5 Hz), 6,92 (d, 2H, J=8.5 Hz), and 5.30 (d, 1H, J=16,8 Hz), 5,18 (m, 2H), 4,22 (m, 2H), 2,98 (t, 2H, J=8.6 Hz), 2,80 (t, 2H, J=8.6 Hz), of 2.38 (m, 1H), and 2.26 (m, 1H). Analysis: Calculated for C25H24ClN3O5HCl H2O: FROM 55,98, H 5,07, N 7,83. Found: 55,92, H 4,80, N Of 7.82. Connection 83 2-{ 2-[4-(N,N'-Bis-tert - butoxycarbonyloxyimino) -phenoxy]ethyl}-4-(3-Chlorobenzyl)-3,4 - dihydro-7-nitro-3-oxo - 2H-1,4-benzoxazin < / BR> Obtained from intermediate 11653-35V (reference example 87) and N, N'-di-tert-butoxycarbonyl -(4-hydroxyphenyl)methylguanine way J with the release of 65%, so pl. 67,5o(Compressed), 84-88o(Melts); MS (FAB) MH+710; IR (KBR) 3730, 3326, 3122, 3089, 2978, 2932, 2413, 1720, 1640, 1615, 1503, 1476, 1081, 931, 558 cm-1;1H NMR (CDCl3) 11,55 (Shir.s, 1H), 8,59 (Shir.s, 1H), of 7.90 (d, 1H, J=2.5 Hz), to 7.84 (DD, J=2.5 a, 8,8 Hz), 7,25 (m, 4H), 7,10 (m, 1H), 6,86 (m, 4H), 5,22 (d, 1H, J=16,3 Hz), and 5.30 (d, 1H, J=16,3 Hz), 5,10 (DD, 1H, J=3,4, and 9.1 Hz), 4,60 (m, 2H), 4,23 (m, 2H), 2,66 (m, 1H), of 2.38 (m, 1H) and 1.51 (s, N), 1,47 (s, N). Analysis: Calculated for C35H40 < / BR> Obtained from compound 83 way To with quantitative yield, so square (decomposes) >101oC; MS (FAB) MN+524; IR (KBr) 3326, 3156, 2968, 2878, 1695, 1665, 1599, 1513, 1473, 1441, 1389, 1178, 1148, 1022, 852, 472 cm-1;1H NMR (DMSO-d6) to 7.93 (d, 0.5 H, J=2,6 Hz), 7,89 (m, 1.5 H), 7.62mm (Shir.t, 1H), 7,43 (s, 1H), 7,40-6,65 (PTS.Shir.s, 3H), 7,35 (m, 2H), 7,27 (d, 2H, J= 8.6 Hz), 7,21 (d, 2H, J=8.6 Hz), 6,92 (d, 2H, J=8.6 Hz), 5,33 (d, 1H, J=16,7 Hz), 5,20 (d, m, 2H, J=16.5 Hz), 4,22 (m, 2H), 3,32 (m, 2H), by 2.73 (t, 2H, J= 7,3 Hz), to 2.41 (m, 1H), 2,32 (m, 1H). Analysis: Calculated for C26H26ClN5O5HCl H2O: 53,99, H OF 5.05, N 12,11. Found: 54,11, H 4,95, N 12,01. Connection 85 2-{ 2-[4-(2-(N,N-Bis-tert - butoxycarbonyl)guanidinate) -phenoxy]ethyl} -4-(2-Chlorobenzyl) -3,4-dihydro-7-nitro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from intermediate 11653-S (reference example 68) and N, N'-di-tert-butoxycarbonyl-2- (4-hydroxyphenyl) -ethylguanidine with the release of 85%, so pl. 69o(Compressed), 90-92o(Melts); MS (FAB) MN+724; IR (KBr) 3329, 3128, 2978, 2934, 1722, 1697, 1638, 1524, 1474, 1414, 1364, 1021, 933 cm-1;1H NMR (DCl3) 11,47 (Shir.s, 1H), of 8.37 (Shir.s, 1H), to $ 7.91 (DD, 1H, J= 2,4, 8,8 Hz), to 7.77 (d, 1H, J=2.5 Hz), 7,27 (m, 2H), 7,19 (Shir.s, 1H), 7,10 (m, 4H), 6,83 (d, 2H, J=8.6 Hz), 5,23 (d, 1H, J=17,9 Hz), 5,14 (d, 1H, J= 17,9 Hz), 5,09 (DD, 1H, J=4,1, 9.1 Hz), 4,20 (m, 2H), 3,63 (m, 2H), 2,82 (t, 2H, J=7,1 Hz), 2,62 (m, 1H), 2,37 (m, 1H), 1,50 () 59,38, H 6,04, N 9,63. Connection 86 2-{2-[4-[2-(N,N'-Bis-tert - butoxycarbonylamino)ethyl] -phenoxy]ethyl} -4-(2 - Chlorobenzyl)-3,4-dihydro-7-nitro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from intermediate 11653-24A (reference example 86) and N, N'-di-tert-butoxycarbonyl-2-(4-(hydroxyphenyl)ethylguanidine way L with a yield of 52% in the form of a yellow foam, so square (decomposition) >85oC; MS (FAB) MH+724; IR (KBR) 3335, 2979, 1637, 1527, 1390, 1341, 1156, 1059 cm-1;1H NMR (CDCl3) 11,48 (Shir.s, 1H), of 7.90 (d, 1H, J=2,50), 7,83 (DD, 1H, J=2,52, cent to 8.85), was 7.45 (d, 1H, J=of 7.90), 7,26 (m, 1H), 7,19 (m, 2H), 7,14 (d, 1H, J=charged 8.52), 6,94 (d, 1H, J= 7,68), 6,85 (d, 2H, J=8,50), to 6.80 (d, 1H, J=8,90), and 5.30 (d, 2H, J= 5,54), to 5.08 (DD, 1H, J=5,02), to 4.23 (m, 2H), 3,65 (m, 2H), 2,82 (t, 2H, J= 7,2), to 2.65 (m, 1H), 2,39 (m, 1H), 1,50 (s, N), to 1.48 (s, N). Analysis: Calculated for C36H42ClN5O9: 59,71, H 5,85, N 9,67. Found: 59,48, H Of 5.89, N 9,52. Connection 87 Monohydrochloride 4-(2-Chlorobenzyl)-3,4 - dihydro-2-{2-[4-(2-guanidinate) phenoxy]ethyl}-7-nitro-3 - oxo-2H-1,4-benzoxazine < / BR> Obtained from compound 86 way To exit 79%, so pl. 120-125oC; MS (CI) MH+524; IR (KBR) 3368, 3322, 3168, 2932, 2878, 1694, 1502, 1334, 1234, 1028, 806 cm-1;1H NMR (DMSO-d6) 7,92 (m, 1.5 H), of 7.90 (d, 0.5 H, J=7.9 Hz), 7,55 (m, 2H), 7,40-6,50 (PTS.Shir.s, 3H), 7,34 (t, 1H, J=7.5 Hz), 7,26 (t, 1H, J= 7.5 Hz), 7,20 (d, 2H, J=8.6 Hz), was 7.08 (m, 2H), 6,92 (>/P>Analysis: Calculated for C26H26lN5O5HCl H2O: 53,99, H OF 5.05, N 12,11. Found: 53,75, H 5,23, N 12,09. The connection 88 2-{2-[4-(2-(N,N'-Bis - tert-butoxycarbonylamino)-ethyl) phenoxy]ethyl} -4-(2-Chlorobenzyl) -3,4-dihydro-6-nitro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from intermediate 11653-44A (reference example 70) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)-ethylguanidine way L with a yield of 50%, so pl. 155o(Compressed), 160-163o(Melts). IR (KBR) 3345, 3108, 2980, 2934, 1723, 1701, 1529, 1338, 1126, 878 cm-1;1H NMR (CDCl3) 11,48 (Shir.s, 1H), scored 8.38 (Shir.s, 1H), to $ 7.91 (DD, 1H, J=2.5 a, 8,8 Hz), 7,69 (d, 1H, J= 2.5 Hz), 7,46 (DD, 1H, J=1,3, and 9.1 Hz), 7,20 (m, 1H), 7,12 (m, 4H), 7,01 (d, 1H, J=7,6 Hz), 6,83 (d, 2H, J=8.6 Hz), 5,31 (s, 2H), 5,11 (DD, 1H, J=4,0, the 8.9 Hz), 4,22 (m, 2H), 3,63 (m, 2H), 2,82 (t, 2H, J=7,2 Hz), 2,65 (m, 1H), 2,39 (m, 1H), 1,50 (s, N), to 1.48 (s, 1H). Analysis: Calculated for C36H42ClN5O9: 59,71, H 5,85, N 9,67. Found: 59,89, H Of 5.84, N Being 9.61. Connection 89 3,4-Dihydro-2-{ 2-[4-(2 -guanidinate)phenoxy] ethyl} - 6-nitro-4-(2-Chlorobenzyl) -3 oxo-2H-1,4-benzoxazin < / BR> Obtained from compound 88 way To exit 90%, so square (Razlog.) >85oC; MS (CI) MH+524; IR (KBR) 3335, 3156, 1651, 1524, 1515, 1446, 1343, 1269, 1243, 1108, 746 cm-1;1H NMR (DMSO-d6) 7,94 (DD, 1H, J=2,5, and 8.9 Hz), 7(m, 2H), 3,29 (m, 2H), 2,71 (t, 2H, J=7,7 Hz), 2,44 (m, 1H), 2,35 (m, 1H). Analysis: Calculated for C26H26lN5O5HCl 0.5 N2O: 54,87, H 4,94, N 12,02. Connection 90 3,4-Dihydro-2-{ 2- [4-(2-(N,N'-bis-tert-butoxycarbonyl-guanidino)ethyl) phenoxy]ethyl)-4 -(3-nitrobenzyl)-7-nitro-3-oxo-2H - 1,4-benzoxazin < / BR> Obtained from intermediate 11653-85-In-1 (reference example 67) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine way L with a yield of 41%, so square (Razlog.) >84oC; MS (CI) MH+735; IR (KBR) 3331, 2979, 2934, 1719, 1638, 1533, 1512, 1477, 1343, 1132, 812 cm-1;1H NMR (CDCl3) of $ 11.48 (s, 1H), of 8.37 (Shir.t, 1H), 8,16 (m, 1H), 8,12 (s, 1H), to $ 7.91 (d, 1H, J= 2.4 Hz), the 7.85 (DD, 1H, J=2,5, and 8.9 Hz), 7,54 (m, 2H), 7,13 (d, 2H, J=8.5 Hz), 6.89 in (d, 1H, J= 8,9 Hz), 6,83 (d, 1H, J=8.6 Hz), of 5.34 (d, 1H, J=16.6 Hz), at 5.27 (d, 1H, J=16,7 Hz), 5,10 (DD, 1H, J=4,0, a 8.9 Hz), 4,24 (m, 2H), 3,63 (q, 2H, J=7.0 Hz), 2,82 (t, 2H, J=7.2 Hz), 2.63 in (m, 1H), of 2.38 (m, 1H), 1,62 (Shir.s, 1H), 1,50 (s, N), to 1.48 (s, N). Analysis: Calculated for C36H42lN6ABOUT11: 58,85, H 5,76, N 11,44. Found: 58,73, H 5,77, N 11,34. Connection 91 3,4-Dihydro-2-{ 2-[4-(2- guanidinate)phenoxy] ethyl} -7-nitro-4-(3 - nitrobenzyl)-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from compound 90 way, so square (Razlog.) >90oC; MS (CI) MH+535; IR (KBR) 3336, 3155, 1696, 1602, 1528, 1390, 1343,7,55 (Shir.t, 1H), 7,51-6,65 (PTS. Shir. s, 3H), 7,31 (d, 1H, J=7,31 Hz), 7,20 (d, 2H, J=8.6 Hz), 6,91 (d, 2H, J= 8.6 Hz), 5,43 (d, 1H, J=16.6 Hz), of 5.34 (d, 1H, J=17.3 Hz), 5,23 (DD, 1H, J=4,1, to 8.7 Hz), is 4.21 (m, 2H), 3,30 (m, 2H), 2,71 (t, 2H, J=7,3 Hz) to 2.41 (m, 1H), 2,30 (m, 1H). Analysis: Calculated for C26H26N6O7HCl 0,7 N2O: 53,51, H 4,91, N 14,40. Found: 53,87, H 4,77, N 14,72. The connection 92 6-Amino-4-(3-Chlorobenzyl) -3,4-dihydro-2-{2-[4-(2- guanidino-ethyl)phenoxy] ethyl}-3-oxo-2H - 1,4-benzoxazin < / BR> 4-(3-Chlorobenzyl)-3,4-dihydro-2-{ 2-[4-(2-guanidinate) -phenoxy]ethyl} -6 - nitro-3-oxo-2H-1,4-benzoxazin (0.3 g) was heated in ethanol (5 ml) and N2O (4 ml) until complete dissolution. With stirring, was added iron powder (0,19 g, 6,8 EQ), then NH4Cl (0.02 g, 0.7 EQ) and the reaction was continued while boiling under reflux for 5 hours In the hot mixture was filtered through celite and the yellow filtrate was concentrated before the formation of a yellow oil. After drying in vacuum at 80oThe product was collected as a yellow solid with a yield of 85%, so square (Razlog.) >94oC; MS (CI) MN+494; IR (KBR) 3332, 1667, 1614, 1512, 1467, 1396, 1243, 830, 774, 680 cm-1;1H NMR (DMSO-d6) 7,66 (Shir.s, 1H), 7,58-6,50 (PTS.Shir.s, 3H), of 7.36 (m, 4H), 7,20 (m, 3H), 6,91 (d, 2H, J=8.6 Hz), 6,74 (d, 1H, J=8,4 Hz), of 6.26 (d, 1H, J= 2.2 Hz), 6,21 (DD, 1H, J=2,2, 8,4 Hz), 5.08 to 8 (m, 1H). Analysis: Calculated for C26H28ClN5O3HCl 0.5 H2O: 57,89, H 5,61, N 12,98. Found: 57,64, H 5,48, N 12,63. Connection 93 2-{2-[4-(2-(N,N'-Bis-tert - butoxycarbonylamino)-ethyl] phenoxy]ethyl} -4-(4 - nitrobenzyl)-3,4-dihydro-3 - oxo-2H-1,4-benzoxazin < / BR> Obtained from intermediate 11653-173 (reference example 71) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)-ethylguanidine way L with a yield of 61%, so square (Razlog.) >78oC; IR (KBR) 3331, 2977, 1722, 1689, 1638, 1513, 1500, 1467, 1278, 922, 859 cm-1; 1H NMR (CDCl3) 11,48 (Shir.s, 1H), of 8.37 (Shir. t, 1H), 8,19 (d, 2H, J=8,8 Hz), 7,41 (d, 2H, J=8,8 Hz), 7,13 (d, 2H, J=8.6 Hz), 7,03 (m, 2H), 6,92 (m, 1H), 6,85 (d, 2H, J=8.6 Hz), 6.75 in (d, 1H, J= 7.9 Hz), from 5.29 (d, 1H, J=16.7 Hertz), is 5.18 (d, 1H, J=16,7 Hz), of 4.95 (DD, 1H, J=3,9, and 9.3 Hz), 4,22 (m, 2H), to 3.64 (m, 2H), of 2.81 (t, 2H, J=7,3 Hz), 2,58 (m, 1H), 2,35 (m, 1H), 1,50 (s, N), to 1.48 (s, N). Analysis: Calculated for C36H43N5O90.5 H2O: 61,88, H 6,35, N 10,02. Found: 62,07, H 6,32, N 9,85. Connection 94 2-{2-[4-(2-(N,N'-Bis-tert - butoxycarbonylamino) -ethyl]phenoxy]ethyl} -3,4-dihydro-4-(3-nitrobenzyl)-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from intermediate 11653-180 (reference example 61) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)-ethylguanidine way L with a yield of 64%, so pl./SUP>;1H NMR (CDCl3) 11,50 (Shir.s, 1H), of 8.37 (Shir.t, 1H), 8,15 (s, 1H), 8,13 (s, 1H), 7,58 (d, 1H, J=7,7 Hz), 7,54 (m, 1H), 7,12 (d, 2H, J=8.6 Hz), 7,02 (m, 2H), 6,91 (m, 2H), 6,85 (d, 1H, J=8.6 Hz), 6,79 (d, 1H, J= 7,7 Hz), a 5.25 (s, 2H), to 4.98 (DD, 1H, J=3,9, and 9.4 Hz), 4,22 (m, 2H), 3,63 (m, 2H), of 2.81 (t, 2H, J=7,3 Hz), 2,58 (m, 1H), 2,34 (m, 1H), 1,50 (s, N), to 1.48 (s, N). Analysis: Calculated for C36H43N5O9H2O: 61,09, H 6,41, N 9,89. Found: 61,40, H 6,47, N Of 9.55. Connection 95 3,4-Dihydro-2-{ 2-[4-(2- guanidinate)phenoxy] ethyl} -4-(3-nitrobenzyl)-3 - oxo-2H-1,4-benzoxazin < / BR> Obtained from compound 94 way To exit 58%, so square (Razlog.) >79oC; MS (FAB) MN+490; IR (KBr) 3321, 3146, 1665, 1529, 1500, 1466, 1399, 1349, 1322, 1279, 1249, 1154, 1097, 1063, 1022, 924, 810, 687, 468 cm-1;1H NMR (DMSO-d6) 8,18 (s, 1H), 8,13 (d, 1H, J=7.9 Hz), to 7.68 (m, 1H), 7,60-6,40 (PTS.Shir.s, 3H), 7,39 (s, 1H), 7,20 (m, 2H), was 7.08 (m, 3H), 6,98 (m, 3H), 6,92 (d, 1H, J=8,4 Hz), are 5.36 (d, 1H, J=18.7 Hz), 5,28 (d, 1H, J=17,0 Hz), 5,02 (m, 1H), 4,28 (t, 1H, J=6.6 Hz), 4,18 (m, 1H), 3,35 (m, 3H), of 2.72 (t, 2H, J=6.3 Hz), 2.40 a (m, 1H), and 2.27 (m, 1H). Analysis: Calculated for C26H27N5O52,1 HCl: 55,16, H 5,18, N 12,37. Found: 55,08, H 5,23, N 12,21. Connection 96 2-{2-[4-(2-(N,N'-Bis-tert - butoxycarbonylamino)-ethyl) phenoxy]ethyl} -7-nitro-4-(4 - nitrobenzyl)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from 12279-11 (reference the use of the KBr) 3329, 3087, 2976, 2932, 2871, 1720, 1639, 1610, 1474, 1390, 1155, 1022, 882, 577, 461 cm-1;1H NMR (CDCl3) 11,49 (Shir.s, 1H), of 8.37 (Shir.t, 1H), 8,21 (d, 2H, J=8.7 Hz), to $ 7.91 (d, 1H, J=2.5 Hz), to 7.84 (DD, 1H, J=2,5, and 8.9 Hz), 7,40 (d, 2H, J=8.6 Hz), 7,14 (d, 2H, J=8.6 Hz), 6,83 (DD, 3H, J= 2.5 and 9.0 Hz), to 5.35 (d, 1H, J=15,4 Hz in), 5.25 (d, 1H, J=to 15.4 Hz), to 5.08 (DD, 1H, J=4,0, a 8.9 Hz), 4,22 (m, 2H), 3,63 (m, 2H), 2,82 (t, 2H, J=7.4 Hz), 2.63 in (m, 1H), of 2.38 (m, 1H), 1,50 (s, N), to 1.48 (s, N). Analysis: Calculated for C36H42N6O11WITH3H6ABOUT: 59,03, H 6,10, N OR 10.60. Found: 58,96, H 6,17, N 10,54. Connection 97 3,4-Dihydro-2-{ 2-[4-(2- guanidinate)phenoxy] ethyl} -7-nitro-4-(4 - nitrobenzyl)-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from compound 96 way To with quantitative yield, so square (Razlog. ) >141oC; MS (FAB) MN+535; IR (KBr) 3323, 3158, 2948, 1702, 1667, 1598, 1470, 1434, 1396, 1182, 1144, 1107, 1012, 995, 898, 860, 826 cm-1;1H NMR (DMSO-d6) by 8.22 (d, 2H, J=8,8 Hz), 7,92 (s, 1H), 7,89 (d, 1H, J=2.6 Hz), to 7.61 (m, 3H), 7,60-6,65 (PTS.Shir.s, 2H), 7.23 percent (m, 4H), 6,94 (d, 2H, J= 8.6 Hz), vs. 5.47 (d, 1H, J=17.3 Hz), are 5.36 (d, 1H, J=17.3 Hz), 5,27 (DD, 1H, J= 8,8, 4,2 Hz) to 4.23 (m, 2H), 3,35 (m, 2H), 2,74 (t, 2H, J=7.4 Hz), a 2.45 (m, 1H), of 2.38 (m, 1H). Analysis: Calculated for C26H26N6O7HCl 0,9 N2O 0,2 IPA: 53,32, H 5,11, N 14,02. Found: 53,07, H 4,84, N 13,74. Connection 98 2-{2-[4-(2-(N,N'-Bis-tert - butoxycarbonylamino)-ethyl) phenoxy]etiochol product 11653-174-A (reference example 73) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine with the release of 40% in the form of a yellow solid product, so square (Razlog. ) >65oC; MS (CI) MN+690; IR (KBr) 3330, 3151, 2978, 2934, 1723, 1694, 1616, 1528, 1502, 1302, 1277, 1228, 1087, 1022, 933, 880, 562, 464 cm-1;1H NMR (CDCl3) 11,40 (Shir.s, 1H), at 8.36 (Shir.s, 1H), 8,18 (d, 1H, J= 8,12 Hz), 7,42 (m, 2H), 7,10 (m, 2H), of 6.96 (m, 4H), 6,85 (m, 1H), 6.73 x (d, 2H, J= 8,27 Hz), 5,50 (d, 2H, J=17,95 Hz), of 4.95 (DD, 1H, J=9,59, 4,21 Hz) to 4.16 (m, 2H), of 3.56 (m, 2H), 2,77 (m, 2H), 2.57 m (m, 1H), 2,35 (m, 1H), 1,46 (s, N), 1,45 (s, N). Analysis: Calculated for C36H43N5O90,9 H2O: 61,25, H 6,40, N 9,92. Found: 60,79, H 6,76, N Accounted For 10.39. Connection 99 2-{2-[4-(2-(N,N'-Bis-tert - butoxycarbonylamino)-ethyl] phenoxy]ethyl} -3,4-dihydro-7-methoxy-4-(3-nitrobenzyl) -3-oxo-2H-1,4-benzoxazin < / BR> Obtained by method L of the intermediate product 12279-18-2 (reference example 63) and N,N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine exit 83%, so square (Razlog.) >71oC; MS (FAB) MH+720; IR (KBr) 3329, 2977, 2934, 1722, 1683, 1639, 1532, 1413, 1350, 1330, 1247, 1164, 1057, 916, 729, 529 cm-1;1H NMR (CDCl3) of $ 11.48 (s, 1H), of 8.37 (Shir.s, 1H), 8,15 (s, 1H), 8,12 (s, 1H), 7,53 (m, 2H), 7,13 (d, 2H, J=8,62 Hz) 6,86 (d, 2H, J=8,62 Hz), of 6.68 (d, 1H, J=8,88 Hz), is 6.61 (d, 1H, J=2,72 Hz), 6,47 (DD, 1H, J=cent to 8.85, 2,70 Hz), to 5.21 (s, 2H), 4,96 (DD, 1H, J=9,36, 3,95 Hz) to 4.23 (m, 2H), 3,74 (s, 3H), 3,63 (m, 2H), of 2.81 (t, 2H, J=7,22 Hz),H 6,30, N 9,73. Found: 61,24, H To 6.43, N 9,76. Connection 100 3,4-Dihydro-2-{ 2-[4-(2- guanidinate)phenoxy] ethyl} -7-methoxy-4-(3 - nitrobenzyl)-3-oxo - 2H-1,4-benzoxazin < / BR> Obtained from compound 99 way To exit 87%, so square (Razlog.) >68oC; MS (CI) MH+520; IR (KBR) 3317, 3147, 2930, 1466, 1407, 1357, 1324, 1309, 1163, 1135, 922, 798, 669, 530 cm-1;1H NMR (DMSO-d6) is 8.16 (s, 1H), 8,13 (d, 1H, J=8,28 Hz), 7,66 (m, 2H), 7,60 (t, 2H, J=7,30 Hz), 7,53-6,70 (PTS. Shir. s, 2H), 7,20 (d, 2H, J=8,48 Hz), 7,01 (d, 1H, J=8,92 Hz), 6,92 (d, 2H, J= 8,48 Hz), 6,69 (d, 1H, J=2,79 Hz), 6,55 (DD, 1H, J=2,70, 8,88 Hz), 5,28 (d, 2H, J=2,72 Hz), to 4.98 (DD, 1H, J=4,05, 8,81 Hz), 4,20 (m, 2H), 3,68 (s, 3H), of 3.32 (m, 2H), 2,71 (t, 2H, J=7,16 Hz), is 2.37 (m, 1H), 2,23 (m, 1H). Analysis: Calculated for C27H29N5O6HCl 0.5 N2O: 57,39, H OF 5.53, N KZT 12.39. Found: 57,71, H 5,90, N 11,99. Connection 101 4-(3-Aminobenzyl)-2-(2-[4-(2- (N,N'-bis-tert-butoxy-carbonylcyanide) ethyl)phenoxy]ethyl}-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained by method L of the intermediate product 12279-13-A (reference example 65) and N,N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine and dedicated flash chromatography with elution with a mixture of acetone/hexane to yield 55% in the form of a white solid product, so square (Razlog.) >68oC; MS (FAB) MH+660; IR (KBR) 3335, 2977, 1722, 1685, 1638, 1512, 1500, 1466, 1408, 1366, 5 (d, 1H, J=8,48 Hz), only 6.64 (d, 1H, J=7,54 HZ), 6,56 (d, 1H, J=11,1 Hz), 5,07 (DD, 2H, J= 15,97, 24,50 Hz), is 4.93 (DD, 1H, J=3,83, 5,49 Hz) to 4.23 (m, 2H), 3,62 (m, 4H), of 2.81 (t, 2H, J=7,16 Hz), of 2.56 (m, 1H), 2,33 (m, 1H), of 1.50 (s, N), to 1.48 (s, N). Analysis: Calculated for C36H45N5O7: 65,54, H 6,87, N 10,61. Found: 65,43, H 6,92, N 10,38. Connection 102 2-{2-[4-(2-(N,N'-Bis-tert-butoxycarbonylamino)-ethyl] phenoxy]ethyl} -3,4-dihydro-6-fluoro-4-(3-nitrobenzyl) -3-oxo-2H-1,4-benzoxazin < / BR> Obtained by method L using intermediate product 12279-21 (reference example 64) and N,N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl) ethylguanidine exit 77%, so square (decomposition) >69oC; MS (FAB) MH+708; IR (KBR) 3330, 2978, 1696, 1638, 1533, 1507, 1453, 1415, 1350, 1249, 1155, 948, 670 cm-1;1H NMR (DlC) 11,47 (Shir.s, 1H), of 8.37 (Shir.t, 1H), 8,16 (d, 1H, J=7,1 Hz), 8,11 (Shir.s, 1H), 7,53 (m, 2H), 7,14 (d, 2H, J=8.6 Hz), 6,98 (DD, 1H, J= 5,1, an 8.9 Hz), 6,85 (d, 2H, J=8.6 Hz), 6,70 (m, 1H), 6,51 (DD, 1H, J= 2,8, and 9.4 Hz), to 5.21 (d, 1H, J=16.4 Hz), 5,20 (d, 1H, J=16.4 Hz), of 4.95 (DD, 1H, J=4.0 a, and 9.3 Hz), 4,22 (m, 2H), to 3.64 (m, 2H), of 2.81 (t, 2H, J=7,1 Hz), 2.63 in (m, 1H), 2,34 (m, 1H), 1,50 (s, N), to 1.48 (s, N). Analysis: Calculated for C36H42FN5ABOUT91,5 H2ABOUT: WITH 60,41, H 6,34, N 9,78. Found: 60,36, H 6,17, N 10,06. Connection 103 2-[2-{ 4-[2-(tert-Butoxycarbonylamino) ethyl] phenoxy}ethyl]-4-(4-carbomethoxy 81) and 4-[2-(N-tert-butoxycarbonylamino) ethyl] phenol by method L in the form of a white solid product with a yield of 69%, so pl. 110-112o;1H NMR (CDCl3) 8,00 (d, J=8,2 Hz, 2H), 7,30 (d, J=8,2 Hz, 2H), 7,10 (d, J=8,4 Hz, 2H), 6,98? 7.04 baby mortality (m, 2H), 6.89 in-to 6.95 (m, 3H), 6,78 (DD, J=1,3, 8.5 Hz, 1H), total of 5.21 (Shir.s, 2H), 4,96 (DD, J= 4,0, 9.5 Hz, 1H), 4,54 (Shir.with ledges, 1H), 4,15-4,30 (m, 2H), 3,90 (s, 3H), 3,31-to 3.36 (m, 2H), 2,74 (t, J=6,7 Hz, 2H), 2,53-2,63 (m, 1H), 2,33 (DDT, J=14,1, and 9.5, 4.8 Hz, 1H), 1,44 (s, N).13With NMR (CDCl3) 166,7, 166,4, 157,3, 155,9, 144,2, 141,3, 131,3, 130,2 (CH), 129,8 (CH), 129,5, 128,7, 126,5 (CH), 124,3 (CH), 122,9 (CH), 117,5 (CH), 115,3 (SN), TO 114.7 (CH), 76,6, 73,9 (CH), 63,1 (CH2), 52,1 (CH3), 45,2 (CH2), A 41.9 (CH2), 35,3 (CH2), 30,4 (CH2), 28,4 (CH3). IR 3376, 1713, 1684 cm-1. MS (FAB) 561 (MN+), 461, 324 (base). Analysis: Calculated for C32H36N2O7: 68,56, H 6,47, N 5,00. Found: 68,16, H 6,45, N 4,90. The connection 104 2-{ 2-[4-(2-Aminoethyl) phenoxy] ethyl}-4-(4-carbomethoxyamino) -3,4-dihydro-3-oxo-2H - 1,4-benzoxazin < / BR> Obtained from compound 103 way To using triperoxonane acid present anisole instead of IPA/HCl. The resulting solid product was washed with ether, receiving the product as a white powder (182 mg, yield 88%, so pl.=164-165oC).1H NMR (DMSO-d6) 8,40 (Shir.s, 3H), 7,98 (d, J=8,2 Hz, 2H), 7,32 (d, J=8,2 Hz, 2H), 7,13 (d, J=8.5 Hz, 2H), 6,77-7,01 (m, 6N), to 5.21 (s, 2H), 4,94 (DD, J=4.0 a, 9,3 Hz, 1H), 4,19-4,27 (m, 2H), 3,90 (s, 3H), 3,06-of 3.12 (m, 2H), 2,90-2,96 3,7 (CH), 122,3 (SN), OF 116.8 (CH), TO 114.7 (CH), 114,2 (CH), 73,1 (CH), 62,5 (CH2), 51,5 (CH3), 44,4 (CH2), 40,4 (CH2), 32,2 (CH2), AND 29.6 (CH2). IR 2700-3200 (W), 1722, 1705, 1680 cm-1. MS 461 (MN+). Analysis: Calculated for C27H28N2O5C2HF3O2: 60,62, H 5,09, N 4,88. Found: 60,31, H 5,07, N 4,78. Connection 105 2-[2-{ 4-[2-(tert-Butoxycarbonylamino )ethyl] phenoxy}ethyl]-4-(3-carbomethoxyamino) -3,4-dihydro-3-oxo-2H - 1,4-benzoxazin < / BR> Obtained from intermediate 11758-93-2A (reference example 82 4-[2-(N-tert-butoxycarbonylamino)ethyl] phenol by method L and isolated in the form of a white solid product with a yield of 66.2 per cent, so pl. 112-113o;1H NMR (CDC13) 7,93-to 7.95 (m, 2H), 7,38-7,41 (m, 2H), 7,10 (d, J=8.5 Hz, 2H), 6,88-7,02 (m, 3H), 6,86 (d, J= 8.5 Hz, 2H), for 6.81 (DD, J=1.5 and 7.7 Hz, 1H), 5,20 (s, 2H), 4,96 (DD, J=4.0 a, and 9.4 Hz, 1H), 4,51 (Shir.s, 1H), 4,18-4.26 deaths (m, 2H), 3,90 (s, 3H), 3,32-3,35 (Shir. m, 2H), by 2.73 (t, J=6.5 Hz, 2H), 2,55-2,60 (m, 1H), 2,32-of 2.38 (m, 1H), USD 1.43 (s, N). IR 3370, 1724, 1888 cm-1. MS (FAB) 561 (MN+), 324. Analysis: Calculated for C32H36N2O7: 68,56, H 6,47, N 5,00. Found: 68,37, H 6,63, N 4,88. The connection 106 2-{ 2-[4-(2-Aminoethyl )phenoxy] ethyl}-4-(3-carbomethoxyamino) -3,4-dihydro-3-oxo-2H - 1,4-benzoxazin < / BR> Obtained from compound 105 sposaro solid product with a yield of 92%, so pl.=112-114,5o; 1H NMR (DMSO-d6) of 7.90 (Shir. s, 1H), 7,86 (d, J=7.5 Hz, 1H), to 7.77 (Shir.s, 3H), 7,47-rate of 7.54 (m, 2H), 7,19 (d, J=8.5 Hz, 2H), 7,00-was 7.08 (m, 4H), to 6.95 (d, J=8.5 Hz, 2H), 5,26 (s, 2H), 5,00 (DD, J=4,0, a 8.9 Hz, 1H), 4,19-to 4.23 (m, 2H), of 3.84 (s, 3H), to 3.02 (t, J=7.8 Hz, 2H), and 2.79 (t, J=7.8 Hz, 2H), 2,35-to 2.40 (m, 1H), 2,23-of 2.28 (m, 1H). IR 2900-3100m (W), 1717, 1683 cm-1; MS 461 (MN+). Analysis: Calculated for C27H28N2O5WITH2HFCO2: 60,62, H 5,09, N 4,88. Found: 60,27, H 5,31, N 4,68. Connection 107 2-[2-{ 4-[2-(tert-Butoxycarbonylamino) ethyl]phenoxy}ethyl]-4-(2 - carbomethoxyamino)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from intermediate 11758 82-2 (reference example 83 4-[2-(N-tert-butoxycarbonylamino) ethyl] phenol by method L and isolated in the form of a white solid product with a yield of 76.9%, so pl. 103-105o;1H NMR (CDCl3) 8,07 (DD, J=1,5, with 7.6 Hz, 1H), 7,41 (dt, J=1,5, with 7.6 Hz, 1H), 7,32 (dt, J=0,9 and 7.6 Hz, 1H), 7,10 (d, J=8.6 Hz, 2H), 6,95-7,07 (m, 3H), 6,85-6,92 (m, 3H with a 2H doublet (J=8.6 Hz) when 6,87), 6,72 (DD, J=1,4, 8.0 Hz, 1H), 5,63 (d, J= and 17.9 Hz, 1H), 5,54 (d, J=and 17.9 Hz, 1H), equal to 4.97 (DD, J=3,9, and 9.4 Hz, 1H), to 4.52 (Shir. s, 1H), to 4.41 (q, J=7,1 Hz, 2H), 4,20-to 4.28 (m, 2H), 3,32-3,36 (Shir. m, 2H), 2,74 (t, J=6,8 Hz, 2H), 2,56-2,69 (m, 1H), 2,36 (DDT, J=14,4, 9,3, 4.8 Hz, 1H), USD 1.43 (t, J= 7,1 Hz, 3H), of 1.42 (s, N).13With NMR (DClC) 166,9, 166,4, 157,4, 155,9, 144,2, 137,7, 132,8 (CH), 131, 5MM (CH), 131,3, 129,8 (CH), 129,0, 128,5, 127,1 (CH), 125,6 B>), 35,3 (CH2), 30,4 (CH2), 28,4 (CH3), 14.4V (CH3). The connection 108 2-{ 2-[4-(2-Aminoethyl) phenoxy] ethyl} -4-(2-carbomethoxyamino) -3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from compound 107 way To using triperoxonane acid present anisole instead of IPA/HCl and isolated in the form of a white powder with a yield of 94.5%, so pl. of 107.5-109o;1H NMR (DMSO-d6) to 7.99 (DD, J= 1,5, 6.2 Hz, 1H), 7,75 (Shir.s, 3H), 7,39-7,53 (m, 2H), 7,18 (d, J=8.6 Hz, 2H), 7,02-7,10 (m, 3H), 6,92-of 6.99 (m, 3H with a 2H doublet at 6,94), for 6.81 (d, J= 8.0 Hz, 1H), 5,51 (d, J=17.5 Hz, 1H), 5,39 (d, J=17.5 Hz, 1H), 5,04 (DD, J= 4,1, to 8.7 Hz, 1H), 4,36 (kV, J=7,1 Hz, 2H), 4,18-to 4.23 (m, 2H), 2,90-to 3.02 (m, 2H), 2,75-of 2.81 (m, 2H), 2,28 at 2.45 (m, 2H), of 1.37 (t, J=7,1 Hz, 3H). IR 2975-3100 (W), 1690 (sh), 1680 cm-1. MS 475 (MH+). Analysis: Calculated for C28H30N2O51.0 C2HF3O21,5 H2O: 58,53, H 5,57, N 4,55. Found: 58,48, H 5,44, N 4,55. Connection 109 4-{ 2-[2-(4-(2-(tert - Butoxycarbonylamino)ethyl)phenoxy)] -ethyl]-3,4-dihydro-3 - oxo-2H-1,4-benzoxazin-4-yl}methylbenzoic acid < / BR> Method A: Compound 103 (150 mg, 1 EQ) and 1 N. NaOH (2.5 EQ) in methanol (10 ml) was heated on an oil bath at 50oWith over 26 hours After evaporation of methanol, the residue was diluted with water (20 ml), cooled to 0oWith the CSO solids with a yield of 89%, so pl. = 147-148o; 1H NMR (DMSO-d6) of 8.04 (d, J=8.1 Hz, 2H), 7,34 (d, J=8,3 Hz, 2H), 7,10 (d, J=8,3 Hz, 2H), 6.75 in? 7.04 baby mortality (m, 6N), 5,22 (Shir.s, 2H), 4,96 (DD, J= 3,8, 9.0 Hz, 1H), 4,55 (Shir.s, 1H), 4,10-to 4.28 (m, 2H), 3,31-to 3.36 (m, 2H), by 2.73 (t, J=6.3 Hz, 2H), 2,55-2,61 (m, 1 H), 2,34 (DDT, J=14,1, 9,8, 5,1 Hz, 1H), USD 1.43 (s, N). IR 3300-3350 (W), 1688 (lat.) cm-1. MS (FAB) 547 (MN+), 447 (M-BOC)+310 (base). Analysis: Calculated for C31H34N2O7: 68,12, H 6,27, N 5,12. Found: 67,71, H 6,47, N 5,00. The connection 110 4-{ 3,4-Dihydro-2-[2-(4- (2-aminoethyl)phenoxy)] ethyl-3-oxo-2H-1,4 - benzoxazin-4-yl} methylbenzoic acid < / BR> Obtained from compound 109 way To using triperoxonane acid present anisole instead of IPA/HCl and isolated in the form of a white powder with a yield of 98%, so pl. 195-197o;1H NMR (DMSO-d6) 12,97 (Shir.s, 1H), of 7.90 (d, J=8,2 Hz, 2H), to 7.77 (Shir.s, 3H), 7,38 (d, J=8,2 Hz, 2H), 7,19 (d, J= 8,3 Hz, 2H), 6,97-7,05 (m, 4H), to 6.95 (d, J=8,3 Hz, 2H), 5,28 (d, J= 16,3 Hz, 1H), 5,20 (d, J=16,3 Hz, 1H), 5,00 (DD, J=4.0 a, 8,7 Hz, 1H), 4,18-4,22 (m, 2H), 2,98-to 3.02 (m, 2H), 2,78 (t, J=7.8 Hz, 2H), 2,35-to 2.40 (m, 1H), 2,23-of 2.28 (m, 1H). 13WITH NMR 166,9, 165,8, 157,2, 143,6, 141,6, 129,8 (CH), 129,7 (SN), WHICH IS 129.3, 128,3, 126,6 (CH), 123,9 (CH), 122,8 (CH), 117,0 (SN), BY 115.7 (CH), TO 114.7 (CH), 73,0 (CH), 63,1 (CH2), 43,7 (CH2), AND 39.9 (CH2), TO 31.9 (CH2), 29,4 (CH2). IR 3000-3200 (W), 1681, 1503 cm-1. MS 447 (MN+), 40,5 H2O: 59,05, H 4,96, N 4,92. Found: 58,96 H 4,71, N 4,76. Connection 111 3-{ 3,4-Dihydro-2-[2-(4-(2-(tert - butoxycarbonylamino)-ethyl) phenoxy)] ethyl-3-oxo - 2H-1,4-benzoxazin-4 - yl}methylbenzoic acid < / BR> Obtained from compound 105 by way Of and allocated in the form of a white glassy product with a yield of 92%, so pl. 76-78o;1H NMR (DMSO-d6) 7,87 (Shir. s, 1H), 7,82 (d, J=7,3 Hz, 1H), 7,51 (d, J=8,8 Hz, 1H), 7,47 (kV, J= 7,4 Hz, 1H), 7,10 (d, J=8.5 Hz, 2H), 6,97-7,07 (m, 4H), 6.87 in (d, J=8.5 Hz, 2H), 6,85 (Shir.s, 1H), 5,24 (s, 2H), to 4.98 (DD, J=4,1, 8,8 Hz, 1H), 4,15-4,19 (m, 2H), 3,06-3,10 (Shir.kV, J=7,6 Hz, 2H), 2,61 (t, J=7,6 Hz, 2H), 2,32-is 2.37 (m, 1H), 2,20-of 2.25 (m, 1H), 1,36 (s, N). IR 2800-3100 (W), 1704, 1700 (sh) cm-1. MS 547 (MN+), 473 (base). Analysis: Calculated for C31H34N2ABOUT70.5 N2O: 67,01, H 6,35, N 5,04. Found: 67,03, H 6,44, N 4,95. The connection 112 3-{ 3,4-Dihydro-2-[2-(4-(2 -aminoethyl)phenoxy)]ethyl-3-oxo-2H-1,4-benzoxazin-4-yl}methylbenzoic acid < / BR> Obtained from compound 111 way To using triperoxonane acid present anisole instead of IPA/HCl and isolated in the form of white crystals with a yield of 92%, so pl. 193-195o;1H NMR (DMSO-d6) 13,03 (Shir.s, 1H), 7,87 (Shir.s, 1H), 7,83 (d, J=7,4 Hz, 1H), to 7.77 (Shir.s, 3H), 7,51 (d, J= 7.9 Hz, 1H), 7,47 (kV, J=7.5 Hz, 1H), 7,18 (d, J=8.5 Hz, 2H), (m, 1H), 2.21 are of 2.34 (m, 1H). IR 2800-3200 (W), 1677, 1636 cm-1. MS 447 (MN+), 429, 194 (base). Analysis: Calculated for C26H26N2O5C2HF3O20.5 H2O: 59,05, H 4,96, N 4,92. Found: 58,74 H 4,87, N 4,69. Connection 113 2-{ 2-[2-(4-(2-(tert - Butoxycarbonylamino)ethyl) phenoxy)]-ethyl-3,4-dihydro-3-oxo-2H-1,4-benzoxazin-4-yl}methylbenzoic acid < / BR> Obtained from compound 107 by way Of and allocated in the form of a white powder with a yield of 93.5%, so pl. 156-159o;1H NMR (CDCl3/ DMSO-d6) 8,13 (d, J=7,4 Hz, 1H), 7,32-7,40 (m, 3H with 1H exchange), 7,11 (d, J=8.0 Hz, 2H), 6,97-7,05 (m, 3H), 6,86 (d, J= 8.0 Hz, 2H), 6,72-6,85 (m, 2H), 5,61 (d, J=18,1 Hz, 1H), of 5.53 (d, J= 18,1 Hz, 1H), 4,91 (DD, J=3,7, 9,3 Hz, 1H) and 4.65 (Shir.s, 1H), 4,14-4,22 (m, 2H), 3,23 of 3.28 (Shir. m, 2H), 2,68 (t, J=7,0 Hz, 2H), 2,47 is 2.51 (m, 1H), 2,25 is 2.33 (m, 1H), 1,38 (s, N). IR 3350-3500 (W), 2950, 1687, 1512 cm-1. MS (FAB) 547 (MN+), 447 (base), 310. Analysis: Calculated for C31H34N2O70.5 H2O: 67,01, H 6,35, N 5,04. Found: 67,24 H 6,56, N 5,02. The connection 114 2-{ 2-[2-(4-(2-Aminoethyl) phenoxy)]ethyl-3,4-dihydro-3-oxo-2H-1,4-benzoxazin-4-yl}methylbenzoic acid < / BR> Obtained from compound 113 way To using triperoxonane acid present anisole instead of IPA/HCl and highlighted the Russian Assembly, 3H), 7,47 (t, J=6,5 Hz, 1H), 7,39 (t, J=7.7 Hz, 1H), 7,18 (d, J=8.5 Hz, 2H), 6,91-to 7.09 (m, 6N with a 2H doublet (J=8,5 Hz) when 6,95), 6,79 (d, J=7,3 Hz, 1H), of 5.53 (d, J=18,4 Hz, 1H), 5,42 (d, J=18,4 Hz, 1H), 5,04 (DD, J=4,0, 8.5 Hz, 1H), 4,18-4,24 (m, 2H), 2.95 and-to 3.09 (m, 2H), 2,75-of 2.81 (m, 2H), 2,23-to 2.42 (m, 2H). IR 2950-3200 (W), 1683, 1514 cm-1. MS 447 (MN+), 138 (base). Analysis: Calculated for C26H26N2O51.02HFCABOUT20,25 H2ABOUT: 59,52, H 4,91, N 4,96. Found: 59,43 H 4,91, N 4,80. Connection 115 2-{ 2-[4-[2-(N,N'-Bis-tert - butoxycarbonylamino)-ethyl]phenoxy]ethyl} -4-(4-carbomethoxyamino)-3,4 - dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained by method L using intermediate product 11758-71-2 (reference example 81) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine and selected after chromatography (elution with a mixture of ethyl acetate/hexane) as a white glassy product, so pl. 68-71o;1H NMR (DCl3) of 11.45 (Shir.s, 1H), of 8.37 (Shir.s, 1H), to 7.99 (d, J=8,4 Hz, 2H), 7,30 (d, J=8,4 Hz, 2H), 7,13 (d, J=8.6 Hz, 2H), 6,74-7,01 (m, 6N with a 2H doublet (J= 8.6 Hz) when 6,85), 5,23 (d, J=16.1 Hz, 1H), 5,16 (d, J=16.1 Hz, 1H), 4.95 points (DD, J=3,8, 9.5 Hz, 1H), 4,19-to 4.28 (m, 2H), 3,90 (s, 3H), 3,61-the 3.65 (m, 2H), of 2.81 (t, J=7.2 Hz, 2H), by 2.55 2.63 in (m, 1H), 2,31-of 2.38 (m, 1H), 1,50 (s, N), to 1.48 (s, N). IR 2950-3300 (Shir. ), 1724, 1688, 1639 cm-1. MS (FAB) 703 (MN+), 503 (base). EN"> The connection 116 4-(4-Carboxybenzoyl)-2-{ 2-[4- [2-(guanidino)ethyl]phenoxy]-ethyl}-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from compound 116 way To using triperoxonane acid present anisole instead of IPA/HCl and isolated in the form of not quite white solid product with a yield of 67%, so pl. 197-199o;1H NMR (DMSO-d6) to $ 7.91 (d, J=8,3 Hz, 2H), 7,76 (Shir.s, 1H), 7,51 (Shir.t, J=5 Hz, 1H), 7,40 (d, J= 8,3 Hz, 2H), 7,19 (d, J=8.5 Hz, 2H), 6,92-to 7.09 (m, N), from 5.29 (d, J=17,0 Hz, 1H), 5,23 (d, J=17,0 Hz, 1H), free 5.01 (DD, J=4,1, 8.6 Hz, 1H), 4,18-to 4.23 (m, 2H), 3,30-3,39 (m, 2H), 3,01 (Shir.s, 1H), 2,62-of 2.81 (m, 2H), 2,35 is 2.43 (m, 1H), 2,20-2,31 (m, 1H). IR 3000-3400 (W), 1676, 1501 cm-1. MS (FAB) 489 (MN+). Analysis: Calculated for C27H28N4O Methyl-4-{ 2-[4-(3-Chlorobenzyl) -3,4-dihydro-3-oxo-2H - 1,4-benzoxazin-2-yl] ethoxy}phenyl acetate < / BR> Obtained by method L, which was modified by combining the intermediate product 10488-22 (reference example 66) with methyl-4-hydroxyphenylacetate boiling under reflux overnight and isolated in the form of a white solid product with a yield of 38%, so pl. 94-95o; 1H NMR (CDCl3) 7,13-7,25 (m, 5H), 7.03 is-7,11 (m, 1H), for 6.81-7,01 (m, 6N), to 5.17 (d, J=16.2 Hz, 1H), 5,08 (d, J=16.2 Hz, 1H), 4,94 (DD, J=3,9, and 9.4 Hz, 1H), 4,16-4,30 (m, 2H), to 3.67 (s, 3H), of 3.57 (s, 2H), 2,53-of 2.64 (m, 1H), of 2.33 (DDT, J=9,6, 14,5, 4.8 Hz, 1H). IR 1736, 1673, 1502 cm-1. MS 466 (MN+), 300 (base). Analysis: Calculated for C26H24ClNO5: 67,02, H 5,19, N 3,01. Found: Up 66,78, H 5,20, N 2,94. Connection 119 4-{2-[4-(3-Chlorobenzyl) -3,4-dihydro-3-oxo-2H - 1,4-benzoxazin-2-yl] ethoxy}phenylacetic acid < / BR> Obtained from compound 118 by way Of, but the product was acidified with concentrated Hcl. The acid obtained in the form of a white solid product with a yield of 95%, so pl. 144-145o;1H NMR (DMSO-d6) 7,19-of 7.24 (m, 5H), 7,11-7,13 (m, 1H), 6,88-7,01 (m, 5H), 6,83 (d, J=7,3 Hz, 1H), 5,16 (d, J=16,3 Hz, 1H), 5,07 (d, J= 16,3 Hz, 1H), is 4.93 (DD, J=5,4, and 9.4 Hz, 1H), 4,19-to 4.23 (m, 2H), 3,61 (s, 2H), of 2.51-of 2.58 (m, 1H), 2,31-of 2.34 (m, 1H). IR 3000-3200 (W), 1714, 1609 cm-1. MS 452 (MH CLASS="ptx2"> Connection 120 3-{ 4-{2-[4-(3-Chlorobenzyl) -3,4-dihydro-3-oxo-2H-1,4-benzoxazin-2-yl] ethoxy}phenyl}propionic acid < / BR> Obtained from compound 120 by way Of, but the product was acidified with concentrated Hcl, and extracted as a white solid with a yield of 90%, so pl. 141-143o;1H NMR (DMSO-d6) 7,30-7,41 (m, 3H), 7,20-of 7.23 (m, 1H), 7,16 (d, J=8.1 Hz, 2H), 3,93-7,10 (m, 4H), 6.87 in (d, J=8.1 Hz, 2H), 5,23 (d, J= 16.0 Hz, 1H), 5,15 (d, J=16.0 Hz, 1H), 5,00 (DD, J=4.2, and the 8.9 Hz, 1H), 4,10-is 4.21 (m, 2H), 2,68 is 2.75 (m, 3H), 2,30-2,52 (m,C26H24ClNO50.5 H2O: 65,75, H 5,31, N 2,95. Found: 65,97, H Of 5.05, N 2,89. The connection 122 Methyl-3-{ 2-[4-(3-Chlorobenzyl) -3,4-dihydro-3-oxo-2H-1,4-benzoxazin-2 - yl]ethoxy}phenyl acetate < / BR> Obtained by method L, which was modified by combining the intermediate product 10488-22 (reference example 66) with methyl-3-hydroxyphenylacetate boiling under reflux during the night, and allocated in the form of a white solid product with a yield of 48%, so pl. 80-82o; 1H NMR (CDCl3) 7,13-7,24 (m, 6N), for 6.81-7,01 (m, 6N), to 5.17 (d, J=16.2 Hz, 1H), 5,08 (d, J= 16.2 Hz, 1H), 4,94 (DD, J=3,8, and 9.3 Hz, 1H), 4,20-to 4.28 (m, 2H), 3,70 (s, 3H), of 3.60 (s, 2H), 2.57 m-2,61 (m, 1H), 2,29-is 2.37 (m, 1H). IR 1735, 1680, 1503 cm-1. MS 466 (MN+). Analysis: Calculated for C26H24ClNO5: 67,02, H 5,19, N 3,01. Found: 66,66, H 5,31, N 2,90. Connection 123 3-{ 2-[4-(3-Chlorobenzyl) -3,4-dihydro-3-oxo-2H-1,4-benzoxazin-2-yl] ethoxy} phenylacetic acid < / BR> Obtained from compound 122 by way Of, but the product was acidified with concentrated Hcl, and extracted as a pale pink amorphous solid product with a yield of 87%;1H NMR (DMSO-d6) 7,22-7,29 (m, 4H), 7,10-7,13 (m, 1H), 6,80-7,03 (m, 7H), to 5.17 (d, J=16,3 Hz, 1H), 5,07 (d, J=16,3 Hz, 1H), 4,94 (DD, J=3,9, and 9.3 Hz, 1H), 4,20-to 4.28 (m, 2H), 3,63 (s, 2H), 2,53 at 2.59 (m, 1H), 2,33 (DDT, H22ClNO50,6 H2O: 64,89, H OF 5.05, N 3,03. Found: 64,62, H 4,91, N 2,95. The connection 124 Methyl-4-{ 4-{2-[4-(3- Chlorobenzyl)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin-2-yl]ethoxy}phenyl}butyrate < / BR> Obtained by method L, which was modified by combining the intermediate product 10488-22 (reference example 66) with methyl 3-(4-hydroxyphenyl)butyrate by boiling under reflux during the night, and allocated in the form of a light amorphous solid product with a yield of 46%;1H NMR (CDCl3) 7,10-7,20 (m, 3H), 6,99-was 7.08 (m, 3H with a 2H doublet (J=8,5 Hz) when 7,03), 6,83-6,94 (m, 3H), 6.75 in-to 6.80 (m, 3H with a 2H doublet (J=8,5 Hz) when 6,78), 5,09 (d, J=16.4 Hz, 1H), 5,00 (d, J=16.4 Hz, 1H), 4,94 (DD, J=3,9, and 9.2 Hz, 1H), 4,10-of 4.25 (m, 2H), 3,60 (s, 3H), 2,41-2,52 (m, 3H), of 2.20 to 2.35 (m, 3H), 1,89 (quintet, J= 7.5 Hz, 2H). IR 1732, 1681, 1502 cm-1. MS 494 (MN+). Connection 125 4-{ 4-{2-[4-(3-Chlorobenzyl) -3,4-dihydro-3-oxo-2H - 1,4-benzoxazin-2-yl] ethoxy}phenyl}butyric acid < / BR> Obtained from compound 124 by way Of, but the product was acidified with concentrated Hcl, and extracted as a white solid with a yield of 83%, so pl. 129-130o;1H NMR (DMSO-d6) 6,99-7,25 (m, 7H with a 2H doublet (J=8,5 Hz) when 7,10), 6,91-of 6.96 (m, 3H), for 6.81-6.87 in (m, 3H, s, 2H, doublet, J=8.5 Hz) when 6,84), 5,16 (d, J=16,3 Hz, 1H), 5,08 (d, J=16,3 Hz, 1H), 4,94 (DD, J=3,8, and 9.4 Hz, 1H), 4,18-4.26 deaths (m, 2H), Analysis: Calculated for C27H26ClNO5: 67,57, H 5,46, N 2,92. Found: 67,19, H 5,39, N 2,78. Connection 126 Methyl-3-[3-[2-{ 4-(3- Chlorobenzyl)-3,4-dihydro-3 - oxo-2H-1,4-benzoxazin-2-yl}ethoxy]phenyl]propionate < / BR> Obtained by method L, which was modified by combining the intermediate product 10488-22 (reference example 66) with methyl-3-(3-hydroxyphenyl)propionate boiling under reflux overnight, and extracted as a white solid in 51% yield, so pl. 92-94o;1H NMR (CDCl3) 6,91-7,24 (m, 8H), 6,76-6,83 (m, 4H), 5,18 (d, J=16.1 Hz, 1H), 5,08 (d, J= 16.1 Hz, 1H), 4,94 (DD, J=3,9, and 9.4 Hz, 1H), 4,21-to 4.28 (m, 2H), 3,68 (s, 3H), of 2.93 (t, J=7.8 Hz, 2H), 2.63 in (t, J=7.8 Hz, 2H), 2,53 at 2.59 (m, 1H), 2,33 (DDT, J=9,4, 14,2, a 4.7 Hz, 1H). IR 1724, 1677, 1503 cm-1. MS 480 (MN+). Analysis: Calculated for C27H26ClNO5: 67,57, H 5,46, N 2,92. Found: 67,38, H 5,51, N 2,71. Connection 127 3-[3-[2-{ 4-(3-Chlorobenzyl) -3,4-dihydro-3-oxo-2H - 1,4-benzoxazin-2-yl} ethoxy] phenyl]propionic acid < / BR> Obtained from compound 126 way, but the product was acidified with concentrated Hcl, and extracted as a white solid with a yield of 93%, so pl. 118-119o;1H NMR (DMSO-db) 7,18-7,24 (m, 4H), 7,10 for 7.12 (m, 1H), 6.90 to? 7.04 baby mortality (m, 3H), 6,77-6,83 (m, 4H), 5,16 (d, J=16.0 Hz, 1H), 1H). IR 3000-3200 (W), 1691, 1679, 1501 cm-1. MS 466 (MN+). Analysis: Calculated for C26H24ClNO5: 67,02, H 5,19, N 3,01. Found: 66,63, H 5,17, N 2,87. Connection 128 Methyl-2-{ 2-[4-(3-Chlorobenzyl) -3,4-dihydro-3-oxo-2H - 1,4-benzoxazin-2-yl] ethoxy}phenyl acetate < / BR> Obtained by method L, which was modified by combining the intermediate product 10488-22 (reference example 66) with methyl-2-hydroxyphenylacetate boiling under reflux overnight, and extracted as a yellow oil.1H NMR (CDCl3) 7,09-7,39 (m, 6N), for 6.81? 7.04 baby mortality (m, 6N), is 5.18 (d, J= 16,3 Hz, 1H), 5,07 (d, J=16,3 Hz, 1H), 4.92 in (DD, J=3,8, 9.6 Hz, 1H), 4,21-4,32 (m, 2H), 3,60 (s, 2H), 2,54-2,62 (m, 2H), 2,33 (DDT, J=14,4, 9,6, a 4.9 Hz, 1H). Connection 129 2-{ 2-[4-(3-Chlorobenzyl)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin-2-yl] ethoxy}phenylacetic acid < / BR> Obtained from compound 128 way, but the product was acidified with concentrated Hcl, and extracted as a white solid with a yield of 89%, so pl. 140-142o; 1H NMR (DMSO-d6) 7,07-7,25 (m, 6N), 6,84-7,00 (m, 6N), to 5.13 (s, 2H), free 5.01 (DD, J=4.0 a, and 9.2 Hz, 1H), 4,20-4,34 (m, 2H), 3,68 (d, J= 16.0 Hz, 1H) and 3.59 (d, J=16.0 Hz, 1H), 2.40 a at 2.59 (m, 1H), 2,28-of 2.38 (m, 1H). IR 3000-3200 (W), 1722, 1677, 1498 cm-1. MS 452 (MN+), 300 (base). Analysis: Calculated for C25HNil) -3,4-dihydro-3-oxo-2H - 1,4-benzoxazin-2 - yl] ethoxy}benzaldehyde < / BR> Obtained by method L, which was modified by combining the intermediate product 10488-22 (reference example 66) with a 4-hydroxybenzaldehyde boiling under reflux overnight. The product was isolated as a white solid after chromatography with 30% yield, so pl. 130-131o;1H NMR (CDCl3) of 9.89 (s, 1H), a 7.85 (d, J=8,8 Hz, 2H), 7.23 percent-7,30 (m, 3H), 7,10-to 7.15 (m, 1H), 6,92-7,05 (m, 5H), 6,83 (DD, J=1,4, and 8.7 Hz, 1H), 5,20 (d, J=16.2 Hz, 1H), 5,07 (d, J=16.2 Hz, 1H), is 4.93 (DD, J=4,1, 9.1 Hz, 1H), 4,25 was 4.42 (m, 2H), 2,58-2,70 (m, 1H), 2.40 a (DDT, J=10,0, 14,2, 5.0 Hz, 1H). IR 1700, 1674, 1598 cm-1. MS 422 (MN+). Analysis: Calculated for C24H20ClNO4: 68,33, H 4,78, N 3,32. Found: 68,01, H 4,82, N 3,27. Connection 131 Methyl-2-[4-{ 2-[4-(3- Chlorobenzyl)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin-2-yl]ethoxy)phenyl]glycolate < / BR> Bromoform (0,31 ml, 3.54 mmol) was added dropwise under nitrogen atmosphere to the connection 130 (1,15 g, 2,73 mmol), lithium chloride (0,231 g, the 5.45 mmol), potassium hydroxide (0,611 g, 10.9 mmol) and water (4 ml) in dioxane (4 ml). After heating in an oil bath at 40oWith over night the reaction mixture was acidified to pH 1 using Hcl (1 BC) and was extracted with ethyl acetate (CH ml). The combined organic layers were washed with water (2 x 50 ml), dried (gSO4), filtrair acetylchloride (0.4 ml) in methanol (10 ml) and the reaction mixture was stirred at room temperature under nitrogen atmosphere overnight. The methanol is evaporated and the residue was dissolved in ether (200 ml). The solution was washed with saturated Panso3(2 x 50 ml), dried (MgSO4), filtered and evaporated. -Hydroxyether was obtained after chromatography on silica gel (elution with a mixture of ethyl acetate/CH2Cl2) with a total yield of 52%.1H NMR (DCl3) to 7.32 (d, J=8.7 Hz, 2H), 7.23 percent-7,26 (m, 3H), 7,10-to 7.15 (m, 1H), 6,93-7,03 (m, 3H), 6,91 (d, J=8.7 Hz, 2H), for 6.81-6.89 in (m, 1H), 5,18 (d, J=16.2 Hz, 1H), 5,13 (d, J=5.6 Hz, 1H), 5,07 (d, J=16.2 Hz, 1H), is 4.93 (DD, J=3,9, and 9.4 Hz, 1H), 4,17-4,32 (m, 2H), 3,76 (s, 3H), 3,40 (d, J= 5.6 Hz, 1H, exchangeable), 2,53-of 2.64 (m, 1H), 2,33 (DDT, J=14,4, 9,4, 4.8 Hz, 1H). Connection 132 2-[4-{ 2-[4-(3-Chlorobenzyl) -3,4-dihydro-3-oxo-2H - 1,4-benzoxazin-2-yl] ethoxy} phenyl]glycolic acid < / BR> Obtained from compound 131 way, but the product was acidified with concentrated Hcl, and extracted as a pale yellow solid with a yield of 85%, so pl. 54-56o;1H NMR (DMSO-d6) of 7.36 (d, J=8.6 Hz, 2H), 7.23 percent-7,26 (m, 4H), 7,09 for 7.12 (m, 1H), for 6.81-7,01 (m, 5H), 5,20 (s, 1H), 5,16 (d, J= 16.6 Hz, 1H), 5,07 (d, J=16.6 Hz, 1H), is 4.93 (DD, J=4.0 a, and 9.2 Hz, 1H), 4,20-4,27 (m, 2H), 3,20 (Shir.s, 1H, exchangeable), 2,53-2,62 (m, 1H), 2,30-of 2.38 (m, 1H). IR 3300-3400 (Shir. ), 2800-3150 (W), 2800-3150 (W), 1731, 1671, 1512 cm-1. MS (FAB) 468 (MN+), 300 (base). Analysis: Calculated for C25H22ClNO60.5 H2O: 62,96, H A 4.86, N 2,94. On oxazin-2-yl]ethoxy}phenyl]acetate < / BR> Thionyl chloride (0,091 ml of 1.24 mmol), then pyridine (0,093 ml, 1.15 mmol) was added to compound 130 (0,460 g, 0.95 mmol) in benzene (10 ml) under nitrogen atmosphere at room temperature. After stirring overnight, the solvent evaporated and the residue was poured into water (50 ml). This mixture was extracted with ethyl acetate (2 x 50 ml). The combined organic layers were washed with water (3 x 50 ml), dried (gSO4), filtered and evaporated, obtaining the corresponding chloride in the form of a transparent gel with a yield of 82%;1H NMR (DMSO-d6) 7,42 (d, J=8.7 Hz, 2H), 7.23 percent-7,29 (m, 3H), 7,11-to 7.15 (m, 1H), 6,99-7,03 (m, 2H), 6.90 to-6,97 (m, 3H with a 2H doublet (J=8,7 Hz) when 6,92), PC 6.82 (d, J= 7,4 Hz, 1H), of 5.34 (s, 1H), 5,18 (d, J=16.2 Hz, 1H), 5,08 (d, J=16.2 Hz, 1H), is 4.93 (DD, J= 4.0 a, and 9.4 Hz, 1H), 4,19-to 4.33 (m, 2H), of 3.78 (s, 3H), 2,54-to 2.65 (m, 1H), 2,34 (DDT, J=14,3, 9,4, 4.8 Hz, 1H). Connection 134 5-[4-{ 2-[4-(3-Chlorobenzyl) -3,4-dihydro-3-oxo-2H-1,4-benzoxazin-2-yl] ethoxy}phenyl]thiazolidin-2,4-dione < / BR> The thiourea (56 mg, of 0.74 mmol) was added to the compound 133 (0,185 g and 0.37 mmol) in 2-methoxyethanol (3 ml). The reaction mixture was heated on an oil bath at 110oC for 3 hours, After cooling, was added Hcl (1 N., 2.5 ml) and the reaction mixture was heated at 100oWith during the night. The cooled reaction mixture was diluted with water (50 ml) and was extracted with ethyl is the best thiazolidinedione in the form of a pale yellow foam with a yield of 64%, so pl. 70-72o;1H NMR (DMSO-d6) 8,05 (Shir.s, 1H), 7,35 (d, J= 8.7 Hz, 2H), 7.23 percent-of 7.25 (m, 3H), 7,11-to 7.15 (m, 1H), for 6.81-7,02 (m, 5H with a 2H doublet (J= 8,7 Hz) when of 6.96), 6,83 (d, J=8.6 Hz, 1H), are 5.36 (s, 1H), 5,19 (d, J= 16.2 Hz, 1H), 5,07 (d, J=16.2 Hz, 1H), 4,94 (DD, J=4,0, 9.1 Hz, 1H), 4,22-4,30 (m, 2H), 2,54-2,62 (m, 1H), 2,32-to 2.40 (m, 1H). IR 1756, 1698, 1500 cm-1. MS 509 (MH+). Connection 135 3,4-Dihydro-2-{ 2-[4-(2- guanidinate)phenoxy] ethyl}-6-methylsulfonylamino-4-(3 - Chlorobenzyl)-3-oxo-2H-1,4-benzoxazin < / BR> Method P: Compound 92 was heated by boiling under reflux with methanesulfonanilide (1 EQ) and DMAP (1.1 EQ) in CH2Cl2(10 ml) for 10 hours. The resulting mixture was diluted with water and indicated in the title compound was isolated by filtration, so square (decomposition) >121oC; IR (KBR) 3240, 1667, 1613, 1512, 1475, 1349, 1245, 1178, 865 cm-1;1H NMR (DMSO-d6) 9,63 (Shir.s, 1H), 8,07 (Shir.s, 1H), 7,43 (Shir.s, 2H), 7,35 (m, 4H), 7,20 (m, 3H), 7,01 (d, 1H, J=8.6 Hz), 6.89 in (m, 2H), PC 6.82 (DD, 2H, J=2,2, 8.5 Hz), 5,16 (d, 1H, J=16.5 Hz), to 5.03 (d, 1H, J=16.5 Hz), equal to 4.97 (DD, 1H, J=4.2, and an 8.8 Hz), 4,16 (m, 2H), of 3.25 (m, 2H), and 2.79 (s, 3H), 2,70 (t, 2H, J=7,2 Hz), 2,35 (m, 1H), 2,22 (m, 1H). Analysis: Calculated for C27H30lN5O5S 1,7 HCl: 51,15, H 5,04, N 11,05. Found: 51,47, H 5,14, N 10,78. Connection 136 2-{ 2-[4-(2-(N,N-Bis-tert - butoxycarbonylamino) ethyl)-phenoxy]ethyl} -3 in the form of a reddish-brown solid product (Razlog.) >79oC; MS (FAB) MH+738; IR (KBR) 3325, 2977, 1723, 1687, 1612, 1501, 1410, 1330, 1245, 1151, 1057, 971, 688 cm-1;1H NMR (DCl3) 11,47 (Shir.s, 1H), of 8.37 (Shir.t, 1H), 7,31 (m, 1H), 7,11 (m, 4H), 7,05-6,89 (m, 3H), 6,83 (m, 3H), 6,45 (Shir.s, 1H), 5,14 (d, 2H, J=7,2 Hz), 4,94 (DD, 1H, J=4.0 a, and 9.3 Hz), 4,20 (m, 2H), 3,62 (m, 2H), equal to 2.94 (s, 3H), of 2.81 (t, 2H, J= 7,2 Hz), to 2.55 (m, 1H), 2,34 (m, 1H), 1,60 (Shir.s, 1H), 1,50 (s, N), to 1.48 (s, N). Analysis: Calculated for C37H47N5ABOUT9S 0,9 N2O: 58,93, H OF 6.52, N 9,29. Found: 59,19, H To 6.58, N 9,00. Connection 137 2-{ 2-[4-(2-Guanidinate)phenoxy] ethyl}-3,4-dihydro-4-(3 - methylsulfonylbenzoyl)-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from compound 136 way To exit 94%, so square (decomposition) >95oC; MS (FAB) MH+538; IR (KBr) 3156, 1664, 1500, 1468, 1402, 1327, 1243, 1147, 1052, 978, 751, 690, 514 cm-1;1H NMR (DMSO-d6) 9,82 (Shir.s, 1H), to 7.64 (Shir. t, 1H), 7,55-6,85 (Shir.s, 3H), 7,28 (t, 1H, J=7.8 Hz), 7,20 (d, 2H, J=8.5 Hz), to 7.09 (s, 1H), 7,05 (m, 2H), 6,99 (m, 4H), 6,92 (d, 2H, J=8.5 Hz), 5,19 (d, 1H, J=16.6 Hz), 5,09 (d, 1H, J=16.6 Hz), 4,94 (DD, 1H, J=4,11, 9.0 Hz), 4,19 (m, 2H), 3.33 and (m, 2H), 2,93 (s, 3H), of 2.72 (t, 2H, J=7.4 Hz), 2,32 (m, 1H), 2,22 (m, 1H). Analysis: Calculated for C27H31N5O5S: 55,32, H 5,93, N 11,32. Found: 55,34, H 5,86, N 11,34. Connection 138 2-{ 2-[4-[2-(N,N-Bis-tert - butoxycarbonylamino)ethyl] -phenoxy]ethyl} -3,4-dihydro-3-oxo-4-pentyl-2H-1,4-benzoato and was highlighted with the release of 42% in the form of a white foam after chromatography on SiO2(hexane/CH2Cl2, 1/3); IR (KBR) 3334, 2977, 2932, 2872, 1685, 1639, 1615, 1501, 1409, 1366, 1331, 1131, 1058, 748 cm-1;1H NMR (CDCl3) of 0.91 (t, J=6.8 Hz, 3H), 1.32 to of 1.40 (m, 4H), to 1.48 (s, N) and 1.51 (s, N), 1,61-1,72 (m, 2H), 2,17-of 2.30 (m, 1H), 2,43 is 2.55 (m, 1H), 2,81 (t, J=7.2 Hz, 2H), 3,63 (kV, J=7,1 Hz, 2H), 3,92 (t, J=6,8 Hz, 2H), 4,13-of 4.25 (m, 2H), 4,79 (DD, J= 9,20, 4.0 Hz, 1H), at 6.84 (d, J=8.5 Hz, 2H), of 6.96-7,07 (m, 4H), 7,12 (d, J=8.6 Hz, 2H), of 8.37 (Shir.t, J=4.3 Hz, 1H), 11,48 (Shir.s, 1H). Analysis: Calculated for C34H48N4O7: 65,36, H 7,74, N 8,97. Found: 65,23, H Of 7.70, N 8,98. Connection 139 3,4-Dihydro-2-{ 2-[4-(2- guanidinate)phenoxy] ethyl} -4-(4-nitrobenzyl)-3 - oxo-2H-1,4-benzoxazin < / BR> Obtained from compound 93 way in the form of a solid product with a yield of 68%, so pl.: Razlog. when >101oC; MS (FAB) MH+at 525; IR (KBR) 3433, 1671, 1600, 1525, 1501, 1468, 1398, 1344, 1253, 1065, 894, 810 cm-1;1H NMR (DMSO-d6/TMS) to 8.20 (d, 2H, J=8,2 Hz), 7,54 (d, 2H, J=8.5 Hz), 7,45-6,60 (PTS.Shir.s, 4H), 7,38 (s, 1H), 7,29 (s, 1H), 7,18 (m, 2H), 7,05 (m, 2H), 6,97 (m, 3H), are 5.36 (d, 1H, J=18,0 Hz), with 5.22 (1H, J=18,0 Hz), 4,99 (m, 1H), 4.26 deaths (m, 2H), 3,35 (m, 2H), 2,68 (t, 2H, J=6.3 Hz), 2.40 a (m, 1H), 2,28 (m, 1H). The connection 140 2-{ 2-[4-[2-(N,N-Bis-tert - butoxycarbonylamino)-ethyl] phenoxy]ethyl} -3,4-dihydro-4-(4-methoxybenzyl)-3-oxo-2H-1,4-benzoxazin < / BR> Obtained by method L using intermediate product one obtained as a white foam. Analysis: Calculated for C27H46N4O8: 65,86, H 6,87, N OF 8.3. Found: 65,51, H 7,02, N 8,27. Connection 141 3,4-Dihydro-4-(2,4 - dichlorobenzyl)-2-{ 2-[4-(2- guanidinate)-phenoxy] ethyl}-3-oxo-2H-1,4-benzoxazin < / BR> Obtained by method L using intermediate product 10005-181-1 (reference example 48) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)gilgandra and way To and allocated in the form of a solid product. Analysis: Calculated for C26H426CL2N4O3HCl 0,75 H2O: 55,43, H 5,10, N 9,94. Found: 55,43, H Of 5.05, N 9,75. Connection 142 2-[2-[4-(3-Aminopropyl) phenoxy]ethyl]4-(4 - chlorbenzyl)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from intermediate 10353-28-1 (reference example 41) and 4-[3-(N-tert-butoxycarbonylamino) propyl]phenol ways J and K. Mentioned in the title compound was obtained as a yellow solid product (yield 11%), so pl. = 95-97oC; MS (FAB) MN+451; IR (KBr) 1250, 1400, 1500, 1590, 1680, 2040, 2950, 3400 cm-1;1H (NMR) 7,40 (d, J=of 8.47 Hz, 2H), 7,30 (d, J= 8,48 Hz, 2H), 2,62 (t, J=rate of 7.54 Hz, 2H), was 2.76 (t, J=7,52 Hz, 2H), 7.23 percent (t, J= 8,12 Hz, 1H), for 6.81 (d, J=7,37 Hz, 3H), to $ 7.91 (Shir.s, 2H), 6,99-was 7.08 (m, 4H), 4,19-4,20 (m, 2H), 2,33-2,49 (m, 1H), 2,19-of 2.30 (m, 1H), 1,82-to 1.87 (m, 2H), by 5.18 (DD, J=16,48 and 23,23 Hz, 2H), to 4.98 (DD, J=4,15 and 8.75 Hz, 1H). Connection 143 2-{ 2-[4-(2-(N,N-Bis-tert - butoxycarbonylamino) ethyl)-phenoxy]ethyl} -3,4-dihydro-7-nitro-4-(2 - nitrobenzyl)-3-oxo - 2H-1,4-benzoxazin < / BR> Obtained by method L using intermediate product 11653-142 (reference example 69) and N, N'-di-tert-butoxycarbonyl-2-(4-hydroxyphenyl)ethylguanidine and in the manner Specified in K. the title compound is obtained in the form of a white solid product with a yield of 13%, so pl.: decomposition at >128oC; MS (FAB) MH+735; IR (KBr) 3323, 3087, 2977, 1723, 1690, 1641, 1613, 1530, 1513, 1476, 1418, 1395, 1240, 1154, 941 cm-1;1H NMR (CDCl3/TMS) 11,43 (s, 1H), of 8.37 (Shir.t, 1H), 8,24 (DD, 1H, J=2.1 a, 7,4 Hz), 7,94 (d, 1H, J=2.5 Hz), to 7.84 (DD, 1H, J=2,5, and 8.9 Hz), 7,52 (m, 2H), 7,14 (d, 2H, J=8.6 Hz), was 7.08 (d, 1H, J=9.1 Hz), at 6.84 (d, 2H, J=8.6 Hz), 6,77 (d, 1H, J=8,9 Hz), of 5.68 (d, 1H, J= 18,1 Hz) to 5.56 (d, 1H, J=18,1 Hz), 5,10 (DD, 1H, J=4,0, a 8.9 Hz), to 4.23 (m, 2H), to 3.64 (m, 2H), 2,82 (t, 2H, J=7,3 Hz), 2.63 in (m, 1H), 2.40 a (m, 1H), 1,50 (s, N), to 1.48 (s, N). Connection 144 2-[2-[4-[2-(tert - Butoxycarbonylamino)ethyl) phenoxy]ethyl}-4-(3 - Chlorobenzyl)-3,4-dihydro-3 - oxo-2H-1,4-benzoxazin < / BR> Methanesulfonanilide (0.8 ml, 1.5 EQ) was added in one portion to a solution of intermediate product 10353-191-1 (2.0 g, 1 EQ, reference example 40), DMAP (0.33 g, 0.4 EQ) and triethylamine (1.2 ml, 1.5 EQ) in 30 ml of CH2Cl2. This mixture was stirred or (MgSO4) and concentrated in vacuum, obtaining mesilate. This mesilate was treated with 4-[2-(N-tert-butoxycarbonylamino) -ethyl] - phenol according to the procedures of method L, getting mentioned in the title compound in the form of a solid product, so pl. 91-92oC. Connection 145 2-[2-[4-(2-Guanidinate) phenoxy]ethyl]-4-(2 - Chlorobenzyl)-6-methyl-3,4-dihydro-2H-1,4-benzoxazin < / BR> Obtained by method L using intermediate product 10353-76 (reference example 89) and N, N'-di-tert-butoxycarbonyl - 2-(4-hydroxyphenyl)ethylguanidine and the way To with the following modifications. Bis-BOC-protected product combinations Mitsunobu were isolated by dissolution of the residue which is the crude product, in aqueous methanol and the processing solution are added dropwise 2 N. NaOH to achieve the basicity of the solution. The precipitate was collected by filtration. The obtained product was dissolved in ether, washed sequentially 1 N. Hcl, saturated Panso3and brine, dried over Na2SO4concentrated in vacuo and used without further purification. The product with the remote protective group was allocated in the form of bicarbonate salt (pale brown solid) with a yield of 22%. The product gave a single homogeneous peak in the analysis of HPLC on a C18-column, 15 cm in 1511, 14658, 1443, 1392, 1352, 1302, 1244, 1223, 1175, 1046, 742 cm-1. Connection 146 2-{ 2-[4-[2-(N,N-Bis-tert - butoxycarbonylamino)ethyl] -phenoxy]ethyl} -4-(3 - Chlorobenzyl)-3,4-dihydro-6-methoxy-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from intermediate 12168-25-1 (reference example 43) and N, N'-di-tert-butoxycarbonyl-2- (4-hydroxyphenyl)-ethylguanidine way L with a yield of 92%. Crystallization from a mixture of ethanol/N2O gave pure product as a white solid. NMR (CDCl3) to 11.28 (s, 1H), 7.23 percent (m, 3H), 7,12 (m, 1H), 7,12 (d, J=9.0 Hz, 2H), 6,94 (d, J=8,9 Hz, 1H), 6,86 (d, J=9.0 Hz, 2H), 6,51 (DD, J=8,4, 2,9 Hz, 1H), 6,41 (d, J=2.1 Hz, 1H), 5,15 (d, J=16.9 and Hz, 1H), of 5.05 (d, J=16,9 Hz, 1H), 4,89 (DD, J=10,0, 4,1 Hz, 1H), 4,20 (m, 2H), to 3.64 (m, 2H), 2,82 (apparent t, J=7,3 Hz, 2H), by 2.55 (m, 1H), 2,32 (m, 1H), 1,52 (s, N), 1,50 (s, N). Connection 147 4-{ 3-Chlorobenzyl)-3,4-dihydro-2-{2-[4-(2-guanidinate) -phenoxy]ethyl} -6-methoxy-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from compound 146 way To and allocated by rubbing with diethyl ether in the form of hygroscopic reddish-brown solid with a yield of 76%; NMR (DMSO-d6) 7,43 (Shir.s, 1H), 7,4-6,5 (PTS.Shir.s, 4H), 7,35 (m, 3H), 7,22 (m, 1H), 7,19 (d, J=8.5 Hz, 2H), 6,98 (d, J=8.6 Hz, 1H), of 6.96 (d, J= 8.5 Hz, 2H), is 6.61 (d, J=2.5 Hz, 1H), 2,58 (DD, J=9,0, 3.1 Hz, 1H), total of 5.21 (d, J=17,0 Hz, 1H), 5,18 (d, J=17,0 Hz, 1H), 4,96 (DD, J=8,8, 4,1 Hz, 1H), 4,19 (m, 2H), 3,64 (with, is enocsi] ethyl}-3,4-dihydro-6-fluoro-4-(3-nitrobenzyl)-3-oxo-2H-1,4-benzoxazin < / BR> Obtained from compound 102 by way To. Specified in the title compound was obtained as solid product: so pl.: decomposition at >76oC; MS (FAB) MN+508; IR (KBR) 3349, 3180, 2932, 2872, 1621, 1531, 1506, 1469, 1296, 948, 838 cm-1;1H (NMR) to 8.20 (s, 1H), 8,13 (d, 1H, J=7.9 Hz), 7,66 (m, 2H), 7,53 (Shir.s, 1H), 7,50-6,60 (PTS.Shir.s, 3H), 7,19 (d, 2H, J=8,4 Hz), to 7.09 (m, 2H), 6.90 to (d, 2H, J=8,4 Hz), 6,85 (m, 1H), 5,32 (s, 2H), free 5.01 (DD, 1H, J=4,3, and 8.7 Hz), 4,18 (m, 2H), or 3.28 (m, 2H), 2,71 (t, 2H, J=7,2 Hz), 2,39 (m, 1H), of 2.25 (m, 1H). 1. Benzoxazinone or pyridoxine compounds selected from compounds of the formula I < / BR> where part of the Q - condensed phenyl, or condensed pyridyl; Z1is hydrogen, halogen, C1-C6alkyl, phenyl, nitro, sulfonylamino or trifluoromethyl; Z2is hydrogen or halogen; X is hydrogen or oxygen; A - C1-C6alkyl, C1-C6alkylaryl or C1-C6alkylglycerol, where aryl represents a biphenyl, naphthyl or phenyl and heterocyclyl represents a 5-membered saturated heterocyclic group containing a sulfur atom, or a 6-membered saturated heterocyclic group containing a nitrogen atom, where the aryl or heterocyclyl group optionally substituted C1-C6) alkyl, oxobenzo ) alkoxy or methylsulfonylamino; n = 0-3; Y - part, selected from (a) other1R2N+R1R2R3< / BR> (b) < / BR> (g) CH(R6)CO2H, CH(Rb)CO2CH3; (d) residue formula < / BR> where R1, R2and R3independently is hydrogen, C1-C6alkyl or tert-butoxycarbonyl; R4and R5regardless - tert-butoxycarbonyl or hydrogen; R6is hydrogen, hydroxy or chlorine; and their pharmaceutically acceptable salts, esters and proletarienne forms. 2. Connection on p. 1, where Q is a condensed phenyl. 3. Connection on p. 1, where part a is chosen from the group comprising C1-C5alkyl, CH2-phenyl, CH2-thienyl, CH2-pyridyl and ethylpiperidine. 4. Connection on p. 1, where part of Y is chosen from a) other1R2N+R1R2R3; b) < / BR> (g) CH(R6)CO2H; (d) residue formula < / BR> where R1, R2and R3independently is hydrogen, C1-C6alkyl or tert-butoxycarbonyl; R4and R5independently - tert-butoxycarbonyl or hydrogen; R6is hydrogen or hydroxy, and its pharmaceutically acceptable salts, esters and proletarienne form. 2is hydrogen or, when Z1- halogen, Z2also halogen; X is oxygen; And - C1-C5alkyl, CH2-phenyl, CH2-thienyl, CH2-pyridyl or ethylpiperidine, where the phenyl, thienyl, pyridyl, or piperidine optionally substituted C1-C6)alkyl, oxybenzyl, phenoxy, hydroxy, alkoxy, halogen, two atoms of halogen, nitro, carboxyla or carbomethoxy; n = 0-3; Y is a part selected from 9. Connection on p. 1, which is 4-(3-Chlorobenzyl)-3,4-dihydro-2-[2-[4-(2-guanidinate)phenoxy] ethyl] -3-oxo-2H-pyrido[3,2-b] 1,4-oxazin. 10. Connection on p. 1, which is a 2-{2-[4-(2-aminomethyl) phenoxy]ethyl}-4-(3,5-dichlorobenzyl)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin. 11. Connection on p. 1, which is 4-(3,5-dichlorobenzyl)-3,4-dihydro-2-(2-[4-(2-guanidinate)phenoxy] -ethyl} -3-oxo-2H-1,4-benzoxazin. 12. Connection on p. 1, which is 6-chloro-4-(3-Chlorobenzyl)-2-{ 2-[4-(2-guanidinylation)phenoxy] ethyl} -3,4-dihydro-3-oxo-2H-1,4-benzoxazin. 13. Connection on p. 1, which is 4-(3-Chlorobenzyl)-6,8-dichloro-2-{ 2-[4-(2-guanidinylation)phenoxy] ethyl}-3,4-dihydro-3-oxo-2H-1,4-benzoxazin. 14. Connection on p. 1, which is 4-(3-Chlorobenzyl)-2-{ 2-[4-(2-guanidinylation)phenoxy] ethyl} -3,4-dihydro-7-methyl-3-oxo-2H-1,4-benzoxazin. 15. Connection on p. 1, which is a 2-{2-[3-(2-aminoethyl)phenoxy]ethyl}-4-(3-Chlorobenzyl-3,4-dihydro-3-oxo-2H-1,4-benzoxazin. 16. Connection on p. 1, which is 4-(3-Chlorobenzyl)-3,4-dihydro-2-{2-(2-[4-(2-guanidinylation)phenoxy]-ethyl}-2H-1,4-benzoxazin. 17. Connection on p. 1, LASS="ptx2">18. Connection on p. 1, which is 4-(3-Chlorobenzyl)-3,4-dihydro-2-{2-[4-(guanidinylation)phenoxy]-ethyl}-2H-1,4-benzoxazin. 19. Connection on p. 1, which is 4-(2-Chlorobenzyl)-3,4-dihydro-2-{ 2-[4-(2-guanidinate)phenoxy]-ethyl}-7-nitro-3-oxo-2H-1,4-benzoxazin monohydrochloride. 20. Connection on p. 1, which is 3,4-dihydro-2-{2-[4-(2-guanidinate)phenoxy] ethyl} -6-nitro-4-(2-nitrobenzyl)-3-oxo-2H-1,4-benzoxazin. 21. Connection on p. 1, which is 3,4-dihydro-4-(2,4-dichlorobenzyl)-2-{ 2-[4-(2-guanidinate)phenoxy] ethyl}-3-oxo-2H-1,4-benzoxazin. 22. Connection on p. 1, which is a 2-[2-[4-(3-aminopropyl)phenoxy[ethyl]-4-(4-chlorbenzyl)-3,4-dihydro-3-oxo-2H-1,4-benzoxazin. 23. Pharmaceutical composition having antibacterial activity, containing an effective amount of the compounds under item 1. 24. A method of treating bacterial infections in mammals by introduction of a mammal suffering from such infection a therapeutically effective amount of the compounds under item 1. 25. The way the increased activity of the antibacterial agent in mammals by introduction of this antibacterial x infections, containing antibacterial agent and a connection on p. 1, in therapeutically effective amounts in combination with a pharmaceutically acceptable carrier. 27. The method of obtaining the compounds of formula I< / BR> where part of the Q - condensed phenyl, or condensed pyridyl; Z1is hydrogen, halogen, C1-C6alkyl, phenyl, nitro, sulfonylamino or trifluoromethyl; Z2is hydrogen or halogen; X is hydrogen or oxygen; A - C1-C6alkyl, C1-C6alkylaryl or C1-C6alkylglycerol, where aryl represents a biphenyl, naphthyl or phenyl and heterocyclyl represents a 5-membered saturated heterocyclic group containing a sulfur atom, a 6-membered saturated heterocyclic group containing a nitrogen atom, where the aryl or heterocyclyl group optionally substituted C1-C6the alkyl, oxybenzyl, phenoxy, hydroxy, alkoxy, halogen, two atoms of halogen, nitro, carboxyla, Carbo(C1-C4)alkoxy or methylsulfonylamino; n = 0-3; Y - part, selected from (a) other1R2N+R1R2RC; (b) < / BR> (g) SN(R6)CO2N; SN(R6)CO2CH3alkyl or tert-butoxycarbonyl; R4and R5independently - tert-butoxycarbonyl or hydrogen; R6is hydrogen, hydroxy or chlorine, and their pharmaceutically acceptable salts, esters and proletarienne forms, which consists in the reaction of compounds of formula < / BR> with the compound of the formula < / BR> where the rest of Y is protected or unprotected, in a suitable solvent in the presence of a suitable phosphine and azodicarbonamide reagent and, when Y is protected, the removal of the protective groups and the allocation of the compounds of formula I. 28. The method of obtaining the compounds of formula < / BR> which lies in the interaction of the compounds of formula < / BR> with the compound of the formula < / BR> in the presence of a suitable base to obtain the compounds of formula < / BR> and then cyclization of this compound with a suitable reducing agent to obtain compounds of the formula < / BR> 29. The method of obtaining the compounds of formula < / BR> which lies in the interaction of the compounds of formula < / BR> with the compound of the formula < / BR> in a suitable basis. 31. Derived tetrahydrofuran formula < / BR> where part of Q is phenyl or pyridyl; Z1is hydrogen, halogen, C1 32. The connection formulas < / BR> where part of Q is phenyl or pyridyl; Z1is hydrogen, halogen, C1-C6alkyl, phenyl, nitro, sulfonylamino or trifluoromethyl; Z2is hydrogen or halogen; A - C1-C6alkylaryl or C1-C6alkylglycerol, where aryl - biphenyl, naphthyl or phenyl and heterocyclyl represents a 5-membered saturated heterocyclic group containing a sulfur atom, or a 6-membered saturated heterocyclic group containing a nitrogen atom, where the aryl or heterocyclyl group optionally substituted C1-C6)alkyl, oxybenzyl, phenoxy, hydroxy, alkoxy, halogen, two atoms of halogen, nitro or carboxyla, Carbo(C1-C4)alkoxy or methylsulfonylamino.
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