Organic chemistry (C07)

C   Chemistry; metallurgy(313007)
C07            Organic chemistry(60703)
C07M - (20)
Specific antibody to s100a4 or its fragment (versions), method of production thereof (versions), pharmaceutical composition containing said compounds, hybridoma cell line (versions), conjugate, composition, method of preventing and/or treating cancer, metastasis, angiogenesis and inflammatory diseases, method and kit for diagnosing cancer or disease associated with inflammation (versions), method of detecting s100a4, method of making individual therapy // 2615684
FIELD: biochemistry.SUBSTANCE: invention relates to biochemistry. Antibody to S100A4 characterized by antiangiogenic activity or its fragment in fact, preserving antiangiogenic activity of above antibody are described, wherein antibody is produced by hybridoma ECACC 10022401. Antibody contains at least area VL containing sequence SEQ ID NO: 1, and at least area VH containing sequence SEQ ID NO: 2, and identifies epitope containing sequence SEQ ID NO: 3, and it is characterized by activity profile, presented in Fig. 15. Antibody to S100A4 characterized by antiangiogenic activity or its fragment in fact preserving antiangiogenic activity of above antibody are also described, wherein antibody is produced by hybridoma selected from group comprising ECACC 11051801, ECACC 11051802 and ECACC 11051803, identifies epitope containing sequence SEQ ID NO: 24, and it is characterized by activity profile, presented in Fig. 15. Use of above antibodies in certain applications is also described.EFFECT: invention extends range of products for preventing and/or treating cancer, metastasis, angiogenesis and inflammatory diseases.36 cl, 26 dwg, 4 tbl, 16 ex
Onium salts of 4- (1,1-dinitroethyl 1-onn-azoxy) -3- (1h-tetrazol-5-yl) furoxan and methods for their preparation // 2615630
FIELD: chemistry.SUBSTANCE: invention relates to novel onium salts of 4-(1.1-dinitroetil-1-azoxy-ONN)-3-(1H-tetrazol-5-yl)furoxan general formula I: ,wherein and also methods for their preparation. A method for producing a new class of high-energy substances - the onium salts of 4-(1.1-dinitroetil-1-azoxy-ONN)-3-(1H-tetrazol-5-yl)furoxan general formula I.EFFECT: compounds may find use as components in rocket propellants and explosives compositions.4 cl, 1 tbl, 3 ex

ethod of producing propylene // 2615512
FIELD: chemistry.SUBSTANCE: method is to feed the metathesis reaction stream containing ethylene with butene in the presence of the first metathesis catalyst by the first metathesis reaction to form the product stream of the first metathesis containing propylene, ethylene, butene, and olefins C5 ; allocating of, at least, a part of propylene and ethylene from the product stream of the first metathesis to form the first upper stream and the first propene stripping bottom stream containing butene and olefins C5 ; reacting of, at least, a portion of the first propene stripping bottom stream with ethylene in the presence of the second metathesis catalyst by the second metathesis reaction to form the product stream of the second metathesis containing propylene, ethylene, butene, and olefins C5 ; and allocating of, at least, a portion of propylene and ethylene from the stream of the second metathesis to form the second upper stream; and recovering propylene from the first upper stream, the second upper stream or their combinations. Herewith the first metathesis reaction occurs at the first correlation of ethylene: butene of 0.3:1 to 3:1, and the second metathesis reaction occurs at the second correlation of ethylene: butene of 2.0: 1 to 10:1.EFFECT: increased degree of the butene conversion to propylene.14 cl, 2 tbl, 1 dwg

7-{(3s,4s)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidin-1-yl}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid crystal // 2615509
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, in particular, to a hydrochloride salt crystal, a hydrochloride salt hydrate crystal and methane sulphonate salt crystal 7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidin-1-yl}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid. Invention also relates to an antibacterial pharmaceutical preparation based on said crystal, a method of producing said crystals.EFFECT: technical result: obtained crystals have high solubility in water, as well as high storage stability.19 cl, 6 dwg, 4 tbl, 13 ex

Immunogenic peptides for application for prevention and/or treatment of infectious diseases, autoimmune diseases, the immune responses to allogeneic factors, allergic diseases, tumour, transplant rejection and immune responses against viral vectors used for genetic therapy or genetic vaccination // 2615460
FIELD: biotechnology.SUBSTANCE: invention relates to new peptides containing epitopes recognized by CD4+ natural killer T(NKT)-cells, and may be used in medicine. An immunogenic fusion peptide binding CD1d and containing [FWHY]-xx-[ILMV]-xx-[FWHY] and [CST]-xx-C or C-xx-[CST] motifs.EFFECT: invention allows to increase the activity of cells for use in case of infectious diseases, autoimmune diseases, immune reaction to allogeneic factors introduction, allergic diseases, for tumour therapy, for transplant rejection prevention and for prevention of immunization against viral proteins.20 cl, 4 dwg, 8 ex

Combined therapy by afucosylated antibody for cd20 with antibody for vegf // 2615459
FIELD: medicine, pharmacy.SUBSTANCE: invention refers to biotechnology, specifically to combination therapy by afucosylated antibody for CD20 and antibody for VEGF for cancer treatment, which can be used in medicine. A afucosylated humanized B-Ly1 antibody is applied in combination with the antibody for VEGF, with a composition containing tthe said antibodies for treatment of CD20-expressing cancer, and treatment of a patient suffering from CD20-expressing cancer.EFFECT: invention can effectively inhibit the growth of CD20-expressing tumors.20 cl, 1 dwg, 2 tbl

Immunostimulating oligodeoxynucleotides // 2615457
FIELD: biotechnology.SUBSTANCE: present invention relates to biotechnology. Immunostimulating methylated CpG-oligodeoxynucleotide, expression vector containing it, vaccine for preventing or controlling infectious disease in poultry, containing above oligodeoxynucleotide and/or expression vector and immunological amount of antigen component extracted from pathogenic for bird virus or microorganism, as well as application of oligodeoxynucleotide as medicinal agent and for prevention of infection in birds are disclosed.EFFECT: proposed oligodeoxynucleotide has high immunomodulatory action and can be used in veterinary as effective immunostimulating component in vaccines against infectious diseases of birds together with antigen component, extracted from virus or microorganism pathogenic for bird.29 cl, 32 dwg, 3 tbl, 24 ex

Human interleukin-7 encoding synthetic dna, expression vector containing this dna (versions), human interleukin-7 producing strain, and method for human interleukin-7 production // 2615447
FIELD: biotechnology.SUBSTANCE: synthetic DNA encoding human IL-7 is obtained, its expression vector containing a strain of Chinese hamster ovary cells - recombinant human Interleukin-7 producer, deposited under number RKKK(P) 770D. Strain provides accumulation of up to 180 mg/l of IL-7 in the culture medium for 15 days in serum-free chemically defined medium. Also, a method for glycosylated human IL-7 purification from the culture medium is provided.EFFECT: obtaining of a high-purity product with high glycosylation and specific activity.5 cl, 7 dwg, 2 tbl, 5 ex

Devices for automatic cell-free production of proteins and methods for proteins production using this product // 2615446
FIELD: biotechnology.SUBSTANCE: automated system for cell-free protein production, a cell-free method for protein production, and a reaction set for automated cell-free protein production are proposed. The system includes a protein expression reaction unit, a reaction temperature control unit, an array of pipettes, a pipette array movement unit, protein purification unit, multiwell plates attachment unit with a multiwell plate. At that, the protein reaction expression unit comprises a reaction vessel with a dialysis tube. Protein purification unit comprises a device for magnetic field application to attach the target protein to magnetic microspheres with subsequent magnetic microspheres attachment to the wall, and the multiwell plate is provided with solutions required for proteins production. The method comprises the stages of mixture preparation for cell-free protein expression, protein expression, protein purification using magnetic particles and purified protein dialysis. The reaction set comprises a set of multiwell plates with individual wells for storage of the solution with amino acids necessary for transcription and translation, a power source and buffer, dialysis tubes with a dialysis membrane.EFFECT: increased protein expression level.24 cl, 11 dwg, 8 ex
Fusion protein, dna, genetic construct, recombinant cell, fusion protein-based vaccine for tuberculosis prevention and treatment (versions) // 2615440
FIELD: biotechnology.SUBSTANCE: fusion proteins are proposed to induce a specific immune response against Mycobacterium tuberculosis, including Ag85B proteins, Tb10.4 M.tuberculosis, fragments of flagellin FliC S.Typhimurium, connected by flexible bridges, encoding polynucleotides, genetic constructs for expression of polynucleotides, recombinant cells, and vaccine options for tuberculosis prevention or treatment based on the described fusion protein, vaccine is developed for humans or animals. The proposed vaccine has an efficiency exceeds that of BCG.EFFECT: security and simplicity in production and application.8 cl, 4 dwg, 4 ex

ethod for treating salt-containing waste water of 2-ethylhexanol and 2-ethylhexanoic acid production, process area for its implementation // 2615422
FIELD: chemistry.SUBSTANCE: method involves the treament of the initial mixture with sulfuric acid and the separation of fatty acids. At the first stage, the waste water (6) is mixed with sulfuric acid (3), the mixture is transferred to a separator (9), from which the lower aqueous layer is fed to the collection tank for sodium sulfate solution (10), and the upper organic layer is fed into the tank for collecting the mixture of organic acids (11) returned to the production cycle. At the second stage, the aqueous sodium sulfate solution from the collecting tank (10) is fed at a rate ensuring the azeotropic mixture evaporation in an amount of 12-15% by weight of the water fed, at the temperature of 98-100°C, into the evaporator (12). The vapour phase from the evaporator (12) is fed through the heat exchanger (13) into the container (14) for separating the layers. The lower layer is fed into the container (15) for the sodium sulfate solution with a minimum content of organic impurities, and the upper layer containing not more than 20-30% of the light alcohols mixture is returned to the 2-ethylhexanol production cycle. The aqueous solution not evaporated in the evaporator (12) is fed into the container (15) for directing into the sewage treatment plant. The process area for the method implementation includes two groups of equipment assemblies providing two-stage treatment of salt-containing wastewater.EFFECT: obtaining at least 15 per cent of the commercial product from the volume of treated salt-containing waste waters, excluding the burning operation when disposing salt-containing waste water, obtaining cleaned water with the pH 6 and a low content of COD.2 cl, 1 dwg,1 ex

ethod of separating mixtures with high content of liquid-phase product // 2615412
FIELD: technological processes.SUBSTANCE: method of separating mixtures with high content of liquid-phase product using a tray column with horizontally mounted curtains and vertically positioned tray drain devices comprises injecting the raw material to the column by one or two streams, forming the raw material of two fluid streams in the column below the water level, forming upwardly flowing vapour (gas) stream at the bottom of the column by injecting a stripping agent and (or) by heating and evaporating of part of the fluid streams, alternating contact of the fluid streams with the upwardly flowing vapour (gas) stream of the column at the curtains of only their group of trays, transporting of fluid streams to the column bottom by avoiding the tray groups of another fluid stream, withdrawal of separation products from the column in liquid and vapour (gas) phases, wherein the alternating contact of the fluid streams with the upwardly flowing vapour (gas) stream is carried out at the curtains of adjacent column trays to produce liquid-vapour (gas) system with high monodispersity degree and highly-developed surface of phase connecting using the curtains with finely perforatedirreversible elements, transporting of fluid streams to the column bottom is carried out only by tray drain devices.EFFECT: increased fluid-carrying capacity and separating capacity of column lower than the level of raw material input.6 cl, 3 dwg, 3 ex

Alkylated cyclodextrin compositions and processes for preparing and using the same related applications // 2615385
FIELD: pharmaceutics.SUBSTANCE: group of inventions relates to pharmaceutics and provides a process for producing sulfoalkyl ethers of cyclodextrin ensuring a low content of the components, degrading the drug in particular the chlorides due the stage of processing by activated carbon with a conductivity of 10 µs or less, as well as to the product, obtained using said process and composition for delivery of active agents sensitive to the content of chlorides.EFFECT: group of inventions allows to reproducibly obtain sulfoalkyl esters of cyclodextrin with reduced chloride content and provides improved stability of the composition with active agents that are sensitive to chloride content.33 cl, 10 dwg, 13 tbl, 21 ex

Il-1 binding proteins // 2615173
FIELD: biotechnology.SUBSTANCE: present group of invention relates to biotechnology and immunology. Bispecifical binding protein is disclosed, which contains first polypeptide chain including two variable heavy chain domains of antibody and second polypeptide chain including two variable light chain domains of antibody (DVD-Ig). Disclosed protein binds human IL-1β and IL-1α. In addition recovered nucleic acid molecule, expression vector, host cell and method of producing binding protein under invention based on their using are disclosed. Besides pharmaceutical composition, methods of reducing activity of human IL-1 and method of treating patient from inflammatory disorder are presented.EFFECT: protein under present invention has neutralizing activity with respect to human IL-1β and IL-1α and thus it can find further application in therapy of diseases associated with IL-1.15 cl, 17 tbl, 4 ex
Production method for 3-[(phenylsulfenyl)methyl]pentane-2,4-dione showing a fungicidal activity // 2615155
FIELD: biotechnology.SUBSTANCE: invention relates to a method of producing 3-[(phenylsulfenyl) methyl] pentane-2.4-dione of formula (1) . The essence of the method is the interaction of the mixture of formaldehyde and thiophenol with 2.4-pentanedione involving the catalyst NiCl2⋅6H2O at the mole ratio of formaldehyde as follows: thiophenol: 2.4-pentanedione: NiCl2⋅6H2O=1:1:1:(0.03-0.07) in the mixture of solvents CHCl3-C2H5OH (1:1, vol.), at room temperature (~20°C) and atmospheric pressure for 6-8 h.EFFECT: obtained compounds have a fungicidal activity to micromycetes of phytopathogenic fungi Bipolaris sorokiniana, Fusarium oxysporum lesion, Rhizoctonia solani.2 cl, 2 tbl, 1 ex
ethod of producing perfluoro-3-methoxypropionyl fluoride // 2615148
FIELD: chemistry.SUBSTANCE: invention relates to a method of producing perfluoro-3-methoxypropionyl fluoride which is the initial product of perfluoro-3-methoxypropyl vinyl ester (monomer M-60MP) production, which provides increased frost resistance to its copolymers-fluororubbers due to the decrease of their glass transition temperature. The method consists in the electrochemical fluorination of methyl 3-methoxytetrafluorinepropionate in liquid anhydrous hydrogen fluoride, wherein triallylamine is used as the electrolyte additive in an amount from 1.0 to 10.0 wt % of the total electrolyte weight.EFFECT: method enables to obtain the end product with 60-65 percents of current output.1 tbl, 3 ex
ethod for organomagnesium oxanaluminoxanes production, binders and impregnating materials based thereon // 2615147
FIELD: chemistry.SUBSTANCE: method includes polyalcoxialuminoxanes interaction with magnesium acetylacetonate [CH3(O)CCH=C(CH3)O]2Mg in an organic solvent at a temperature of 20°C-70°C, followed by distilling off the solvent, first at atmospheric pressure and then under reduced pressure at a temperature up to 140°C. Binders and impregnating materials based on organomagnesium oxanaluminoxane are also proposed.EFFECT: invention provides production of organomagnesium oxanaluminoxanes that can be used as precursors of high-purity ceramic based on aluminium and magnesium oxides, and may have fiber-forming properties.2 cl, 3 dwg, 2 tbl, 2 ex

Self-delivered rnai compounds of reduced size // 2615143
FIELD: biotechnology.SUBSTANCE: invention relates to self-delivered interfering RNA (sd-RNA), which can be used in medicine. Self-delivered interfering sd-RNA contains leading strand and passenger strand, wherein sd-RNA contains double-stranded region and single-stranded region, where single-stranded region is located at 3'-end of leading strand, double-stranded region has length of 8–15 nucleotides, and single-stranded region has length of 4–12 nucleotides, at least 40 % of sd-RNA nucleotides are modified, wherein modifications are selected from group containing 5'-phosphorylation, phosphorothioate modification of frame, 2'-deoxy-, 2'F- and 2'O-methyl modification of ribose, hydrophobic modification of U and/or C, wherein hydrophobic modification is in position 4 or 5 U and/or C, at least two U and/or C include hydrophobic modification, selected from group consisting of metyl, octyl, thiophene, octyn-1-yl, ethynyl, pyridyl amide, isobutyl, phenyl, 4-pyridyl, 2-pyridyl, indolyl, butyl, naphthyl and imidazole modification; single-stranded region contains 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12 phosphorothioate modifications; and modifications include at least one 2'F- or 2'O-methyl modification; sd-RNA optionally contains at least one additional single stranded region and sd-RNA optionally contains cholesterol or long-chain alkylcholesterol analogue attached to 3'-end directly or by linker fragment.EFFECT: novel self-delivered interfering RNA and compositions based thereon effective for gene silencing.10 cl, 85 dwg, 1 tbl, 7 ex
ethod and device for heat recovery in plants for producing vinyl chloride monomer or in integrated plants for producing vcm/pvc // 2615141
FIELD: chemistry.SUBSTANCE: invention relates to the method for producing vinyl chloride by thermal cleavage of 1,2-dichloroethane in the complex to prepair vinyl chloride by distillation purification of 1,2-dichloroethane with, at least, one column of high boiling compounds, in which materials with a higher boiling point than 1,2-dichloroethane are removed, and by optionally associated plant for producing PVC. The said method comprises the steps of: (a) operating the column of the high boiling compounds at the column top temperature of 120-150°C and (b) applying of, at least, a portion of the overhead stream from the column of the high boiling compounds to obtain the heat energy used in the heat sinks of the installation component intended for the preparation of 1,2-dichloroethane and/or in the heat sinks of the installation component intended for the preparation of vinyl chloride and/or heat sink component of the installation downstream, designed to produce PVC with (c) applying a top stream for indirect heating heat sinks by application of, at least, a portion of the overhead stream from the column of the high boiling compounds to produce a low pressure steam and returning of the overhead stream to the column of the high boiling compounds with subsequent condensation with or without supercooling and application of the low pressure steam for heating the selected parts of the installation. Also it relates to the device for preparing vinyl chloride by thermal cracking of 1,2-dichloroethane in the complex for prepairing vinyl chloride by distillation purification of 1,2-dichloroethane and by optionally attached device for prepairing PVC. The said apparatus comprises the following elements: (A) at least, one column of the high-boiling compounds in the installation component for distillation purification of 1,2-dichloroethane, in which substances having a boiling point higher than of 1,2-dichloroethane are removed (B) at least, one heat exchanger, which is connected with the column of the high boiling compounds and which is supplied with, at least, a portion of the overhead stream from the column of the high boiling compounds for condensation and optional subcooling in it to get heat by the formation of low-pressure steam, and then to return to the column of the high boiling compounds and (C) at least, one heat sink in the installation component for the preparation of 1,2-dichloroethane and/or in the connected component of the installation for prepairing vinyl chloride and/or in the connected component of the installation for prepairing PVC, which serves low pressure steam obtained in the heat exchanger (B) for heating.EFFECT: significant improvement in the energy balance of the installations complex and the improvement of the method and device safety by allowing heat of the physically remote heat sinks.12 cl

Solid forms of nematocidal sulfonamides // 2615139
FIELD: chemistry.SUBSTANCE: invention relates to the field of organic chemistry, namely to polymorphous form A and polymorphous form TS 8-chloro-N - [(2-chloro-5-methoxyphenyl) sulfonyl] -6- (trifluoromethyl) imidazo [1,2- a] pyridine-2-carboxamide (compound 1).EFFECT: invention provides obtaining polymorphous forms of the compounds of nematicidal sulfonamides with different resistance in the compositions.2 cl, 1 dwg, 26 tbl, 23 ex
Compounds for metabolic syndrome treatment // 2615136
FIELD: pharmacy.SUBSTANCE: invention relates to new compounds of formula I .EFFECT: new compound of formula I are obtained, their application for metabolic syndrome, metabolic disease or metabolic disorders treatment is proposed.16 cl, 8 tbl, 37 ex, 8 dwg

Pyrrolidin-3-ylacetic acid derivative // 2615135
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula (1) , where R is a C1-6alkyl group, unsubstituted or containing 1–3 substitutes, selected from a group of substitutes A, C3-8cycloalkyl group, unsubstituted or containing 1–3 substitutes, selected from group of substitutes A, or C3-8cycloalkenyl group, unsubstituted or containing 1–3 substitutes, selected from a group of substitutes A, X denotes C1-6alkyl group, Y and Z are identical or differ from each other, and each of them is a halogen atom or C1-6alkyl group, unsubstituted or containing 1–3 substitutes, selected from a group of substitutes B, n equals 0 or 1, group of substitutes A consists of halogen atoms, and group of substitutes B consists of halogen atoms, having inhibitory effect on fractalkine-CX3CR1 pathway.EFFECT: disclosed is a pyrrolidin-3-yl acetic acid derivative.20 cl, 4 dwg, 5 tbl, 14 ex
ethod for producing furadonin // 2615132
FIELD: chemistry.SUBSTANCE: method of obtaining pharmacopoeia furadonina consists of dissolving technical furadonina heated to a temperature of 50±10°C dimethylformamide, followed by heating the reaction mass to a temperature of 100±5°C and held for 20÷40 minutes, the reaction mass is cooled and it was held for 1.5÷2.5 hours at 20±10°C. After soaking the paste is pressed onto a centrifuge, washed with isopropyl alcohol and purified water, and transferred to the drying which is carried out at a temperature of 65±10°C to a moisture content of not more than 7.5%.EFFECT: increased output of beta-chlorine-L-alanine of suitable quality.1 tbl

Zinc-lysine complex // 2615131
FIELD: hygiene.SUBSTANCE: invention relates to zinc-lysine complex of formula [Zn(C6H14N2O2)2Cl]+Cl-. Invention also discloses composition of personal hygiene mean, oral care composition, method of reducing sweating and body odor, method of destroying bacteria, method of producing zinc-lysine complex and its application.EFFECT: zinc-lysine complex possesses antibacterial and antiperspirant properties.24 cl, 1 dwg, 3 tbl, 2 ex

Heterocyclic compounds useful as pdk1 inhibitors // 2615130
FIELD: chemistry.SUBSTANCE: present invention relates to novel compounds of general formulae II, III, IV and V, where values of radicals are given in description, or pharmaceutically acceptable salts thereof, which can be used as PDK1 inhibitors.EFFECT: present invention also relates to pharmaceutical compositions based thereon and to methods of treating cancer, mediated by protein kinase PDK1.32 cl, 2 tbl, 445 ex

Organometallic compounds in solid form, method for its production and use // 2615128
FIELD: chemistry.SUBSTANCE: invention relates to the method for producing a solid organomagnesium precursor having the formula {Mg(OR')X}.a{MgX2}.b{Mg(OR')2}.c{R'OH}, where R' is selected from the hydrocarbon group, X is selected from the halide group, and a:b:c is in the range of 0.01-0.5:0.01-0.5:0.01-5. The method comprises the magnesium source contact with a solvating agent, an organohalide and an alcohol with obtaining a solid organomagnesium precursor. The solvating agent is selected from the group consisting of dimethyl ether, diethyl ether, dipropyl ether, diisopropyl ether, ethyl methyl ether, n-butyl ether, n-butyl ethyl ether, di-n-butyl ether, di-isobutyl ether, isbutyl methyl ether, isobutyl ethyl ether, dioxane, tetrahydrofuran, 2-methyltetrahydrofurane, tetrahydropyrane, and combinations thereof. The solid organomagnesium precursor, the method for obtaining the catalyst composition, the catalyst composition, the method for obtaining the catalyst system, the catalyst system and method for the polymerization and / or copolymerization of olefins are proposed as well.EFFECT: invention allows to simplify the method of obtaining the organomagnesium precursor which is used in manufacturing the catalyst for the polymerization of olefins, having high activity.43 cl, 1 dwg, 3 tbl, 3 ex
ethod of producing 4-[2-r-2-oxoethyl]-5-nitrobenzene-1,2-dicarboxylic acids // 2614979
FIELD: chemistry.SUBSTANCE: invention relates to a method of producing 4-[2-R-2-oxoethyl]-5-nitrobenzene-1,2-dicarboxylic acids of said general formula, where R = C6H5 or 4-CH3C6H4, or 4-OCH3C6H4, or 2-thienyl, which can be used as precursors for synthesis of biologically active substances and drugs. Method comprises heating substituted 4-nitro-5-(2-oxoethyl)phthalonitriles in a solution of sulphuric acid with weight ratio of 75–90 % at a temperature of 100–120 °C for 20–36 hours. After reaction obtained reaction mass is cooled, diluted with ten-fold excess cold water with ice, precipitate of 4-[2-R-2-oxoethyl]-5-nitrobenzene-1,2-dicarboxylic acid is filtered, washed with water, recrystallised from alcohol and dried on air.EFFECT: proposed method enables to obtain said compounds with sufficient degree of purity.1 cl, 4 ex

Crystalline forms of 1-(5'-(5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-3'h-spiro[azetidine-3,1'-isobenzofuran]-1-yl)-2-(methylsulfonyl)ethanone // 2614978
FIELD: chemistry.SUBSTANCE: invention relates to a crystalline form of A (S)-1-(5'-(5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-3'H-spiro[azetidine-3,1'-isobenzofuran]-1-yl)-2-(methylsulphonyl)ethanone.EFFECT: technical result is obtaining a crystalline form of A (S)-1-(5'-(5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-3'H-spiro[azetidine-3,1'-isobenzofuran]-1-yl)-2-(methylsulphonyl)ethanone, as well as a veterinary composition and a method of treating parasitic infection or infestation with parasites in an animal in need thereof is described.13 cl, 7 dwg, 5 tbl, 3 ex

Catalytic composition and process for dehydrogenation of butenes or mixtures of butanes and butenes to give 1,3-butadiene // 2614977
FIELD: chemistry.SUBSTANCE: invention relates to a catalyst composition and a method, wherein said composition is used for production of 1,3-butadiene of separate butenes or mixtures thereof or mixtures of butanes and butenes. Catalyst composition includes microspherical aluminium oxide, modified with silicon dioxide, and an active component. Active component contains platinum and/or platinum oxide in amount from 1 ppm to 500 ppm with respect to total weight of catalyst composition, gallium oxides, selected from Ga2O3 Ga2O and mixtures thereof, tin and/or tin oxides and oxides of alkaline and/or alkaline-earth metals. Also described is a method for dehydrogenation of reagents.EFFECT: technical result is obtaining active, non-toxic catalyst composition which exhibits function of thermal vector for compensating for endothermic nature of dehydrogenation reaction and overcomes critical aspects of industrial technologies.24 cl, 1 dwg, 2 tbl, 2 ex
Pesticide compositions and related methods // 2614976
FIELD: chemistry.SUBSTANCE: invention relates to a molecule of formula one, where R1 is H, F, Cl, Br or I; R2 is H, F, Cl, Br or I; R3 is H, F, Cl, Br or I; R4 is H, F, Cl, Br or I; R5 is H, F, Cl, Br or I; R6 is a (C1-C8)halogenalkyl; R7 is H; R8 is H; R9 is H; R10 is F, Cl, Br, I, (C1-C8)alkyl or halogen(C1-C8)alkyl; R11 is C(=O)N(R14)((C1-C8)alkylC(=O)R15); R12 is H; R13 is H; R14 is H; R15 is N(R16)(R17) or (C1-C8)alkyl-C(=O)N(R16)(R17); R16 is H; R17 is halogen(C1-C8)alkyl; X1 is CR12; X2 is CR13; X3 is CR9. Formula oneEFFECT: obtaining novel compounds which can be used against pests.9 cl, 3 tbl, 129 ex
ethod for praparing 1-phenyl-4-oxaspiro[2,4]heptane // 2614945
FIELD: pharmacology.SUBSTANCE: invention relates to the method for preparing 1-phenyl-4-oxaspiro[2.4]heptane (1), characterized in that styrol is reacted with γbutyrolactone and aluminium chloride (AlCl3), magnesium (Mg, powder) and catalyst Cp2ZrCl2 in a molar ratio of styrol: γ-butyrolactone:AlCl3:Mg:Cp2ZrCl2=10:15:(20-30):(10-14):(1.8-2.2), in tetrahydrofuran in the argon atmosphere at 20-22°C and under the atmospheric pressure for 6-10 hours. The yield of 1-phenyl-4-oxaspiro[2.4] heptane (1) is 78-92%.EFFECT: compound is of interest as a source of synthons for creating biologically active compounds for the medical and agricultural purposes, which can be used for the medicine synthesis, which exhibit antibacterial, antiviral, antiinflammatory, antifungal, analgesic properties.1 tbl, 1 ex

Animals different to human animal expressing antibodies with common light chain // 2614859
FIELD: biotechnology.SUBSTANCE: genetically modified mouse is described. The mouse expresses a repertoire of immunoglobulin light chains, characterized by a limited number of light chain variable domains. Also mice are described that express only one or more variable domains of an immunoglobulin light chain from a limited repertoire in their germline. Methods for production of variable sections of the mouse light chain, including variable sections of human light chain, and methods for producction of human variable sections suitable for use in multispecific binding proteins, such as bispecific antibodies.EFFECT: higher efficiency of compound application.31 cl, 9 dwg, 14 tbl, 10 ex
ethod for zinc dimethacrylate preparation // 2614766
FIELD: chemistry.SUBSTANCE: invention relates to methacrylic acid zinc salt - Zn dimethacrylate, which can be used as an activator in sulfur vulcanization systems with an accelerator for rubber compounds preparation, as well as biocides, intended for combating pathogenic microorganisms, for creation of differentvarious products with biocidal properties. The method comprises aqueous sodium hydroxide addition to methacrylic acid and water under cooling, at a molar ratio of 1:1, followed by vigorous stirring at a temperature not higher than 50°C, addition of zinc chloride aqueous solution to the resulting sodium salt of methacrylic acid by equal portions at a molar ratio of 2:1, at a temperature not higher than 40°C, formed product isolation by filtration, washing with water, squeezing and drying at a temperature of 100-110°C.EFFECT: simplified method due to hardware design simplicity, no need to apply high temperature and catalysts.2 ex
Analgesic peptide of sea anemone // 2614759
FIELD: biotechnology.SUBSTANCE: invention relates to biologically active peptide of sea anemone Metridium senile, having the following amino acid sequence H2N-Asnl-Ile2-Ile3-Val4-Gly5-Gly6-Cys7-Ile8-Lys9-Cys10-His11-Val12-Lys13-Asn14-Ala15-Ser16-Gly17-Arg18-Cys19-Val20-Arg21-Ile22-Val23-Gly24-Cys25-Gly26-Val27-Asp28-Lys29-Val30-Pro31-Asp32-Leu33-Phe34-Ser35-COOH. The peptide can be used as a medicament alone or in conjunction with other components to relieve pain conditions in humans and animals stipulated by participation of TRPA1 receptors, as well as for clarification of topology and molecular mechanisms of TRPA1 channels functioning, studying of TRPA1 channels distribution in living organisms, in test systems for detection and testing of new drugs against pain and/or inflammation, TRPA1 receptor agonists and antagonists, or for production of antibodies used for scientific and medical purposes.EFFECT: increase of analgesic effect by inhibiting the functional activity of ion channel TRPA1.10 dwg, 13 ex

Pharmaceutical composition based on β-modification of 2,3-bis-(hydroxymethyl)quinoxaline-n,n'-dioxide and method for obtaining thereof // 2614736
FIELD: chemistry.SUBSTANCE: group of inventions relates to medicine. Disclosed a pharmaceutical composition containing crystalline modification of β2,3-bis-(hydroxymethyl)quinoxaline-N,N'-dioxide, characterised by a number of diffraction peaks (d, Ǻ) and their intensity (Irel., %), and silver nanoparticles. Disclosed production process. Antimicrobial, antibacterial and bactericidal pharmaceutical composition, comprising crystalline β-modification of 2,3-bis-(hydroxymethyl)quinoxaline-N,N'-dioxide, characterised by a number of diffraction peaks (d, Ǻ) and their intensity (Irel., %), and silver nanoparticles, constitutes a light fluffy powder of yellowish to light-brown colour, non-odorous.EFFECT: disclosed the said pharmaceutical composition and method for obtaining thereof.7 cl, 6 dwg, 4 ex
ethod for 1,3-bis- and 1,4-bis(4,5-di[thiophen-3-yl]-1h-imidazol-2-yl)benzenes production // 2614447
FIELD: chemistry.SUBSTANCE: invention relates to the method for preparation of 1,3-bis- and 1,4-bis (4,5-di [thiophen-3-yl]-1H-imidazol-2-yl)benzenes of the general formula (1) , where R=CH3 (1a, 1c); R=Cl (1b, 1d), which comprises six-hour refluxing of the corresponding 1,2-ditieniletan-1,2-diones of formula (2) , where R=CH3 (2a); R=Cl (2b) with terephthalic or isophthalic aldehydes in acetic acid in the presence of a tenfold excess of ammonium acetate.EFFECT: compounds can be used for synthesis of photoswitchable structures for sensor technology, optical memory devices, photochromic fluorescent materials.4 ex
ethod for production of 1,1-difluoroethane // 2614442
FIELD: chemistry.SUBSTANCE: invention refers to a method for production of 1,1-difluoroethane including liquid-phase fluorination of vinyl chloride by hydrogen fluoride in presence of tetrachlorated tin, distillation of fluorination products in presence of anhydrous hydrogen fluoride with taking in light fraction hydrogen chloride, raw 1,1-difluoroethane and partially hydrogen fluoride with hydrogen fluoride content from 0.3 to 3 mol.% and organic products boiling away at temperature which is higher than that for 1,2-difluoroethane (not more than 1 mol.%); high-boiling organic products and the greater hydrogen fluoride quantity is returned to fluorination stage. Rectification of the obtained fraction is used to isolate hydrogen chloride in the light fraction and raw 1,1-difluoroethane in still fraction. Additional removal of vinyl chloride from the still fraction is carried out in gas phase at a temperature in the range from 150 to 250°C by means of contact with aluminum oxide based catalyst with components of the group including chromium, nickel or antimony with subsequent isolation of the target product.EFFECT: increased method efficiency.3 cl, 2 tbl, 8 ex
ethod of producing 1,2-benzisothiazolin-3-one // 2614424
FIELD: chemistry.SUBSTANCE: invention relates to production of 1,2-benzisothiazolin-3-one or its sodium salt. Method comprises steps (i) heating a mixture of sodium sulphide hydrate and N-methyl-2-pyrrolidone, (ii) distillation of water from mixture and, optionally, at least part of N-methyl-2-pyrrolidone, leaving sodium sulphide with depleted water content and, optionally, water and/or N-methyl-2-pyrrolidone, (iii) introduction of at least one benzamide, substituted in position 2, selected from a group, consisting of 2-chlorobenzamide, 2-fluorobenzamide, 2-nitrobenzamide, 2-cyanobenzamide and 2-C1-6 alkoxybenzamide with a branched or linear chain, in sodium sulphide with depleted water content to form a composition containing 2-mercaptobenzamide or its sodium salt, and (iv) of oxidative cyclisation of composition, containing 2-mercaptobenzamide or its sodium salt, by reaction with a reagent selected from a group consisting of aqueous hydrogen peroxide, MCPBA (meta-chloroperoxybenzoic acid), peracetic acid, perbenzoic acid and perphthalic acid.EFFECT: production of 1,2-benzisothiazolin-3-one and its sodium salt with good output and purity.3 cl, 8 ex
Catalyst and method for fischer-tropsch reaction implementation with application // 2614420
FIELD: chemistry.SUBSTANCE: complex cobalt salts catalyst for Fischer-Tropsch synthesis comprises cobalt particles, wherein cobalt phthalocyanine complex (C32H16N8Co) is selected as the cobalt complex salt, and 1-butyl-3-methylimidazolium tetrafluoroborate and 1-butyl-3-methylimidazolium bis (triftorboratsulfonil) imide ion liquids are selected as cobalt particle dispersant. The method of Fischer-Tropsch reaction is implemented in an autoclave at a temperature of 280°C, synthesis gas with a molar ratio H2/CO=2 pressure equal to 60 atm, while stirring the reaction mass which is a mixture of catalyst and ionic liquid. The reaction is carried out with perfluorodecalin addition to the reaction mass at a mass ratio of - catalyst:ionic liquid:perfluorodecalin = 0.04:1:1.EFFECT: increased catalytic activity and productivity of the Fischer-Tropsch synthesis process.2 cl, 1 tbl, 3 ex
1,6-diazabicyclo [3,2,1] octane-7-ona derivatives and use thereof for treating bacterial infections // 2614418
FIELD: chemistry.SUBSTANCE: invention relates to a heterocyclic compound of formula (I), or to stereoisomer thereof, or to a pharmaceutically acceptable salt thereof, where R1 is SO3M; M is a hydrogen or Na; R2 is (a) hydrogen or (b) (CH2)n-R3; n equals 0 or 1; R3 is (a) hydrogen, (b) C1-C6 alkyl, not necessarily substituted with one or a few substituents, independently selected from (a) 4-10-membered saturated or unsaturated heterocyclyl containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulfur, not necessarily substituted with one or more substituents, independently selected from OH, CN, NHCOCF3, NH2, C(=NH)NH2, oxo, C1-C6 alkyl, C6H5OH or pyrrolidine, (b) NH2 or (c) NHC(=NH)NH2,(c) 4-6-membered heterocyclyl containing 1 or 2 nitrogen atoms, not necessarily substituted with one or a few substituents, independently selected from CN or CONH2. The invention also relates to a pharmaceutical composition based on the compound of formula (I), to a method of preventing or treating bacterial infection, based on injecting one compound of formula (I), as well as in a combination with another antibacterial agent. .EFFECT: obtaining novel heterocyclic compounds, useful in the treatment of bacterial infections.18 cl, 4 tbl, 51 ex
Ruthenium complexes containing paracyclophane and carbonyl ligands and their use as catalysts // 2614415
FIELD: chemistry.SUBSTANCE: invention relates to the ruthenium complexes of formulas (1a), (1b), (1c) or (1d): [Ru Hal2 L CO S] (1a); [Ru2 Hal4 L2 (CO)2 ] (1b); [Ru2 Hal4 L2 CO] (1c); [Ru Hal2 L (CO)2 ] (1d). In these formulas Hal represents a halogen ligand, L is a substituted or an unsubstituted paracyclophane ligand of the formula (2): ,where X1 X2 represent bonding groups including linear, branched, or cyclic structures where the link is formed via 2, 3 or 4 carbon atoms, each group Y1 Y2 Y3 Y4 independently from each other is selected from the group including an unsubstituted C1-C20 alkyl, replaced by C1-C20 alkyl, an unsubstituted C3-C10cycloalkyl, substituted C3-C10 cycloalkyl, unsubstituted C6-C20 aryl, substituted C6-C20 aryl, unsubstituted C5-C20 heteroaryl and substituted C5-C20 heteroaryl; or Y1 Y2 and/or Y3 Y4 are connected so that the ring structure is formed, that includes the phosphorus atom, each of the groups Z1, Z2 and Z3 is the same or different, and they are selected from the group consisting of unsubstituted branched C1-C30 alkyl, substituted branched C1-C30 alkyl, unsubstituted linear C1-C30alkyl, substituted linear C1-C30 alkyl, unsubstituted C6-C20 aryl, substituted C6-C20 aryl, benzyl, substituted benzyl, halogen, hydroxyl, -O-(C1-C30 alkyl), -OSi(C1-C30 alkyl), -OCH2Ph, carbonyl, carboxyl, anhydride, methacrylate, epoxide, vinyl, nitrile, sulfate, sulfonyl, mercapto group, sulfide, amino group, amine, imine, amide and imide; a, b, C, d, e and f represent integers of 0 or 1 and a+b+c+d+e+f = from 0 to 6, CO represents a carbonyl ligand; and S represents a ligand solvent. Also methods of producing such complexes are proposed.EFFECT: ruthenium complexes of the formula are useful in a variety of chemical reactions, such as those of isomerization, hydrogenation, hydrogen transfer, hydrogenation, hydroformylation or carbonylation.16 cl, 8 ex
Continuous process for alkylation of cyclic tertiary amine // 2614412
FIELD: chemistry.SUBSTANCE: invention relates to the continuous process for alkylation of tertiary amines and, in particular, to the continuous process for quaternizing cyclic tertiary amines.EFFECT: process provides cyclic salts of quaternary ammonium with a high conversion value and a high purity value.19 cl, 1 tbl, 6 ex

ethod for catalytic epoxidation // 2614409
FIELD: chemistry.SUBSTANCE: invention relates to a method of producing epoxide, which includes: feeding components to form a reaction mixture, wherein components comprise: olefin, having maximum solubility in water at 20 °C from 0.01 to 100 g/l; hydrogen peroxide; ions of alkaline-earth metal, containing metal ions formed from salts of alkali-earth metal and acid with pKa level equal to 15 or less; water-soluble manganese complex; buffer component; as well as water; and reaction of olefin with hydrogen peroxide in reaction mixture. Manganese complex includes one or more compounds, selected from a group consisting of: mononuclear complex formula (I): [LMnXm]Y (I), binuclear complex of formula (II): [LMn(μ-X)mMnL]Yn (II) or polynuclear complex of formula (III): [LnMnn(μ-X)m]Yn (III), where Mn denotes a manganese atom; L or each of L independently is a polydentate ligand, each X is independently a coordination particle and each μ-X independently represents a bridge coordination particle, where Y is a non-coordinated counterion, and m assumes values from 1 to 4, and value of n ranges from 1 to 2.EFFECT: increased number of turns of catalyst (TON) due to higher efficiency of using an oxidising agent.15 cl, 1 dwg, 5 tbl, 3 ex

Phosphorus amidate derivatives of 5-fluoro-2'-deoxyuridine applicable for treating cancer // 2614406
FIELD: pharmaceutics.SUBSTANCE: invention relates to compounds of formula (I) used in oncology, their pharmaceutically acceptable salts and compositions based on: where Ar is phenyl or naphthyl and optionally substituted with -NO2; R3 is selected from benzyl, methyl, ethyl, n-propyl, n-butyl, n-pentyl, n-hexyl, isopropyl, cyclohexyl, 2-indanyl, 3,3-dimethyl-1-butyl, cyclobutyl, cyclopropylmethyl, cyclopentyl, tetrahydropyranyl and 2,2-dimethylpropyl; R4 is H atom; R1 and R2 are selected from H atom and C1-C16alkyl, optionally substituted with phenyl, or one of R1 and R2 has C3-alkylene link connected to N atom so, that total number of ring atoms, including N and C atoms, is equal to 5 atoms, atom H, connected with N atom, is absent and one from R1 and R2 comprises atom H or C1-C16 alkyl; or pharmaceutically acceptable salt of compound of formula I, if said compound is not compound containing in combination unsubstituted phenyl as Ar, CH3 as R3, H as R4, H as one of R1 and R2 and CH3 as one of R1 and R2.EFFECT: new effective anticancer agent and method of its production are presented.67 cl, 11 dwg, 8 tbl, 8 ex
ethod for preparation of collagen product // 2614273
FIELD: pharmacy.SUBSTANCE: invention refers to processing and cosmetics industris, namely to a method for production of a collagen product with the following characteristics: reception of skins of freshwater fish such as silver carp, carp, grass carp, mirror carp, manual or machine cleaning from scale, muscle tissue, fins and mechanical impurities, washing for 30 minutes in drum type machines with a solution of soap and then in water - to remove residual soap, the rinsed skins are subjected to peroxide and alkaline treatment, for which they are poured with a mixture of hydrogen peroxide with mass concentration of 3% and sodium hydroxide with mass concentration of 3 % and kept at 20-25°C for 1.5-2 hours and liquor ratio of 1:4, the treated skins are washed with flowing water at 8-12°C for 10-15 min, then the skins are poured with citric acid solution with mass concentration of 6% and kept for 6 days, the resulting mass is homogenized, packaged in polyethylene and stored at 0…+4°C for° max. 4 months.EFFECT: increase of collagen product quality indicators: increase in collagen output, improved organoleptic properties, reduced complexity and cost by reducing the number of process steps and reagents, intensification of the pre-treatment process and raw materials degreasing.1 tbl, 2 ex

Alpha-v beta-8-binding antibodies // 2614252
FIELD: pharmacy.SUBSTANCE: antibodies with high affinity for β8-subunit αvβ8 proposed. Pharmaceutical composition comprising such antibodies, and methods of their application are also described. The proposed group of inventions can be used in medicine.EFFECT: improved antibody properties.23 cl, 14 dwg, 19 ex
ethod for substituted quinolines production from aniline, 1,2-diols and ccl4 under iron catalysts // 2614251
FIELD: chemistry.SUBSTANCE: invention relates to a method for preparation of substituted quinolines of the formula shown below , where R1=CH3, R2 and R3=H; R1=CH2CH3, R2=CH3 and R3=H; R1=CH2CH3, R2=H and R3=CH3; R1=CH2CH2CH3, R2=CH2CH3 and R3=H; X=H, o-CH3, "м"-CH3, "п"-CH3, o-C2H5, o-Cl, "м"-Cl, "п"-Cl, "п"-OMe, o-OH, from aniline, wherein the substituted anilines of formula XC6H4NH2 where X is as defined above, is reacted with 1,2-diols (1,2-ethylene glycol, 1,2-propanediol or 1,2-butanediol) and CCl4 in the presence of a catalyst selected from FeCl3⋅6H2O, FeCl3, FeCl2⋅4H2O, Fe(C5H5)2, Fe(acac)3, Fe(OAc)2 and Fe2(CO)9, at a molar ratio [catalyst]:[aniline]:[CCl4]:[1,2-diol] = 1:100: 200:400, at 150 °C for 8 hours.EFFECT: process for preparation of quinoline derivatives that are raw materials for corrosion inhibitors, dyes and medicines production from available initial reactants.1 tbl, 35 ex
ethod for methyl n-[3,4-dialkyl-5-(n-methoxy-n-oxoalkyl)-2-furyl] alkanoates production // 2614250
FIELD: chemistry.SUBSTANCE: invention relates to a method for methyl n-[3,4-dialkyl-5-(n-methoxy-n-oxoalkyl)-2-furyl]alkanoates production by the general formula where R = C2H5, C3H7, C4H9; R'=(CH2)nCOOCH3, n=5, 6, by reaction of dialkyl acetylenes of the general formula R-C≡C-R, where R=C2H5, C3H7, C4H9, with carboxylic acid esters in the presence of magnesium (Mg, powder) and Cp2TiCl2 catalyst with methyl esters α,ω-dicarboxylic acids CH3CO2(CH2)nCO2CH3, where n=5, 6, at the molar ratio of RC≡CR : CH3CO2(CH2)nCO2CH3:EtAlCl2 : Mg:Cp2TiCl2 = 10:20(50-70):40:(1.8-2.2) in tetrahydrofuran under argon atmosphere at 60°C and atmospheric pressure during 4-8. Methyl n-[3,4-dialkyl-5-(n-methoxy-n-oxoalkyl)-2-furyl]alkanoates (1) yield is 54-76%.EFFECT: compound are important as initial synthons for biologically active compounds creation for medical and agricultural purposes, exhibiting antibacterial, antiviral, anti-inflammatory, antifungal, antitumor, analgesic, anticonvulsant properties.1 tbl, 1 ex

ethod for trimethyl substituted furodihydroquinolines synthesis // 2614248
FIELD: chemistry.SUBSTANCE: invention relates to a method for 7,7,9-trimethyl-6,7-dihydro-furo[3,2-ƒ]quinoline synthesis, comprising the 5-aminobenzofuran condensation with acetone in the presence of n-toluenesulphonic acid and magnesium perchlorate at a temperature of 70-125°C in an autoclave. At that, 5-aminobenzofuran is obtained by a sequence of steps consisting of: a - n-anisidine acylation with acetic anhydride to give N-(4-methoxyphenyl)acetamide; b - N-(4-methoxyphenyl)acetamide obtained in step interaction with chloroacetyl chloride to give N-[3-(chloroacetyl)-4-hydroxyphenyl]acetamide; c - dihydrofurane cycle circuit closure by treating the product obtained in step b by sodium acetate and subsequent intermediate reduction without isolation from the reaction mixture by sodium borohydride to yield N-(3-hydroxy-2,3-dihydro-1-benzofuran-5-yl)acetamide; d - dehydration of the product obtained in step c by treatment with n-toluenesulphonic acid and magnesium perchlorate to yield N-1-benzofuran-5-yl acetamide; e - acidic hydrolysis of the product obtained in step d to yield 5-aminobenzofurane. The method may be used as the basis for synthesis of various derivatives of furodihydroquinolines (FDHQ) trimethyl substituted by quinoline ring, that are of practical interest as potential sensitizers for application in PUVA-treatment of skin diseases, and they may be used in various fields of technology as antioxidants and antiozonants .EFFECT: simplification and cheapening of the desired product obtaining process and increase of its total output compared with the prototype.2 dwg, 2 ex

ethod of producing enantiomerically pure (s)-amino acids on basis of [(s)-bpb-gly]ni(ii) complex, directly bonded with fullerene core through α-carbon atom in form of chiral (f,ta) and (f,tc) 1,4-adducts of [60]fullerene // 2614247
FIELD: chemistry.SUBSTANCE: invention relates to a method for stereoselective synthesis of (S)-α-fullerenylglycine, wherein α-carbon atom of an acid is directly bonded with a fullerene core, in form of complex of Ni(II) of type of Schiff base with an auxiliary [(S)-BPB] ligand in form of chiral (f,tA) and (f,tC) 1,4-adducts of formula (I). Method includes steps A–E. Step A comprises modifying an initial amino acid by its incorporation in form of a Schiff base into coordination sphere of nickel complex with an auxiliary chiral ligand ((S)-2N-(N'-benzylprolyl)aminobenzophenone) [(S)-BPB-Gly]Ni(II). Step B comprises deprotonation of amino acid fragment of obtained complex. Step C comprises stereoselective reaction of anionic (deprotonated) complex with fullerene to form fullerene carbanion. Step D comprises reaction of fullerene carbanion with an electrophile, such as allyl- or benzyl halide, with formation of diastereomeric mixture of target fullerene (f,tA) and (f,tC) 1,4-adducts, containing (S)-α-amino acid fragment, directly bonded with fullerene core through α-carbon atom, in form of Schiff base in coordination sphere of Ni(II). Step E comprises separating and cleaning fullerene-containing adducts by column chromatography on silica gel to obtain a mixture of target fullerene (f,tA) and (f,tC) 1,4-adducts, containing (S)-α-amino acid fragment in coordination sphere of Ni(II). Invention also relates to a mixture of diastereomers, consisting of (f,tA) and (f,tC) 1,4-adducts, and optically pure (f,tA) and (f,tC) adducts.EFFECT: method enables stereoselective synthesis fullerenylglycine derivative having (S)-configuration of α-amino acid stereocentre.8 cl, 1 dwg, 6 ex (I)
 
2551195.
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