The method of obtaining 2-oxo-2 - methyl-4 - diethylamino-5,5 - dimethyl-1,3,2 - oxazaphosphorin-3-in

 

(57) Abstract:

Usage: in agriculture as a plant growth regulator. The inventive product 2-oxo-2 - methyl-4 - diethylamino-5,5 - dimethyl-1,3,2 - oxazaphosphorin-2-in f-ly 1. BF C9H19N2O2P , yield 94%. Reagent 1: compound f-crystals 2, where R is a C1-C4-alkyl. Reagent 2: (C2H5)2NH . Reaction conditions: reagent ratio 1 and 2 is equal to 1:(3-5), the process is carried out by boiling the reaction mixture for 3 hours f-crystals 1, 2:

The invention relates to chemistry fosforsodyerzhascikh heterocyclic compounds, and in particular to methods for obtaining compounds of formula

H3C - N(C2H5)2which is an effective postregulation some agricultural crops.

The aim of the invention is to develop a convenient method of obtaining 2-oxo-2-methyl-4-diethylamino-5,5-dimethyl-1,3,2-oxa - sapoval-3-in.

This goal is achieved by reacting 2-okno-2-methyl-4-alkoxy-5,5-dimethyl-1,3,2-oxazaphosphorin-3-in [1] with an excess of diethylamine in a molar ratio of 1:(3-5), respectively. The reaction proceeds within 3 hours at the boiling temperature of the reaction mixture. The selection of the product with allaamah method consists in the following:

H3C - OR + (C2H5)2NHhouses_ N(C2H5)2+ ROH

where R = C1-C4-alkyl (isoalkyl).

Diethylamin in the process of playing the role of the reagent and solvent.

The technique of synthesis of the target compounds is as follows. In a reactor equipped with a stirrer and reflux condenser was loaded 2-oxo-2-methyl-4-alkoxy-5,5-dimethyl-1,3,2-oxazaphosphorin-3-in diethylamine in a molar ratio of 1: (3-5). Using diethylamine less than 3-fold decreases the yield of the target product, and more than 5 times does not increase output, but only leads to a waste of diethylamine. Under stirring for 3 h, warmed up the reaction mixture at the boiling point amine. Then the excess amine and the reaction alcohol drove away under reduced pressure. The output of the compounds obtained is a slightly coloured viscous liquid when stored prone to crystallization, soluble in most organic solvents and in water. The identity and structure of the synthesized compounds was confirmed by thin-layer chromatography, full elemental analysis, determination of molecular refraction and molecular weight (cryoscopy in benzene), IR spectra the situations of groups of molecules , cm-1: 1630 (C=N); 1390 (C(CH3))2; 1305 (P-CH3); 1230 (P=0); 1050 (P-O-Salk); 820 (P-N).

(table, experiment 1). P R I m e R 1. In a reactor equipped with a stirrer, reflux condenser, downloaded 1.6 g (0,007 g/mole) 2-oxo-2-methyl-4-isopropoxy-5,5-dimethyl-1,3,2-oxazaphosphorin-3-ina and 2.0 g (0,0274 mol) of diethylamine (molar ratio of reactants is 1:3). With stirring, they were heated the reaction mixture at the boiling temperature of the mixture (60aboutC) for 3 hours and Then under reduced pressure drove the excess amine and the reaction of alcohol. Final purification of the target product was performed by the method of column chromatography on silica gel brand stewards, eluent - hexane: 2-propanol 1:6. Obtained 1.6 g of 2-oxo-2-methyl-4-diethylamino-5,5-dimethyl-1,3,2-oxa - sapoval-3-in. Output 94,1%.

Found, %: C 49,73; H 8,88; N 13,00; P 14,43.

Calculated, %: C 49,53; H 8,77; N Is 12.85; P 14,19.

nD201,4876; d4201,1720. MR 55,29 calculated 55,79. M 215, calc. 218 (cryoscopy in benzene).

Due to the identical methods, the parameters of other examples are given in the table showing the dependence of the yields of the target compounds from the parameters of synthesis.

The table shows that the increase in excess diethylamine above 5 mol) in relation to the South exit. The same reduction of the reaction time below 3 h or excess diethylamine below 3-molar reduces the yield of the target product (up 3%). In table summarizes the results of 8 experiments, in which the molar amount of one of the reagents (1,3,2-oxazaphosphorine) remained constant, and the molar number of diethylamine varied from 2.5-fold to 5-fold excess.

The compound obtained showed high astragulus activity in the primary and in-depth testing on some crops. The results of these tests it is recommended for industrial tests.

Thus, the proposed method of producing 2-oxo-2-methyl-4-diethylamino-5,5-dimethyl-1,3,2-oxazaphosphorin-3-in is easy, adaptability, high efficiency and allows to obtain a sufficiently pure target product with high yield.

The METHOD of OBTAINING 2-OXO-2-METHYL-4-DIETHYLAMINO-5,5-DIMETHYL-1,3,2-OXAZAPHOSPHORIN-3-INA, characterized in that 2-oxo-2-methyl-4-alkoxy-5,5-dimethyl-1,3,2-oxazaphosphorin-3-in is subjected to interaction with diethylamine at a molar ratio of reagents, 1 : 3 - 5 at the boiling temperature of the reaction mixture for 3 hours

 

Same patents:

The invention relates to the field of organofluorine compounds, particularly to a method of obtaining derivatives softinterface acid next строенияQ STN - RA , where R is--OR or NR-2; R is lower alkali

The invention relates to the chemistry of organophosphorus compounds, namely to a new method of obtaining S-trialkylsilyl - ash and stanilova esters of 4-methoxyphenylacetic or triiodobenzoic acids of General formula I 4-MeOC6Hwhere R, R1is lower alkyl; E is Si, Sn; X Is O, S

The invention relates to the field of organofluorine compounds, particularly to a method of obtaining derivatives softinterface acid next строенияQ STN - RA , where R is--OR or NR-2; R is lower alkali

FIELD: organic chemistry, in particular improved method for production of phosphorinated and chlorinated methacrylates.

SUBSTANCE: invention relates to method for production of compounds having general formula , wherein R is lower alkyl and R1 is lower alkoxyl, phenoxyl, or group of formula . Claimed method includes reaction of pentavalent phosphorous acid chloroanhydride with glycydil methacrylate at 20-50°C in presence of titanium tetrachloride as catalyst in amount of 0.02-0.05 % calculated as reagent mass.

EFFECT: one-step method for production of phosphorous and chlorine containing methacrylates with improved water resistance.

2 tbl, 7 ex

FIELD: chemistry of organophosphorus compounds.

SUBSTANCE: invention relates to compounds with the bond C-P, namely to phosphorus-boron-containing methacrylate that can be used as inhibitor of combustion of polyvinyl alcohol-base film materials. Invention describes phosphorus-boron-containing methacrylate of the following formula: wherein n = 4-8. Polyvinyl alcohol films modified with indicated phosphorus-boron-containing methacrylate shows the enhanced refractoriness, rupture strength up to 206 kgf/cm2, water absorption up to 240% and relative elongation up to 12%.

EFFECT: valuable properties of substance.

1 tbl, 2 ex

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to the improved method for preparing N-phosphonomethylglycine. Method involves interaction of derivative of hexahydrotriazine of the formula (II):

wherein X represents CN, COOZ, CH2OY and others; Z and Y represent hydrogen atom and others with triacylphosphite of the formula: P(OCOR3)3 (III) wherein R3 means (C1-C18)-alkyl or aryl that can be substituted. The prepared product is hydrolyzed and (if X represents CH2OY) oxidized. The proposed method is a simple in realization, economy and provides high degree of the end product purity.

EFFECT: improved preparing method.

19 cl, 11 ex

FIELD: organic chemistry, chemical technology, medicine.

SUBSTANCE: invention relates to acyclic nucleoside phosphonate derivatives of the formula (1): wherein means a simple or double bond; R1 means hydrogen atom; R2 and R3 mean hydrogen atom or (C1-C7)-alkyl; R7 and R8 mean hydrogen atom or (C1-C4)-alkyl; R4 and R5 mean hydrogen atom or (C1-C4)-alkyl possibly substituted with one or more halogen atoms, or -(CH2)m-OC(=O)-R6 wherein m means a whole number from 1 to 5; R6 means (C1-C7)-alkyl or 3-6-membered heterocycle comprising 1 or 2 heteroatoms taken among the group consisting of nitrogen (N) and oxygen (O) atoms; Y means -O-, -CH(Z)-, =C(Z)-, -N(Z)- wherein Z means hydrogen atom, hydroxy-group or halogen atom, or (C1-C7)-alkyl; Q (see the claim invention); its pharmaceutically acceptable salts or stereoisomers. Also, invention proposes methods for preparing compounds of the formula (1) and their using in treatment of hepatitis B or preparing a medicinal agent designated for this aim.

EFFECT: improved preparing method, valuable medicinal properties of compounds and agent.

16 cl, 10 tbl, 87 ex

FIELD: chemistry of organophosphorus compounds.

SUBSTANCE: invention relates to the improved method for synthesis phosphorus-chlorine-containing methacrylates that can be used in synthesis of polymeric, among them, uncolored, optically transparent and composition materials with reduced inflammability. Invention describes a method for synthesis of phosphorus-chlorine-containing methacrylates of the general formula:

wherein R means lower alkyl, chloroalkyl, alkoxyl, phenoxyl or group of the formula:

R1 means lower alkoxyl, phenoxyl or group of the formula:

Method involves interaction of phosphoric pentavalent acid chloroanhydrides with methacrylic acid glycidyl ester at heating in the presence of hexamethylenephosphorotriamide or dimethylformamide as a catalyst wherein catalyst is taken in the amount 0.3-0.6% of reagents mass, and process is carried out at rise of temperature from 40°C to 80°C in the presence of compound chosen from the group: alkyl- or alkoxy-substituted phenols taken in the amount 0.03-0.3% of reagents mass. Method provides decreasing water absorption of (co)polymerization products of synthesized phosphorus-chlorine-containing methacrylates and reducing retention time of surface stickiness of fiber glass synthesized on their basis and at retention the level of other properties, among them transparence and colorless.

EFFECT: improved method of synthesis, improved and valuable properties of compounds.

2 tbl, 10 ex

FIELD: organic chemistry, biochemistry, medicine.

SUBSTANCE: invention relates to phosphonic acid compounds used as inhibitors of serine proteinase of the general formula (I): wherein R1 is chosen from group comprising piperidinyl, pyrrolidinyl and 1,3,8-triazaspiro[4,5]dec-8-yl (wherein heterocyclic ring as added to nitrogen atom in ring) and -N(R7R80 wherein this heterocyclic ring is substituted optionally with one or two substitutes chosen independently from group comprising the following compounds: (a) C1-C8)-alkyl substituted optionally at terminal carbon atom with a substitute chosen from group comprising aryl, heteroaryl; c) phenyl and naphthalenyl; i) benzothiazolyl; R7 is chosen from group comprising hydrogen atom and (C1-C8)-alkyl; R8 is chosen from group comprising: (aa) (C1-C8)-alkyl; (ab) cycloalkyl; (ac) cycloalkenyl, and (ad) heterocyclyl (wherein R8 is added to carbon atom in ring) wherein (ab) cycloalkyl; (ac) cycloalkenyl, and (ad) heterocyclyl (wherein heterocyclyl (ad) comprises at least one cyclic nitrogen atom) substitutes and cycloalkyl moiety (aa) of a substitute is substituted optionally with substitutes chosen independently from group comprising: (ba) (C1-C8)-alkyl substituted at terminal carbon atom with a substitute chosen from group comprising amino-group (with two substitutes chosen independently from group comprising hydrogen atom and (C1-C8)-alkyl); (bb) (C1-C8)-alkoxy-group substituted at terminal carbon atom with a substitute chosen from group comprising carboxyl; (bc) carbonyl substituted with a substitute chosen from group comprising (C1-C8)-alkyl, aryl, aryl-(C2-C8)-alkenyl; (bd) aryl; (be) heteroaryl; (bf) amino-group substituted with two substitutes chosen independently from group comprising hydrogen atom and (C1-C8)-alkyl; (bh) halogen atom; (bi) hydroxy-group; (bk) heterocyclyl wherein (bd) is aryl substitute, and heteroaryl moiety (bc) comprise a substitute (halogen atom)1-3; R4 is chosen from group comprising aryl and heteroaryl wherein heteroaryl comprises halogen atom as a substitute; R2 and R3 are bound with benzene ring and represent hydrogen atom, and R2 and R3 form in common optionally at least one ring condensed with benzene ring forming polycyclic system wherein this polycyclic system is chosen from group comprising (C9-C14)-benzocondensed cycloalkenyl, (C9-C14)-benzocondensed phenyl; R5 is chosen from group comprising hydrogen atom and (C1-C8)-alkyl; R6 is chosen from group comprising (C1-C8)-alkyl and hydroxy-group; Y is absent, and X represents a single substitute that is added by a double bond and represents oxygen atom (O), and Z is chosen from group comprising a bond, hydrogen atom, and its salts. Also, invention relates to a method for synthesis of these compounds, to their composition inhibiting serine proteinase and to a method for its preparing. Proposed invention describes a method for treatment of inflammatory or serine proteinase-mediated disorder.

EFFECT: valuable biochemical and medicinal properties of compounds.

64 cl, 5 tbl, 38 ex

FIELD: organic chemistry, medicine, biochemistry.

SUBSTANCE: invention describes compound of the formula (I): wherein R1 means hydrogen atom (H); R2 means -SH, -S-C(O)-R8, -P(O)(OR5)2, -P(O)(OR5)R6, -P(O)(OR5)-R7-C(O)-R8, -P(O)(OR5)-R7-N(R5)-S(O)2-R9 or -P(O)(OR5)-R7-N(R5)-C(S)-N(R6)2; R3 means tetrazole, -C(O)OR6, -C(O)O-R7-OC(O)R5; R4 means optionally substituted aryl, or R4 means N-heterocyclyl. Also, invention describes compounds of the formula (II): and (III): wherein X means -CH2- or -O-, and pharmaceutical compositions comprising indicated compounds. Proposed compounds possess inhibitory effect on activity of plasma carboxypeptidase B and used as anti-thrombosis agents.

EFFECT: valuable medicinal and biochemical properties of compounds.

34 cl, 19 ex

FIELD: chemistry.

SUBSTANCE: invention concerns process of production of diisopropyl {[1-(hydroxymethyl)-cyclopropyl]oxy}methylphosphonate represented by the formula , which is the key intermediate compound in synthesis of antiviral nucleoside analogue. The invention also concerns new intermediate compounds of formulae and , and their production of compound (2) obtained under this invention, which is an antiviral nucleoside analogue (especially against hepatitis B virus) represented by the formula .

EFFECT: high purity grade and high output.

4 ex

FIELD: chemistry.

SUBSTANCE: invention relates to protection of metals from corrosion using lacquer coating. This engineering problem can be solved by using calcium hydroxyethylidenediphosphonate with formula CH3(OH)C(PO3)2Ca2 as an anti-corrosion pigment, with higher anti-corrosion activity as compared to the prototype - protonated zinc hydroxyethylidenediphosphonate and a control specimen - zinc tetraoxychromate.

EFFECT: low-toxic high performance anti-corrosion pigment.

1 tbl, 3 ex

FIELD: chemistry.

SUBSTANCE: invention refers to method of production of C-phosphorylated alkylamidines serving as parent compounds of biologically active compounds for medicine and agriculture, of formula: where R1=C3-C4alkyl or isoalkyl; R2=CH3, C6H5; R3=C2-C4-alkyl or isoalkyl; R4=H, CH3, C3H7, C6H5, COOC2H5. Method includes in production of sodium derivatives of C-phosphorylated alkylamidines resulted from reaction of C-phosphorylated acetamidine with sodium. Produced sodium derivative is alkylated with alkylhalogenide in dioxane medium at mole ratio sodium:C-phosphorylated acetamidine:alkylhalogenide (1:1:1÷1.1), respectvely at temperature 20÷50°C.

EFFECT: production of new C-phosphorylated alkylamidines with high yield exceeding 78%.

1 cl, 9 ex

FIELD: chemistry of organophosphorus compounds, biochemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new bisamidate phosphonate compounds that are inhibitors of fructose 1,6-bis-phosphatase. Invention describes a compound of the formula (IA): wherein compound of the formula (IA) is converted in vivo or in vitro to compound of the formula M-PO3H2 that is inhibitor of fructose 1,6-bis-phosphatase and wherein M represents R5-X- wherein R5 is chosen from a group consisting of compounds of the formula or wherein each G is chosen from the group consisting of atoms C, N, O, S and Se and wherein only one G can mean atom O, S or Se and at most one G represents atom N; each G' is chosen independently from the group consisting of atoms C and N and wherein two G' groups, not above, represent atom N; A is chosen from the group consisting of -H, -NR42, -CONR42, -CO2R3, halide, -S(O)R3, -SO2R3, alkyl, alkenyl, alkynyl, perhaloidalkyl, haloidalkyl, aryl, -CH2OH, -CH2NR42, -CH2CN, -CN, -C(S)NH2, -OR2, -SR2, -N3, -NHC(S)NR42, -NHAc, or absent; each B and D is chosen independently from the group consisting of -H, alkyl, alkenyl, alkynyl, aryl, alicyclyl, aralkyl, alkoxyalkyl, -C(O)R11, -C(O)SR11, -SO2R11, -S(O)R3, -CN, -NR92, -OR3, -SR3, perhaloidalkyl, halide, -NO2, or absent and all groups except for -H, -CN, perhaloidalkyl, -NO2 and halide are substituted optionally; E is chosen from the group consisting of -H, alkyl, alkenyl, alkynyl, aryl, alicyclyl, alkoxyalkyl, -C(O)OR3, -CONR42, -CN, -NR92, -NO2, -OR3, -SR3, perhaloidalkyl, halide, or absent; all groups except for -H, -CN, perhaloidalkyl and halide are substituted optionally; J is chosen from the group consisting of -H, or absent; X represents optionally substituted binding group that binds R5 with phosphorus atom through 2-4 atoms comprising 0-1 heteroatom chosen from atoms N, O and S with exception that if X represents urea or carbamate then there are 2 heteroatoms that determine the shortest distance between R5 and phosphorus atom and wherein atom bound with phosphorus means carbon atom and wherein X is chosen from the group consisting of -alkyl(hydroxy)-, -alkynyl-, - heteroaryl-, -carbonylalkyl-, -1,1-dihaloidalkyl-, -alkoxyalkyl-, -alkyloxy-, -alkylthioalkyl-, -alkylthio-, -alkylaminocarbonyl-, -alkylcarbonylamino-, -alkoxycarbonyl-, -carbonyloxyalkyl-, -alkoxycarbonylamino- and -alkylaminocarbonylamino- and all groups are substituted optionally; under condition that X is not substituted with -COOR2, -SO3H or -PO3R22; n means a whole number from 1 to 3; R2 is taken among the group -R3 and -H; R3 is chosen from the group consisting of alkyl, aryl, alicyclyc and aralkyl; each R4 is chosen independently from the group consisting of -H and alkyl, or R4 and R4 form cycloalkyl group; each R9 is chosen independently from the group consisting of -H, alkyl, aryl, aralkyl and alicyclyl, or R9 and R9 form in common cycloalkyl group; R11 is chosen from the group consisting of alkyl, aryl, -NR22 and -OR2; each R12 and R13 is chosen independently from the group consisting of hydrogen atom (H), lower alkyl, lower aryl, lower aralkyl wherein all groups are substituted optionally, or R12 and R13 in common are bound through 2-5 atoms comprising optionally 1-2 heteroatoms chosen from the group consisting of atoms O, N and S to form cyclic group; each R14 is chosen independently from the group consisting of -OR17, -N(R17)2, -NHR17, -NR2OR19 and -SR17; R15 is chosen from the group consisting of -H, lower alkyl, lower aryl, lower aralkyl, or in common with R16 is bound through 2-6 atoms comprising optionally 1 heteroatom chosen from the group consisting of atoms O, N and S; R16 is chosen from the group consisting of -(CR12R13)n-C(O)-R14, -H, lower alkyl, lower aryl, lower aralkyl, or in common with R15 is bound through 2-6 atoms comprising optionally 1 heteroatom chosen from the group consisting of atoms O, N and S; each R17 is chosen independently from the group consisting of lower alkyl, lower aryl and lower aralkyl and all groups are substituted optionally, or R17 and R17 at atom N are bound in common through 2-6 atoms comprising optionally 1 heteroatom chosen from the group consisting of atoms O, N and S; R18 is chosen independently among the group consisting of hydrogen atom (H), lower alkyl, aryl, aralkyl, or in common with R12 is bound through 1-4 carbon atoms forming cyclic group; each R19 is chosen independently from the group consisting of -H, lower alkyl, lower aryl, lower alicyclyl, lower aralkyl and -COR3; and under condition that when G' represents nitrogen atom (N) then the corresponding A, B, D or E are absent; at least one from A and B, or A, B, D and E is chosen from the group consisting of -H, or absent; when G represents nitrogen atom (N) then the corresponding A or B is not halide or group bound directly with G through a heteroatom; and its pharmaceutically acceptable salts. Also, invention describes a method for treatment or prophylaxis of diabetes mellitus, a method for inhibition of activity 0f fructose 1,6-bis-phosphatase, a method for decreasing blood glucose in animals, a method for treatment of diseases associated with glycogen deposition, a method for inhibition of gluconeogenesis in animal and a pharmaceutical composition based on compounds of the formula (IA).

EFFECT: valuable medicinal and biochemical properties of compounds.

69 cl, 7 tbl, 64 ex

FIELD: chemistry of organophosphorus compounds, chemical technology.

SUBSTANCE: invention relates to novel compounds used for extraction of rare-earth metal ions and comprising phosphoneamide compound represented by he formula [1]: wherein R1 means aryl group, aralkyl group under condition that each group can comprise a substitute chosen from alkoxy-groups; R2 means alkyl group, alkenyl group, aryl group, aralkyl group under condition that each group can comprise a substitute chosen from alkyl groups, alkoxy-groups; R3 means hydrogen atom, aryl group, aralkyl group under condition that each group can comprise a substitute chosen from alkyl groups, alkoxy-groups, halogen atoms; and two radical R can be combined to form alkylene group. Also, invention relates to a method for extraction of rare-earth metal ions and to a method for reverse extraction of rare-earth metal ions. Invention provides preparing novel phosphoneamide compounds and method for extraction and reverse extraction of rare-earth metal ions.

EFFECT: improved preparing method, valuable properties of compounds.

3 cl, 4 tbl, 44 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to a method of producing methyl-phosphonic acid thionylamide esters of formula: CH3P(O)(OR)N=S=O, where R = i-C3H7, C4H9, i-C4H9, which can be used as semi-finished products in organophosphorus synthesis. The disclosed method lies in obtaining end products by reacting thionylamide choroanhydride of methyl-phosphonic acid with alkoxytrimethylsilanes of general formula (CH3)3SiOR, where R = i-C3H7, C4H9, i-C4H9 at 40-50°C for 2 hours.

EFFECT: design of a new method of producing the said compounds.

1 cl, 2 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: present invention relates to a method of producing thionylamide cyan-anhydride of methylphosphonic acid of formula CH3P(O)(CN)N=S=O, which can be used as a semi-finished product in organophosphorus synthesis. The disclosed method lies in obtaining the end product by reacting thionylamide chloroanhydride of methylphosphonic acid with alkoxydimethylsilylcyanides of general formula (CH3)2Si(OR)CN, where R = CH3, C2H5,C3H7, i-C3H7 at 40°C for 20 minutes.

EFFECT: design of a new method of producing organophosphorus compounds.

1 cl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to compounds of formula VIII suitable in medicine as T3 mimetic drugs: VIII, where G is O, -S(=O)2- or -CH2-; R2 is halogen, alkyl, -CF3, -OCF3, alkoxy or cyano; R3 and R4 are H, halogen, alkyl or -(CRa2)maryl; T is selected from -(CRa2)k-, -CRb=CRb-(CRa2)n-, -(CRa2)n-CRb=CRb, -(CRa2)-CRb=CRb-(CRa2)-, O(CRa2)(CRa2)n-, -S(CRa2)(CRa2)n-, -N(Rc)(CRb2)(CRa2)n-, -N(Rb)C(O)(CRa2)n-, -(CRa2)nCH(NRbRc) -C(O)(CRa2)m-, -(CRa2)mC(O)-, -(CRa2)C(O)(CRa2)n-, -(CRa2)n C(O)(CRa2)- and -C(O)NH(CRb2)(CRa2)p-; Ra, Rb, Rc, R1, R6, R7, R8 and R9 are H, halogen or alkyl; or R6 and T with C atom form a 5-6-members ring with 0-2 groups -NRi-, -O- or -S-; Ri is H, -C(O)alkyl, alkyl or aryl; R5 is OH, alkoxy, -OC(O)Re, -OC(O)ORh, -F, -NHC(O)Re, -NHS(=O)Re, -NHS(=O)2Re, -NHC(S)NH(Rh) or -NHC(O)NH(Rh); Re is alkyl, -(CRa2)n-aryl, -(CRa2)n-cycloalkyl or -(CRa2)n- heterocycloalkyl; Rh is H or alkyl; X is P(O)YRllY'Rll; Y and Y' are O or -NRv-; R11 is H, alkyl, -C(Rz)2-OC(O)Ry, -C(RZ)2-O-C(O)ORy, -alkyl-S-C(O)Ry, -[C(Rz)2]q-COORy, -cycloalkylene-COORy, aryl, -C(Rz)2OC(O)SRy, -C(Rx)2COORy or two R11 and R11 form a cycle; k is within 1 to 4; m is within 0 to 3; n is within 0 to 2; p is within 0 to 1; q is 2 or 3; Rv, Rz, Ry and Rx are H or alkyl, or two Rx and Rx form a cycle.

EFFECT: production of new thymomimetic drugs.

19 cl, 80 ex, 10 tbl, 13 dwg

FIELD: chemistry.

SUBSTANCE: invention refers to the way of production of amide nitrilotrismethylenephosphonic acid ammonium salt used in creation of fire resistant composite materials based on thermoplasts with the formula: The method consists in the following: nitrilotrismethylenephosphonic acid is amidated at a high temperature under the influence of gas ammonia under some pressure until pH of the 1% solution of the obtained product makes up 6-6.5.

EFFECT: simplification of the synthesis process and reduction of the prime cost of amide nitrilotrismethylenephosphonic acid ammonium salt.

2 cl, 1 tbl, 3 ex

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