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Method of polyolefin composition nucleation by acetal compounds |
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IPC classes for russian patent Method of polyolefin composition nucleation by acetal compounds (RU 2348637):
Polymer composition / 2186799
The invention relates to a non-flammable polymer compositions of cold hardening filler in the form of hollow microspheres intended for local hardening of structures in the areas of installation fasteners, sealing the ends and filling voids in the parts made of composite materials, including repairs
Method of obtaining epotilone derivatives / 2343155
Method ensures carrying out aldole condensation in presence of epoxide mesilate and tosilate, using auxiliary chiral sultamic group as carboxyl- protecting group, as a result, reduction and oxidation stages, requiring extra time, before carrying out final stage of macrolactonisation are excluded. Introduction of epoxidic group at early stages of method allows also excluding stage of epoxilation of more complex intermediate compounds at further stages of process.
New tetracyclic compounds containing heteroatom, used as selective modulators of oestrogen receptors / 2331645
Invention pertains to new tetracyclic compounds containing a heteroatom. The compounds can be used in treating and/or prevention of disorders, associated with oestrogen depletion, such as hot flash, vaginal dryness, osteopenia and osteoporosis; sensitive cancerous diseases hormone and hyperplasia of the lacteal gland, endometrium, cervix uteri and prostate; endometriosis, uterus fibrosis and osteoarthritis, and as contraceptive agents, used either separately or combined with progestogen or a progestogen antagonist.
Analogs of himbacin, their using and pharmaceutical composition based on thereof possessing property of thrombin receptor antagonist / 2319704
Invention relates to heterocycle-substituted tricyclic compounds of the formula (I): or their pharmaceutically acceptable salts wherein R means hydrogen atom; R1 and R2 are chosen independently from group comprising hydrogen atom or alkyl comprising 1-6 carbon atoms; R3 means hydrogen atom; n1 and n2 = 0-3 independently under condition that they both do not mean 0; Het means pyridyl wherein pyridyl is added to B through cyclic carbon atom and it comprises from 1 to 4 substitutes (W) chosen independently from group comprising -NR4R5, -NHCOR26, -NHSO2R16; R21 means aryl and R21 means heteroaryl wherein heteroaryl represents furyl, thienyl, pyridyl, thiazolyl, pyrrolidinyl, azethidinyl; R4 and R5 mean hydrogen atom or alkyl comprising 1-6 carbon atoms, or R4 and R5 mean in common -(CH2)3-, -(CH2)4-, -(CH2)5- or -(CH2)2NR7-(CH2)2- wherein R7 means hydrogen atom or alkyl comprising 1-6 carbon atoms; R8, R, R10 and R11 mean hydrogen atom; B means -(CH2)n4CR12=CR12a(CH2)n5 wherein n4 and n5 = 0-2 independently; R12 and R12a are chosen independently from group comprising hydrogen atom or alkyl comprising 1-6 carbon atoms; R21 means from 1 to 3 substitutes chosen independently from group comprising hydrogen atom, trifluoromethyl, trifluoromethoxy, halogen atom, cyano, alkyl comprising 1-6 carbon atoms, alkoxy group comprising 1-6 carbon atoms, or -CR29(=NOR28); R22 means -COR23, -S(O)R31, -S(O)2R31 or -COOR27; R23 means cycloalkyl comprising 3-7 carbon atoms, (C3-C7)-cycloalkyl-(C1-C6)-alkyl, cycloalkyl comprising 3-7 carbon atoms containing from 1 to 3 substitutes chosen from group comprising halogen atom, (C1-C3)-alkoxy-(C1-C3)-alkyl, hydroxy group and alkoxy group comprising 1-6 carbon atoms, aryl, aryl-(C2-C6)-alkyl; R27 means alkyl comprising 1-6 carbon atoms, phenyl or benzyl; R28 and R29 are chosen independently from group comprising hydrogen atom or alkyl comprising 1-6 carbon atoms; R31 means alkyl comprising 1-6 carbon atoms, halogenalkyl comprising 1-6 carbon atoms, aryl, aryl-(C1-C6)-alkyl. Also, invention relates to pharmaceutical compositions containing these substances and their using for preparing a drug used in treatment of thrombosis, atherosclerosis, restenosis, hypertension, stenocardia, arrhythmia, heart failure and cancer.
Azaheterocycles, combinatory library, focused library, pharmaceutical composition and method for preparing (variants) / 2318818
Invention relates to novel azaheterocycles of the general formula (I): possessing inhibitory effect on activity of tyrosine kinase and can be used in treatment of different diseases mediated by these receptors. In compound of the general formula (1) W represents azaheterocycle comprising 6-13 atoms that can be optionally annelated with at least one (C5-C7)-carbocycle and/or possibly annelated with heterocycle comprising 4-10 atoms in ring and comprising at least one heteroatom chosen from oxygen (O), sulfur (S) or nitrogen (N) atom; Ra 1 represents a substitute of amino group but not hydrogen atom, such as substituted (C1-C6)-alkyl, possibly substituted aryl and possibly substituted 5-10-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; Rb represents carbamoyl group -C(O)NHRa wherein Ra represents a substitute of amino group but not hydrogen atom, such as possibly substituted alkyl, possibly substituted aryl, possibly substituted 5-10-membered heterocyclyc comprising at least one heteroatom chosen from O, S or N; Rc represents a substitute of cyclic system, such as possibly substituted (C1-C6)-alkyl, possibly substituted aryl and possibly substituted 5-6-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; or Rb and Rc form in common aminocyanomethylene group [(=C(NH2)CN], or their pharmaceutically acceptable salts. Also, invention relates to methods for synthesis of these compounds (variants), a pharmaceutical composition, combinatory and focused libraries.
C-glycoside derivatives and their salts / 2317288
Invention relates to novel compounds representing C-glycoside derivatives and their salts of the formula: wherein ring A represents (1) benzene ring; (2) five- or six-membered monocyclic heteroaryl ring comprising 1, 2 or 4 heteroatoms chosen from nitrogen (N) and sulfur (S) atoms but with exception of tetrazoles, or (3) unsaturated nine-membered bicyclic heterocycle comprising 1 heteroatom representing oxygen atom (O); ring B represents (1) unsaturated eight-nine-membered bicyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O; (2) saturated or unsaturated five- or six-membered monocyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O; (3) unsaturated nine-membered bicyclic carbocycle, or (4) benzene ring; X represents a bond or lower alkylene wherein values for ring A, ring B and X correlate so manner that (1) when ring A represents benzene ring then ring B is not benzene ring, or (2) when ring A represents benzene ring and ring B represents unsaturated eight-nine-membered bicyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O and comprising benzene ring or unsaturated nine-membered bicyclic carbocycle comprising benzene ring then X is bound to ring B in moiety distinct from benzene ring comprised in ring B; each among R1-R4 represents separately hydrogen atom, -C(=O)-lower alkyl or lower alkylene-aryl; each R5-R11 represents separately hydrogen atom, lower alkyl, halogen atom, -OH, =O, -NH2, halogen-substituted lower alkyl-sulfonyl, phenyl, saturated six-membered monocyclic heterocycle comprising 1 or 2 heteroatoms chosen from N and O, lower alkylene-OH, lower alkyl, -COOH, -CN, -C(=O)-O-lower alkyl, -O-lower alkyl, -O-cycloalkyl, -O-lower alkylene-OH, -O-lower alkylene-O-lower alkyl, -O-lower alkylene-COOH, -O-lower alkylene-C(=O)-O-lower alkyl, -O-lower alkylene-C(=O)-NH2, -O-lower alkylene-C(=O)-N-(lower alkyl)2, -O-lower alkylene-CH(OH)-CH2(OH), -O-lower alkylene-NH, -O-lower alkylene-NH-lower alkyl, -O-lower alkylene-N-(lower alkyl)2, -O-lower alkylene-NH-C(=O)-lower alkyl, -NH-lower alkyl, -N-(lower alkyl)2, -NH-lower alkylene-OH or NH-C(=O)-lower alkyl. Indicated derivatives can be used as inhibitor of co-transporter of Na+-glucose and especially as a therapeutic and/or prophylactic agent in diabetes mellitus, such as insulin-dependent diabetes mellitus (diabetes mellitus 1 type) and non-insulin-dependent diabetes mellitus (diabetes mellitus 2 type), and in diseases associated with diabetes mellitus, such as insulin-resistant diseases and obesity.
Tetracyclic heterocompounds as estrogen receptor modulating agents / 2305099
Invention relates to novel tetracyclic heterocompounds of the formula (I): wherein X, Y, Z, R1 - R4, n and m has values given in the invention description and used as selective modulating agents for estrogen receptors. Also, invention relates to a method for synthesis of these compounds and pharmaceutical compositions comprising thereof, and their using in treatment and/or prophylaxis of disorders mediated by one or more estrogen receptors. Proposed compounds are useful in treatment and/or prophylaxis of disorders associated with depleting estrogen and comprising such disorders as rush of blood, vaginal dryness, osteopenia and osteoporosis, hormone-dependent cancer and hyperplasia of breast, endometrium, uterus cervix and prostate, endometriosis, uterus fibroma, osteoarthritis that can be used as contraceptive agents both separately and in combination with progestogen or progestogenous antagonist.
Method for isolating epotilons from reaction mixture and desorption from synthetic resin (variants), using low-polar or nonpolar solvent for realization of method / 2285007
Invention relates to a method for isolation of epotilons used in medicine in treatment of cancer diseases. Method for desorption of epotilons A, B, D and/or E from synthetic resin is based on using low-polar or nonpolar solvent chosen from the group comprising (lower)-alkyl halides and aromatic solvents, or mixture of two or more amount of such solvents wherein prefix "(lower)" means that radical comprises up to 7 carbon atoms. Used aromatic solvent is chosen from the group including naphthalene, benzene or naphthalene and benzene substituted with one or some substitutes chosen from the following group: (lower)-alkyl, (lower)-alkoxy-group, halogen atom, nitro-group and (lower)-alkoxy-(lower)-alkyl wherein prefix "(lower)" means that radical comprises up to 7 carbon atoms. Solvent is removed to the required level but up to preparing a dry residue preferably. If necessary, residue is dissolved in mixture alcohol/hydrocarbon in the corresponding volume ratio. Alcoholic phase is evaporated until dry and then alcoholic extract is crystallized from mixture alcohol and hydrocarbon. Then formed crystallized product is dissolved in mixture nitrile/water but preferably in mixture acetonitrile/water taken in the ratio = 2:3 (vol./vol.). Formed solution is applied on column (if necessary, after separation for some distillates) for preparative chromatography in reversed phase followed by elution with mixture nitrile/water, removing nitrile and extraction of an aqueous phase with ester. Ester extract is evaporated and formed product is subjected for crystallization. Method for preparing epotilons A, B, D and/or E from resin or reaction mixture involves the following steps: (a) desorption of epotilons with low-polar or nonpolar solvent chosen from the group including (lower)-alkyl halides and aromatic solvents, or mixture of two or more amount of such solvents being the desorption step can be repeated up to achievement of the more complete desorption; (b) removal of solvent used in desorption from formed solutions by evaporation; (c) optional crystallization of epotilon(s) after desorption and first of all for crystallization of epotilon B by addition of mixture of alcohol with hydrocarbon and the following evaporation of alcoholic phase until dry and crystallization of epotilon B from the corresponding mixture of solvents; (d) (obligatory step) separation of epotilons by method of chromatography in reversed phase and the following dissolving a residue obtained in previous step in suitable solvent, elution with mixture nitrile/water and removing nitrile from epotilon-containing fractions by evaporation. If necessary, water remained with epotilon is extracted with ester followed by evaporation of epotilon-containing ester phase until dry; (e) optional purification by adsorption chromatography method, and final recrystallization of purified epotilon from corresponding solvents or mixture of solvents. If necessary, in this process between each step formed solutions or suspensions are concentrated, and/or liquid or solid components are separated of one another. Separation of epotilons A and B is carried out by chromatography method based on a mobile layer modeling. Invention provides simplifying methods for preparing large amounts of epotilons for satisfying requirement in these agents.
Crystals of taxane derivatives and method for their preparing / 2284328
Invention relates to a novel crystalline form of (1S,2S,3R,4S,5R,8R,9S,10R,13S)-4-acetoxy-2-benzoyloxy-9,10-[(1S)-2-(dimethylamino)ethylideneoxy]-5,20-epoxy-1-hydroxytax-11-ene-13-yl-(2R,3S)-3-(tert.-butoxycarbonylamino)-3-(3-fluoro-2-pyridyl)-2-hydroxypropionate that shows the diffraction picture of roentgen rays in powder with characteristic peaks at diffraction angles (θ)= 6.2o, 10.3o, 10.7, 11.4o and 12.0, and a method for its preparing. Method involves carrying out the crystallization step by using organic solvent chosen from group consisting of ketone type solvent, nitrile solvent type and their mixture, or mixture of said solvent and water. Also, invention relates to an antitumor agent based on the prepared crystalline form. Invention provides the stable quality of a medicinal agent based on its lower hygroscopicity.
Method for preparing 1,11-dialkyl-3,5-dihydrofuro-[2',3':3,4]-cyclohepta[c]isochromens / 2282633
Invention relates to a method for synthesis of new compounds, namely, 1,11-dialkyl-3,5-dihydrofuro-[2',3':3,4]-cyclohepta[c]isochromens of the formula: (Ia-f): wherein (Ia): R means hydrogen atom (H); R1 means hydrogen atom (H); (Ib): R means bromine atom (Br); R1 means hydrogen atom (H); (Ic): R means chlorine atom (Cl); R1 means hydrogen atom (H); (Id): R means hydrogen atom (H); R1 means bromine atom (Br): (Ie): R means hydrogen atom (H); R1 means chlorine atom (Cl); (If): R means methoxy-group (-OCH3); R1 means hydrogen atom. Method involves formation of condensed tetracyclic system as result of the successive recyclization reactions of furan ring of derivatives of 2-bis-(5-methyl-2-furylmethyl)phenylmethanol and the secondary cyclization of formed isochromen ketone in boiling of solution containing derivatives of 2-bis-(5-methyl-2-furylmethyl)phenylmethanol of the formula: in ethanol medium in the presence of hydrogen chloride alcoholic solution for 15-40 min. Invention provides synthesis of new derivatives of isochromens possessing the potential anti-inflammatory activity.
Method for preparing derivatives of baccatin iii / 2264394
Invention relates to a novel method for preparing 14β-hydroxy-1,4-carbonate-desacetylbaccatin III and intermediate substances used in preparing new derivatives of taxane and possessing an antitumor activity. Method involves the following stages: a) protection of hydroxyls at positions 7 and 10 in 10-desacetylbaccatin III wherein R and R1 are taken among hydrogen atom, (C1-C10)-alkyl or aryl, (C1-C10)-alkyl- or aryl-carbonyl, trichloroacetyl, (C1-C4)-trialkylsilyl; preferably, when R and R1 are similar then they represent trichloroacetyl; when they are different then, preferably, R represents trichloroacetyl and R1 represents acetyl; or R represents triethyl or trimethylsilyl and R1 represents acetyl; b) two-stage oxidation to yield a derivative oxidized to carbonyl at position 13 and hydroxylated at position 14; c) carboxylation of vicinal hydroxyls at positions 1 and 14 to yield 1,14-carbonate derivative; d) reduction of carbonyl at position 13; e) removal of protective groups at positions 7 and 10. Also, invention relates to intermediate substances. Invention provides preparing intermediate substances used in synthesis of taxane.
Hexahydrofuro[2,3-b]furan-3-yl-n-{3-[(1,3-benzodioxol-5- yl- sulfonyl)(isobu tyl)amino]-1-benzyl-2-hydroxypropyl}carbamate, pharmaceutical composition based on thereof, methods for inhibition and method for treatment / 2247123
Invention relates to new bis-tetrahydrofuranbenzodioxolyl sulfonamide compounds of the formula (I): , its salts, stereoisomers and racemates that are effective inhibitors of protease activity. Also, invention relates to pharmaceutical preparations, methods for inhibition of retrovirus proteases, in particular, to resistant retrovirus proteases, to many drugs, methods for treatment and prophylaxis of infection or disease associated with retrovirus infection in mammals and to methods for inhibition of retrovirus replication. Invention provides preparing new derivatives of bis-tetrahydrofuranbenzodioxalyl sulfonamides eliciting the valuable pharmaceutical properties.
Taxane pentacyclic compound and antitumor agents based on thereof / 2257387
Invention relates to a new pentacyclic compound derivative of taxane represented by the formula:
Method for preparing derivatives of baccatin iii / 2264394
Invention relates to a novel method for preparing 14β-hydroxy-1,4-carbonate-desacetylbaccatin III and intermediate substances used in preparing new derivatives of taxane and possessing an antitumor activity. Method involves the following stages: a) protection of hydroxyls at positions 7 and 10 in 10-desacetylbaccatin III wherein R and R1 are taken among hydrogen atom, (C1-C10)-alkyl or aryl, (C1-C10)-alkyl- or aryl-carbonyl, trichloroacetyl, (C1-C4)-trialkylsilyl; preferably, when R and R1 are similar then they represent trichloroacetyl; when they are different then, preferably, R represents trichloroacetyl and R1 represents acetyl; or R represents triethyl or trimethylsilyl and R1 represents acetyl; b) two-stage oxidation to yield a derivative oxidized to carbonyl at position 13 and hydroxylated at position 14; c) carboxylation of vicinal hydroxyls at positions 1 and 14 to yield 1,14-carbonate derivative; d) reduction of carbonyl at position 13; e) removal of protective groups at positions 7 and 10. Also, invention relates to intermediate substances. Invention provides preparing intermediate substances used in synthesis of taxane.
Method for preparing 1,11-dialkyl-3,5-dihydrofuro-[2',3':3,4]-cyclohepta[c]isochromens / 2282633
Invention relates to a method for synthesis of new compounds, namely, 1,11-dialkyl-3,5-dihydrofuro-[2',3':3,4]-cyclohepta[c]isochromens of the formula: (Ia-f): wherein (Ia): R means hydrogen atom (H); R1 means hydrogen atom (H); (Ib): R means bromine atom (Br); R1 means hydrogen atom (H); (Ic): R means chlorine atom (Cl); R1 means hydrogen atom (H); (Id): R means hydrogen atom (H); R1 means bromine atom (Br): (Ie): R means hydrogen atom (H); R1 means chlorine atom (Cl); (If): R means methoxy-group (-OCH3); R1 means hydrogen atom. Method involves formation of condensed tetracyclic system as result of the successive recyclization reactions of furan ring of derivatives of 2-bis-(5-methyl-2-furylmethyl)phenylmethanol and the secondary cyclization of formed isochromen ketone in boiling of solution containing derivatives of 2-bis-(5-methyl-2-furylmethyl)phenylmethanol of the formula: in ethanol medium in the presence of hydrogen chloride alcoholic solution for 15-40 min. Invention provides synthesis of new derivatives of isochromens possessing the potential anti-inflammatory activity.
Crystals of taxane derivatives and method for their preparing / 2284328
Invention relates to a novel crystalline form of (1S,2S,3R,4S,5R,8R,9S,10R,13S)-4-acetoxy-2-benzoyloxy-9,10-[(1S)-2-(dimethylamino)ethylideneoxy]-5,20-epoxy-1-hydroxytax-11-ene-13-yl-(2R,3S)-3-(tert.-butoxycarbonylamino)-3-(3-fluoro-2-pyridyl)-2-hydroxypropionate that shows the diffraction picture of roentgen rays in powder with characteristic peaks at diffraction angles (θ)= 6.2o, 10.3o, 10.7, 11.4o and 12.0, and a method for its preparing. Method involves carrying out the crystallization step by using organic solvent chosen from group consisting of ketone type solvent, nitrile solvent type and their mixture, or mixture of said solvent and water. Also, invention relates to an antitumor agent based on the prepared crystalline form. Invention provides the stable quality of a medicinal agent based on its lower hygroscopicity.
Method for isolating epotilons from reaction mixture and desorption from synthetic resin (variants), using low-polar or nonpolar solvent for realization of method / 2285007
Invention relates to a method for isolation of epotilons used in medicine in treatment of cancer diseases. Method for desorption of epotilons A, B, D and/or E from synthetic resin is based on using low-polar or nonpolar solvent chosen from the group comprising (lower)-alkyl halides and aromatic solvents, or mixture of two or more amount of such solvents wherein prefix "(lower)" means that radical comprises up to 7 carbon atoms. Used aromatic solvent is chosen from the group including naphthalene, benzene or naphthalene and benzene substituted with one or some substitutes chosen from the following group: (lower)-alkyl, (lower)-alkoxy-group, halogen atom, nitro-group and (lower)-alkoxy-(lower)-alkyl wherein prefix "(lower)" means that radical comprises up to 7 carbon atoms. Solvent is removed to the required level but up to preparing a dry residue preferably. If necessary, residue is dissolved in mixture alcohol/hydrocarbon in the corresponding volume ratio. Alcoholic phase is evaporated until dry and then alcoholic extract is crystallized from mixture alcohol and hydrocarbon. Then formed crystallized product is dissolved in mixture nitrile/water but preferably in mixture acetonitrile/water taken in the ratio = 2:3 (vol./vol.). Formed solution is applied on column (if necessary, after separation for some distillates) for preparative chromatography in reversed phase followed by elution with mixture nitrile/water, removing nitrile and extraction of an aqueous phase with ester. Ester extract is evaporated and formed product is subjected for crystallization. Method for preparing epotilons A, B, D and/or E from resin or reaction mixture involves the following steps: (a) desorption of epotilons with low-polar or nonpolar solvent chosen from the group including (lower)-alkyl halides and aromatic solvents, or mixture of two or more amount of such solvents being the desorption step can be repeated up to achievement of the more complete desorption; (b) removal of solvent used in desorption from formed solutions by evaporation; (c) optional crystallization of epotilon(s) after desorption and first of all for crystallization of epotilon B by addition of mixture of alcohol with hydrocarbon and the following evaporation of alcoholic phase until dry and crystallization of epotilon B from the corresponding mixture of solvents; (d) (obligatory step) separation of epotilons by method of chromatography in reversed phase and the following dissolving a residue obtained in previous step in suitable solvent, elution with mixture nitrile/water and removing nitrile from epotilon-containing fractions by evaporation. If necessary, water remained with epotilon is extracted with ester followed by evaporation of epotilon-containing ester phase until dry; (e) optional purification by adsorption chromatography method, and final recrystallization of purified epotilon from corresponding solvents or mixture of solvents. If necessary, in this process between each step formed solutions or suspensions are concentrated, and/or liquid or solid components are separated of one another. Separation of epotilons A and B is carried out by chromatography method based on a mobile layer modeling. Invention provides simplifying methods for preparing large amounts of epotilons for satisfying requirement in these agents.
Tetracyclic heterocompounds as estrogen receptor modulating agents / 2305099
Invention relates to novel tetracyclic heterocompounds of the formula (I): wherein X, Y, Z, R1 - R4, n and m has values given in the invention description and used as selective modulating agents for estrogen receptors. Also, invention relates to a method for synthesis of these compounds and pharmaceutical compositions comprising thereof, and their using in treatment and/or prophylaxis of disorders mediated by one or more estrogen receptors. Proposed compounds are useful in treatment and/or prophylaxis of disorders associated with depleting estrogen and comprising such disorders as rush of blood, vaginal dryness, osteopenia and osteoporosis, hormone-dependent cancer and hyperplasia of breast, endometrium, uterus cervix and prostate, endometriosis, uterus fibroma, osteoarthritis that can be used as contraceptive agents both separately and in combination with progestogen or progestogenous antagonist.
C-glycoside derivatives and their salts / 2317288
Invention relates to novel compounds representing C-glycoside derivatives and their salts of the formula: wherein ring A represents (1) benzene ring; (2) five- or six-membered monocyclic heteroaryl ring comprising 1, 2 or 4 heteroatoms chosen from nitrogen (N) and sulfur (S) atoms but with exception of tetrazoles, or (3) unsaturated nine-membered bicyclic heterocycle comprising 1 heteroatom representing oxygen atom (O); ring B represents (1) unsaturated eight-nine-membered bicyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O; (2) saturated or unsaturated five- or six-membered monocyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O; (3) unsaturated nine-membered bicyclic carbocycle, or (4) benzene ring; X represents a bond or lower alkylene wherein values for ring A, ring B and X correlate so manner that (1) when ring A represents benzene ring then ring B is not benzene ring, or (2) when ring A represents benzene ring and ring B represents unsaturated eight-nine-membered bicyclic heterocycle comprising 1 or 2 heteroatoms chosen from N, S and O and comprising benzene ring or unsaturated nine-membered bicyclic carbocycle comprising benzene ring then X is bound to ring B in moiety distinct from benzene ring comprised in ring B; each among R1-R4 represents separately hydrogen atom, -C(=O)-lower alkyl or lower alkylene-aryl; each R5-R11 represents separately hydrogen atom, lower alkyl, halogen atom, -OH, =O, -NH2, halogen-substituted lower alkyl-sulfonyl, phenyl, saturated six-membered monocyclic heterocycle comprising 1 or 2 heteroatoms chosen from N and O, lower alkylene-OH, lower alkyl, -COOH, -CN, -C(=O)-O-lower alkyl, -O-lower alkyl, -O-cycloalkyl, -O-lower alkylene-OH, -O-lower alkylene-O-lower alkyl, -O-lower alkylene-COOH, -O-lower alkylene-C(=O)-O-lower alkyl, -O-lower alkylene-C(=O)-NH2, -O-lower alkylene-C(=O)-N-(lower alkyl)2, -O-lower alkylene-CH(OH)-CH2(OH), -O-lower alkylene-NH, -O-lower alkylene-NH-lower alkyl, -O-lower alkylene-N-(lower alkyl)2, -O-lower alkylene-NH-C(=O)-lower alkyl, -NH-lower alkyl, -N-(lower alkyl)2, -NH-lower alkylene-OH or NH-C(=O)-lower alkyl. Indicated derivatives can be used as inhibitor of co-transporter of Na+-glucose and especially as a therapeutic and/or prophylactic agent in diabetes mellitus, such as insulin-dependent diabetes mellitus (diabetes mellitus 1 type) and non-insulin-dependent diabetes mellitus (diabetes mellitus 2 type), and in diseases associated with diabetes mellitus, such as insulin-resistant diseases and obesity.
Azaheterocycles, combinatory library, focused library, pharmaceutical composition and method for preparing (variants) / 2318818
Invention relates to novel azaheterocycles of the general formula (I): possessing inhibitory effect on activity of tyrosine kinase and can be used in treatment of different diseases mediated by these receptors. In compound of the general formula (1) W represents azaheterocycle comprising 6-13 atoms that can be optionally annelated with at least one (C5-C7)-carbocycle and/or possibly annelated with heterocycle comprising 4-10 atoms in ring and comprising at least one heteroatom chosen from oxygen (O), sulfur (S) or nitrogen (N) atom; Ra 1 represents a substitute of amino group but not hydrogen atom, such as substituted (C1-C6)-alkyl, possibly substituted aryl and possibly substituted 5-10-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; Rb represents carbamoyl group -C(O)NHRa wherein Ra represents a substitute of amino group but not hydrogen atom, such as possibly substituted alkyl, possibly substituted aryl, possibly substituted 5-10-membered heterocyclyc comprising at least one heteroatom chosen from O, S or N; Rc represents a substitute of cyclic system, such as possibly substituted (C1-C6)-alkyl, possibly substituted aryl and possibly substituted 5-6-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; or Rb and Rc form in common aminocyanomethylene group [(=C(NH2)CN], or their pharmaceutically acceptable salts. Also, invention relates to methods for synthesis of these compounds (variants), a pharmaceutical composition, combinatory and focused libraries.
Analogs of himbacin, their using and pharmaceutical composition based on thereof possessing property of thrombin receptor antagonist / 2319704
Invention relates to heterocycle-substituted tricyclic compounds of the formula (I): or their pharmaceutically acceptable salts wherein R means hydrogen atom; R1 and R2 are chosen independently from group comprising hydrogen atom or alkyl comprising 1-6 carbon atoms; R3 means hydrogen atom; n1 and n2 = 0-3 independently under condition that they both do not mean 0; Het means pyridyl wherein pyridyl is added to B through cyclic carbon atom and it comprises from 1 to 4 substitutes (W) chosen independently from group comprising -NR4R5, -NHCOR26, -NHSO2R16; R21 means aryl and R21 means heteroaryl wherein heteroaryl represents furyl, thienyl, pyridyl, thiazolyl, pyrrolidinyl, azethidinyl; R4 and R5 mean hydrogen atom or alkyl comprising 1-6 carbon atoms, or R4 and R5 mean in common -(CH2)3-, -(CH2)4-, -(CH2)5- or -(CH2)2NR7-(CH2)2- wherein R7 means hydrogen atom or alkyl comprising 1-6 carbon atoms; R8, R, R10 and R11 mean hydrogen atom; B means -(CH2)n4CR12=CR12a(CH2)n5 wherein n4 and n5 = 0-2 independently; R12 and R12a are chosen independently from group comprising hydrogen atom or alkyl comprising 1-6 carbon atoms; R21 means from 1 to 3 substitutes chosen independently from group comprising hydrogen atom, trifluoromethyl, trifluoromethoxy, halogen atom, cyano, alkyl comprising 1-6 carbon atoms, alkoxy group comprising 1-6 carbon atoms, or -CR29(=NOR28); R22 means -COR23, -S(O)R31, -S(O)2R31 or -COOR27; R23 means cycloalkyl comprising 3-7 carbon atoms, (C3-C7)-cycloalkyl-(C1-C6)-alkyl, cycloalkyl comprising 3-7 carbon atoms containing from 1 to 3 substitutes chosen from group comprising halogen atom, (C1-C3)-alkoxy-(C1-C3)-alkyl, hydroxy group and alkoxy group comprising 1-6 carbon atoms, aryl, aryl-(C2-C6)-alkyl; R27 means alkyl comprising 1-6 carbon atoms, phenyl or benzyl; R28 and R29 are chosen independently from group comprising hydrogen atom or alkyl comprising 1-6 carbon atoms; R31 means alkyl comprising 1-6 carbon atoms, halogenalkyl comprising 1-6 carbon atoms, aryl, aryl-(C1-C6)-alkyl. Also, invention relates to pharmaceutical compositions containing these substances and their using for preparing a drug used in treatment of thrombosis, atherosclerosis, restenosis, hypertension, stenocardia, arrhythmia, heart failure and cancer.
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FIELD: chemistry. SUBSTANCE: invention concerns method of polyolefin composition nucleation by mixing the composition with compound of the structural formula: , where: n is 0, 1 or 2; Ar1 and Ar2 are independently selected out of group including non-substituted aryl groups and aryl groups substituted by substitutes selected out of group including alkyl groups, alkenyl groups, alkinyl groups, alkoxy groups, carboxy groups and halogens; and R is selected out of group including alkenyl groups, alkyl groups, alkoxy groups, hydroxyalkyl groups and alkylhalide groups. Also invention claims the compound itself, method of its obtaining and moulded or cast polyolefin article including this compound. EFFECT: efficient method of polyolefin composition nucleation. 19 cl, 3 tbl, 22 ex
Cross-reference to related applications This application is a partial continuation of the application entitled "Acetaline compositions", filed on 26 April 2004 under registration number 10/831920. Prior art Derivatives acetals polyhydric alcohols can be used for various purposes, including, for example, used as nucleation agents for polymer resins, as well as gelling agents and thickening agents for organic liquids. It is known that these purposes can be used connection type dibenzylideneacetone (DBS). The use of nucleation agents to reduce the turbidity of products made from crystalline polyolefin resins, known in the art. Typical acetals of sorbitol and xylitol, which were used as brightening agents are described in several patents, including, for example, U.S. patent No. 4016118, Hamada et al.(dibenzylideneacetone); U.S. patent No. 4314039, Kawai et al. (di(alkylbenzenes)sorbite)); U.S. patent No. 4371645, Mahaffey, Jr. (diacetyl sorbitol having at least one atom of chlorine or bromine as a substituent); U.S. patent No. 4954291, Kobayashi et al. (distribution of diacetals sorbitol and xylitol made from a mixture of dimethyl - or trimethylsilanol benzaldehyde and unsubstituted benzaldehyde). In other work, and there is but in U.S. patent No. 5049605, Reckers et al., described bis(3,4-dialkylanilines)sorbite containing substituents, forming a carbocyclic ring. The substitution of various groups in the position(s) benzyl ring DBS connections can significantly affect the suitability of these compounds as nucleation agents or bleaching agents. A significant number of previous works focused on the modification of substitution of the substituent(s) benzylidene rings. However, at present, attempts are being made to obtain other compounds that also would reduce the turbidity (and thus would increase the transparency of the polymer when used as plastic additives in polymer compositions. The result of chemical transformations is often unpredictable. Change any part or substituted groups in the compounds of a specific type can significantly affect the technological properties and the efficiency of this connection. The present invention relates to new and valuable compositions, which were not known up to the present time and which can be successfully used as plastic additives, or as gelling agents, thickeners or agents used for other purposes. Detailed description of the invention Listed below are the specific options ASU is estline of the present invention, described in one or more examples below. Each example is provided to illustrate the present invention and is not limiting. For each specialist in this area it is obvious that the present invention can be made of various modifications and changes do not go beyond being or scope of the invention. In the present application describes a composition of additives for polyolefins. In some cases, the composition of additives for polyolefin polymers enhances the transparency of the plastic polymer compositions when it is added to such compositions. In some cases, the specified composition of the additives should preferably be used in combination with polypropylene, however, the scope of the present invention includes various applications of this composition in combination with other polymers. Olefin polymers, which can be subjected to nucleation with the use of these compositions (and transparency which can be enhanced by the method according to the invention are polymers and copolymers of aliphatic monoolefins containing from 2 to 6 carbon atoms and having a molecular weight of from about 10000 to 2000000, preferably about 30,000 to 300,000, such as polyethylene, including linear low density polyethylene, the polyethylene is iscoe density and high density polyethylene, polypropylene, a crystalline copolymer of ethylene/propylene (statistical or block copolymers), poly(1-butene) and polymethylpentene. Examples of other thermoplastic polymer resins that can be subjected to nucleation using this acetylenic compounds are polyesters, poly(ethyleneterephthalate)(PET) and poly(butilstearat) and polyamide, including nylon 6 and nylon 6,6, poly(problemsolved), syndiotactic polystyrene and polyketone, having in its backbone carbonyl group. This composition may contain a polymer selected from aliphatic polyolefins and copolymers containing at least one aliphatic olefin and one or more Ethylenediamine copolymers, and at least one mono-, di - or triacetate substituted Aldata (such as allylboronic, profilarbed, allelectric, propicillin etc). Mono-, di - or triacetate substituted Aldata may include a composition described below. A non-limiting example may be substituted aldit formula (I), combined with at least one mol of benzaldehyde, selected from compounds of the formula (II)below: In the formula (I): n is 0, 1 or 2; and R is not hydrogen and is independently selected from the group comprising alkeneamine group (such as allyl), alkyl group, alkoxygroup, hydroxyalkyl group, alkylhalogenide group. In the formula (II) R1, R2, R3, R4and R5independently selected from the group consisting of hydrogen, fluorocarbons, alkenyl, alkyl groups, etkinlik groups, alkoxygroup, carboxypropyl, halides and phenyl, or, in some embodiments of the invention, any two adjacent groups can be merged to form a cyclic group, where this cyclic group may consist of methylendioxy, cyclopentyloxy group, tsiklogeksilnogo group or other similar cyclic groups. In one of specific embodiments of the invention acetaline connection can be obtained by a method including (a) the reaction of a polyhydric alcohol with alkenylphenol molecule with the formation of the first connection; and (b) the reaction of condensation of the specified first connection with aromatic aldehyde with education acatalog connection. However, the present invention can be implemented in other ways. Thus obtained acetylene compound can be a mono-, di - or triacetate, but as it was found, in many cases, particularly suitable is diacetyl. In one of specific embodiments the image is the shadow, described below, acetaline connection may contain allyl. In some cases, this reaction product or the final composition is diacetyl (and thus obtained reaction product of Aldata and benzaldehyde has a molar ratio of 1:2). Can be obtained a composition having the structure of formula (III)below. The method according to the invention can also be obtained monoacetal or triacetyl, but below are just one particular diacetylene composition: In this composition n can be 0, 1 or 2; and Ar1and Ar2independently selected from substituted or unsubstituted arylesterase groups. In addition, R may be selected from the group consisting of alkenyl, Akilov, alkoxy, hydroxyalkyl and alkylhalogenide. R may contain alkenyl, however, it was found that in some specific embodiments of the invention for group R preferred is allyl. It should be noted that the stereochemical structure of the group R does not have a binding value and the present invention is not limited to any particular stereochemical structure of the group R, so everything described here chemical structure include all isomers, the formation of which is determined by the stereochemistry of the carbon atom to which connec the N. R. With regard to the above-described composition, in this connection, it should be noted that although here are presented only 1,3:2,4-isomer (isomer position of carbon atoms in the chain sorbitol, which form two acetal) and this structure is only for convenience and for purposes of illustration, but the present invention is not limited to isomers of type 1,3:2,4 and may include any other isomers, such as the isomers of type 1,3:4,6 and 2,4:3,5. Diacetate, triacetate and monoacetal according to the invention may be condensation products of substituted alditol, such as (but not limited to, allylboronic, profilarbed, 1-methyl-2-propenylboronic, allelectric, propicillin and (substituted) benzaldehyde. Examples of suitable (substituted) benzaldehyde are benzaldehyde, 4-ethylbenzaldehyde, 4-isobutylbenzene, 4-fluoro-3-methylbenzaldehyde, 5,6,7,8-tetrahydro-2-afterdeserialize, 3-methylbenzaldehyde, 4-propylbenzamide, 4-butylbenzaldehyde, 4-methoxybenzaldehyde, 3-chlorobenzaldehyde, 3,4-dimethylbenzaldehyde, 3,5-differentally, 3-fermentology, 4-fermentology, 3-bromo-4-fermentology, 3-methyl-4-methoxybenzaldehyde, 2,4,5-trimethylbenzaldehyde, 4-chloro-3-fermentology, 4-methylbenzaldehyde, 3-bromobenzaldehyde, 4-methoxybenzaldehyde, 3,4-dichlorobenzamide is d, 4-fluoro-3,5-dimethylbenzaldehyde, 2,4-dimethylbenzaldehyde, 4-bromobenzaldehyde, 3-ethoxybenzaldehyde, 4-allyloxymethyl, 3,5-dimethylbenzaldehyde, 4-chlorobenzaldehyde, 3-methoxybenzaldehyde, 4-(trifluoromethyl)benzaldehyde, 2-naphthaldehyde, 4-isopropylbenzaldehyde, 3,4-diethoxybenzene, 3-bromo-4-ethoxybenzaldehyde, piperonal, 3,4-dimethoxybenzaldehyde, 4-carboxybenzene, 3-Gex-1-universalized and 2-chlorobenzaldehyde. The preferred diacetylene according to the invention are 1,3:2,4-bis(4-ethylbenzamide)-1-allylboronic, 1,3,2,4-bis(3'-methyl-4'-formanilide)-1-profilarbed, 1,3,2,4-bis(5',6',7',8'-tetrahydro-2-afterdeserialize)-1-allelectric, bis-1,3,2,4-(3',4'-dimethylbenzylidene)-1"-methyl-2-profilarbed, 1,3,2,4-bis(3',4'-dimethylbenzylidene)-1-propixel. Diacetate and monoacetal according to the invention can be obtained by various methods, some of which are known in the art. Typically in such methods is based on reaction of one mole of the substituted Aldata (such as allylboronic, profilarbed, allelectric, propicillin etc.) with 2 moles of aldehyde (for diacetate), with 1 mol of aldehyde (for monoacetate) or with 3 moles of aldehyde (for triacetate) in the presence of acid catalyst (inorganic acid such as hydrochloric acid, or organic acids, t is coy as p-toluensulfonate acid (pTSA)). In addition, the used organic solvent miscible with water (such as lower alkilany alcohol, N,N-dimethylformamide or acetic acid) at room temperature. In accordance with the present invention in the structure can have any number of groups DBS. Usually in the hydrocarbon skeleton is one, two or three DBS (i.e arylesterase) group. Below are a few examples of groups that can be used in the method of the nucleation polyolefin composition. That is, there can be used one or several groups: where: Ar, Ar1and Ar2independently selected from substituted or unsubstituted arylesterase groups; and R is selected from the group consisting of alkenyl, Akilov, alkoxy, hydroxyalkyl, alkylhalogenide and their derivatives. In addition, this polyolefin composition may be combined with additives. Examples of co-additives, which can be used are given below in sections (1)to(3). In the example below 21 presents another example of co-additives, which can be used, namely, sodium lauryl sulfate. I can give many other examples of co-additives, and additives listed below may be used in essentially any agent nucleation patterns or their compositions is s, described in this application. In addition, one of the co-additives listed below may be used more than one co-additive, and the amount used or the concentration may vary depending on the purpose of the application. (1) a Co-additive for inhibiting migration of smell and taste: Alkali metal salts, formed by amino acids (at least one amino acid selected from the following amino acids: glycine, L-alanine, L-phenylalanine, L-isoleucine, L-valine, L-leucine, L-Proline, L-arginine, L-aspartic acid, L-cystine, L-glutamic acid, L-serine, L-histidine, L-tryptophan, L-lysine, L-threonine, L-methionine, DL-ethionine, L-cysteine, L-tyrosine, L-asparagine, L-glutamine, L-Norvaline and L-α-aminobutyric acid) and 0.1 to 100 parts by weight of at least one fatty acid having 8-32 carbon atoms (octanoic acid, capric acid, laurinovoj acid, myristic acid, palmitic acid, stearic acid, 12-hydroxystearate acid, beganovi acid, montenovo acid, oleic acid, linoleic acid, areostationary acid, ricinoleic acid and erucic acid). (2) a Co-additive for inhibiting migration of smell and taste and for lowering the melting temperature DBS: : At least a saturated or unsaturated aliphatic alcohol with 6-32 atoms in which Lerida (for example, lauric alcohol). In: at least saturated or unsaturated aliphatic carboxylic acid with 8-32 carbon atoms, having in its molecule at least one hydroxy-group (for example, 12-hydroxystearate acid), With: at least one type selected from the following groups: lithium salts, sodium salts or potassium salts of saturated or unsaturated fatty acid having 8-32 carbon atoms, where these groups may have in its molecule at least one hydroxyl group, or D: salt of ester of sulfuric acid of at least one type selected from the following group: salt euryceros acids, salts SteelSeries acids, salts yerserday acid and salts polyoxyethyleneglycol ether sulfuric acid. (3) Co-additives with granulated or powdered diacetolol compositionwhere the binding agent is selected from the group consisting of monocarboxylic acids, polycarboxylic acids, partial salts of polycarboxylic acids, esters of phosphoric acid and at least one member selected from the group consisting of monohydroxy aliphatic C1-C30alcohols and polyhydric aliphatic C2-C30alcohols; esters of phosphorous acid and at least one member selected from the group consisting of monohydroxy aliphatic the ski With the 1-C30alcohols and polyhydric aliphatic C2-C30alcohols; esters of phosphoric acid and at least one member selected from the group consisting of monohydroxy aromatic With6-C30alcohols and polyhydric aromatic With6-C30alcohols; esters of phosphorous acid and at least one member selected from the group consisting of monohydroxy aromatic With6-C30alcohols and polyhydric aromatic With6-C30alcohols; taurine, salts of ester of sulfuric acid, sulfonic acid salts, salts of ester of phosphoric acid and salts of mono-, di - and tri(C6-C30fatty acid)aluminum, where each of these components in a given molecule may contain at least one bond or functional group selected from the group consisting of essential communication, ester bonds, thioester communication, amide bond, halogen atom, amino group, hydroxyl group, heterocyclic group and a carbonyl group. Methods of synthesis of diacetate One of the methods that can be used to obtain diacetate according to the invention described in U.S. patent No. 51106999, Gardlik et al., which is included in the present description by reference. Methods of obtaining and synthesis of carbohydrates, having chains of different lengths is, described by Kim Gordon, Schmid and Whitesides,Tin and Indium Mediated Allylation in Aqueous Media: Application to Unprotected Carbohydrates,J. Org. Chem., 5500-5507, 58(1993) and in the work Whiteside,Journal of the American Chemical Society,113, 6674-6675 (1991). In the work Whiteside was proposed by the reaction of glucose with allylbromide/tin. One of the methods that can be used to obtain the starting compounds for the synthesis of compositions required for the implementation of the present invention, described below, in which the carbohydrate may be added allyl group. This is illustrated by the reaction scheme is given only as examples, and such reactions can be carried out for carbohydrates that have a greater or fewer carbon atoms in its chain. In accordance with the present invention acetylene compound produced by the method comprising (a) reaction of carbohydrate and alkenylphenol group with the first connection; and (b) the reaction of condensation of the specified first connection with aromatic aldehyde with education acatalog connection. In some cases, this Alchemilla group contains allyl. During the research that led to the creation of one of the embodiments of the present invention, it was found that the above-described chemical reaction with allylbromide/tin one is by one of the methods of synthesis of hydrocarbon chains of carbohydrate, and this reaction can be carried out as one of the stages in the sequence of reactions, which, as it has been unexpectedly discovered, allow to obtain a composition having a number of advantages and valuable properties. The total path of the reaction can be used in various forms for the synthesis of carbohydrates upon receipt of the compositions according to the invention. In one of the embodiments the present invention relates to the use of reactions for the synthesis of carbohydrates in combination with other reactions of formation of acetals to obtain compositions according to the invention. Can be obtained substituted diacetate, triacetate and monoacetal sorbitol. These structures contain a mixture of acetals any correlated types (such as di-, tri - and/or monoacetal related to the desired acetal). Although the removal of these impurities is not always going to happen (especially if they are present in very low proportions) before the introduction of the specified diacetate, triacetate or monoacetal in the target polyolefin, however, removing these impurities may still be desirable, and such clearance may contribute to increasing the transparency of the resin produced by the above method. In one of the embodiments of the invention cleanup diacetate can be done by removing any present t is acetale their extraction with the use of relatively non-polar solvent. As one non-limiting example, the removal of impurities can serve as a cleaning product, which resulted in the number of diacetyl in such a composition of the additive is at least 95%, and even up to 98 percent or more, depending on the purpose of the application. The following illustrates how a more complete synthesis, which is shown here only for purposes of illustration, and is not limited to the following compounds or reactions: Scheme(s) synthesis The General structure of the synthesized compositions based on acetal To implement the present invention as Ar1and Ar2can be used many different substituted benzyl groups, as illustrated in several typical examples listed in table 1, where these groups were synthesized and tested as described in examples below. Substituted group for Ar1and/or Ar2not limited to only the groups are presented in table 1. For example, table 1 shows different compositions for different substituted groups Ar1and Ar2where n=0, and where n=1. If n=0, is used xilitla group. If n=1, is used Corbina group. Although compounds in which n=2, without the camping in table 1, however, such compounds are also included in volume and being described here present invention. In fact, the number of substituents in such compositions is not limited, provided that they are chemically possible. However, it was discovered that certain substituted group in this compound is able to enhance its properties. In accordance with this invention R can be selected from a wide range of compounds, including, but not limited to, for example: -CH3; -CH2CH3; -CH2CH2CH3; -CH2CH2CH2CH3; -CH2CH=CH2; -CH(CH3)CH=CH2; -CH2SN-X-CH2-X'; CH2CH2-X-CH2-CH3; -CH2SN-X"'-CH2HE; -CH-HE-HF-HE-CH2HE. In the above selected compounds X, X', X" and X"', if present, contain independently selected halide group. Sometimes especially preferred are allyl group (-CH2CH=CH2), and some of these groups were synthesized and submitted along with other groups in table 1. The synthesis of the compound of example 21 Example 1 1-Allylboronic A 3-liter three-neck round bottom flask, equipped with the th of the heating casing, stirrer, intake of nitrogen and refrigerator loaded with 900 ml of ethanol, 150 ml of water, 180 g (1.00 mol) of D-glucose, 119 g (1.00 mol) of tin powder (˜100 mesh) and 121 g (1.00 mol) of allylbromide. The mixture was stirred and slowly heated to boiling point under reflux with 60°there was a significant release of heat and gas. The gray suspension was stirred while boiling under reflux for two days, and during this time the reaction mixture was bought orange/brown color. After completion of the heat dissipation and the mixture was left to cool to room temperature. The reaction mixture was neutralized to pH 7 by adding about 200 ml of 5M aqueous NaOH solution. The resulting suspension was filtered to remove solids, and the yellow solution was decolorized several treatments of activated carbon. Activated charcoal was removed by filtration and the solvent was removed by evaporation on a rotary evaporator to obtain a white syrup. Usually the yield was 200 g with threo:Erythro-ratio 1:6, which is confirmed by GC-MS. The resulting syrup was used without further purification. Pure Erythro-isomer can be obtained by hydrolysis as described in any of examples 2-8.1H-NMR (500 MHz, D2O, ppm): 2,34-is 2.37 (m, 2H), 3,63-3,95 (m, 7H), 5,13-5,20 (m, 2H), 5,88-of 5.89 (m, 1H).13C-NMR (125 MHz, D2 O, ppm): 38,32; 63,69; 70,74; 71,14; 71,80; 71,92; 74,58; 118,60; 135,72. Example 2 Bis-1,3:2,4-(4'-ethylbenzamide)-1-allylboronic A 2-liter reactor equipped with a stirrer and a hole for the intake of nitrogen, downloaded 111 g (0.50 mol) of syrup of 1-allylcarbamate (the product of example 1) in 100 ml of 6N HCl solution. Then the reactor was added 134 g (1.0 mol) of 4-ethylbenzaldehyde in 800 ml of methanol. A clear solution was stirred 48 hours, and during this time we observed formation of a significant amount of white precipitate. The powder was isolated by filtration and washed with 250 ml of a 1M aqueous solution of NaOH. Then the powder is suspended in water and neutralized to pH 7 with a small amount of NaOH. The suspension was heated to boiling, then filtered. The white powder was washed 7×500 ml of boiling water. The washed powder was dried overnight. Then the powder was stirred in 500 ml of cyclohexane was heated to boiling, filtered and washed 2×250 ml of boiling cyclohexane. Selected white powder was dried in a vacuum oven and got 107 g of the product, TPL 244-246°C. the purity of the product exceeded 99%, as confirmed by GC-MS.1H-NMR (300 MHz, DMSO-d6, ppm): 1,14-1,19 (t, 6N), 2,39 is 2.44 (t, 2H), 2,56-2,63 (kV, 4H), 3,41-4,10 (m, 7H), of 4.38 was 4.42 (t, 1H), 4,81 of 4.83 (d, 1H), 5,07-5,19 (kV, 2H), ceiling of 5.60-5,64 (d, 2H), of 5.84-of 5.89 (m, 1H), 7,19-of 7.23 (t, 4H), 7,34-7,38 (t, 4H). Examples 3-8 Various allylamine dibenzylidene (DBS) molecules were Synthe is iravani in accordance with the methods similar to the procedures described above in example 2. The structure of these molecules and their measured the melting temperature are presented in table 1. All derivatives are NMR data corresponding to the above structures, and their purity is at least 95%, which was confirmed by GC-MS. Example 9 1-Allelectric A 5-liter three-neck round bottom flask, equipped with a heating jacket, stirrer, intake of nitrogen and refrigerator, downloaded 1.8 l of ethanol, 0.3 l of water, 300 g (2.00 mol) of D-xylose, 242 g (2.04 mol) of tin powder (˜325 mesh) and 242 g (2.00 mol) of allylbromide. The mixture was stirred and slowly heated to boiling point under reflux with 60°there was a significant release of heat and gas. The gray suspension was stirred while boiling under reflux for three days, and during this time the reaction mixture was bought orange/brown color. After completion of the heat dissipation and the mixture was left to cool to room temperature. The reaction mixture was neutralized to pH 7 by the addition of approximately 400 ml of 5M aqueous NaOH solution. The resulting suspension was filtered to remove solids and the yellow solution was decolorized several treatments of activated carbon. Activated charcoal was removed by filtration, and dissolved the al was removed by evaporation on a rotary evaporator to obtain a white syrup. The output is typically 320,1H-NMR (300 MHz, D2O, ppm): 2,33-2,39 (m, 2H), 3,55-to 3.89 (m, 6N), 5,14-5,23 (m, 2H), of 5.89 (m, 1H). The resulting syrup was used without further purification. Example 10 Bis-1,3:2,4-(5',6',7',8'-tetrahydro-2-afterdeserialize)-1-allelectric In a two-liter reactor equipped with a stirrer and a hole for the intake of nitrogen, downloaded 144 g (0.75 mol) of syrup of 1-elixiride (product of example 9), 300 ml of water and 100 ml of concentrated (12N) HCl. The mixture was stirred until complete dissolution of 1-elixiride. Then the reactor was added 240 g (1.50 mol) 5',6',7',8'-tetrahydro-2-naphthaldehyde in 400 ml of methanol. The solution was stirred for two days, during which dropped a significant amount of white precipitate. The powder was isolated by filtration and washed with 250 ml of a 1M aqueous solution of NaOH. Then the powder is suspended in water and neutralized to pH 8 with a small amount of NaOH. The suspension was heated to boiling, then filtered. The white powder was washed 7×500 ml of boiling water. The washed powder was dried overnight. Then the powder was stirred in 0.5 l of cyclohexane was heated to boiling, filtered and washed 2×250 ml of boiling cyclohexane. Selected white powder was dried in a vacuum oven and got to 47.8 g of the product, TPL 210-212°C. the purity of the product exceeded 99%, which was confirmed by GC-MS.1H-NMR (300 MHz, DMSO-d6, ppm): 1,72 (m, 8H), 2,6-of 2.51 (t, 2H), 2,71 (m, 8H), 3,54-a 4.03 (m, 6N), 4,76-4,80 (t, 1H), 5,07-5,17 (kV, 2H), 5.56mm is 5.77 (d, 2H), 5,80-5,90 (m, 1H), 7,02-7,06 (m, 2H), 7,11-7,17 (m, 4H). Examples 11, 12 Various allyl-DBX were synthesized in accordance with methods similar to the method described in example 2. The structure of the compounds of examples 10 and 11 are presented in table 1. All derivatives are NMR data corresponding to the above structures, and their purity is at least 95%, which was confirmed by GC-MS. Example 13 Bis-1,3:2,4-(3',4'-dimethylbenzylidene)-1-propicia 58 g (0.3 mol) of syrup of 1-elixiride (product of example 8) was dissolved in 60 ml of water. Then add approximately 0.6 g of platinum (5 wt.% on charcoal) and the mixture was first made at room temperature under hydrogen pressure of 60 psi. The reaction was stopped until, until there was a decrease of the hydrogen pressure. The solid was filtered. Allyl group in the specified solution is completely turned in through the group, which was confirmed by NMR. In the sugar solution was added 100 g (0.6 mol) of 3,4-dimethylbenzaldehyde, 500 ml of ethanol and 50 ml of concentrated (12N) HCl. A clear solution was stirred at room temperature overnight, and during this time we observed the formation of a considerable amount of white precipitate. The powder was isolated by filtration and washed with 100 ml of 1M aqueous solution of NaOH. The ZAT is powder suspended in water and neutralized to pH 7 with a small amount of NaOH. The suspension was heated to boiling, then filtered. The white powder was washed 7×500 ml of boiling water. The washed powder was dried overnight. Then the powder was stirred in 500 ml of cyclohexane was heated to boiling, filtered and washed 2×250 ml of boiling cyclohexane. Selected white powder was washed with methanol, dried in a vacuum oven and got 21 g of the product, TPL 255-257°C. the purity of the product exceeded 98%, which was confirmed by GC-MS.1H-NMR (300 MHz, DMSO-d6, ppm): 0,89-of 0.93 (t, 3H), 1,30-1,50 (m, 2H), 1,50-1,70 (m, 2H), 2,22 (N), 3,50-of 4.05 (m, 6N), 4,78 (1H), 5,56-5,59 (d, 2H), 7,14-7,21 (m, 6N). Example 14 Bis-1,3:2,4-(3 methyl-4'-formanilide)-1-profilarbed Approximately 85 g (0.38 mol) of syrup of 1-allylcarbamate (the product of example 1) was dissolved in 85 ml of water. Then was added 0.8 g of platinum (5 wt.%. on charcoal) and the mixture was first made at room temperature under hydrogen pressure of 60 psi. The reaction was stopped until, until there was a decrease of the hydrogen pressure. The solid was filtered. Allyl group in the specified solution is completely turned in through the group, which was confirmed by NMR. In the sugar solution was added 75 g (0.54 mol) of 3-methyl-4-forventelige, 500 ml of ethanol and 56 ml of concentrated (12N) HCl. A clear solution was stirred at room temperature overnight, and during this time the viewers the elk formation of a significant amount of white precipitate. The powder was isolated by filtration and washed with 100 ml of 1M aqueous solution of NaOH. Then the powder is suspended in water and neutralized to pH 7 with a small amount of NaOH. The suspension was heated to boiling, then filtered. The white powder was washed 7×500 ml of boiling water. The washed powder was dried overnight. Then the powder was stirred in 500 ml of cyclohexane was heated to boiling, filtered and washed 2×250 ml of boiling cyclohexane. Selected white powder was washed with methanol, dried in a vacuum oven and got 21 g of the product, TPL 253°C. the purity of the product exceeded 98%, which was confirmed by GC-MS.1H-NMR (300 MHz, DMSO-d6, ppm): 0,91-of 0.95 (t, 3H), of 1.40 to 1.48 (m, 2H), 1,54-to 1.67 (m, 2H), 2,13-2,25 (6N), 3,42-of 4.05 (m, 7H), and 4.40 (t, 1H), 4,82-4,84 (d, 1H), ceiling of 5.60-5,62 (d, 2H), 7,11-7,16 (m, 2H), 7,30-7,37 (m, 4H). Example 15 Bis-1,3:2,4-(3',4'-dimethylbenzylidene)-1'-methyl-2'-propenylboronic In a two-liter three-neck round bottom flask, equipped with a heating jacket, stirrer, intake of nitrogen and refrigerator loaded with 600 ml of ethanol, 100 ml of water, 126 g (0.70 mol) of D-glucose, 84 g (0.7 mol) of tin powder (˜100 mesh) and 131 g (0.97 mol) of brothelbased. The mixture was stirred and slowly heated to boiling point under reflux with 60°there was a significant release of heat and gas. The gray suspension was stirred while boiling with britishtelecom during the night, and during this time the reaction mixture had become light yellow in color. After completion of the heat dissipation and the mixture was left to cool to room temperature. The reaction mixture was filtered and the solution was mixed with 188 g (1.4 mol) of 3,4-dimethylbenzaldehyde during the night, and at this time we observed formation of a significant amount of sediment. The yellow solid was isolated by filtration and washed with methanol to obtain a white powder, TPL 233-235°C. GC-MS and NMR analyses indicated the presence of the desired compound as a mixture of two diastereomers (2:1) 1-methyl-2-propenyl. Example 16 Bis-1,3,2,4-dibenzylidene-2',3'-dibromopropyl/bis-1,3,2,4-dibenzylidene-2'-bromo-3'-hydroxypropionic An aqueous solution of 90 g of syrup allylbromide (example 1) in 110 g of methanol was titrated with bromine until then, until the solution became light yellow. Then added a small amount of NaHSO3getting colourless solution. After this was added 1.9 grams of monohydrate p-toluensulfonate acid. A clear solution was stirred overnight and was observed the formation of a considerable amount of white precipitate. The powder was isolated by filtration and washed with 1M aqueous NaOH solution. Then the powder is suspended in water and neutralized to pH 7 with a small amount of NaOH. The suspension was heated to boiling, then Phi is travali. The white powder was washed 7×500 ml of boiling water. The washed powder was dried overnight. Then the powder was stirred in 50 ml of cyclohexane was heated to boiling, filtered and washed 2×25 ml of boiling cyclohexane. The product was dried in a vacuum oven and got to 7.3 g of white powder, TPL 188-190°C. GC-MS and NMR analyses indicated the presence of a mixture of bis-1,3:2,4-dibenzylidene-2',3'-dibromopropionate (90%) and bis-1,3:2,4-dibenzylidene-2'-bromo-3'-hydroxypropylamino (10%). Example 17 Asymmetric, benzyliden/2,4-dimethylbenzylidene-1-allylboronic A 2-liter reactor equipped with a stirrer and a hole for the intake of nitrogen, downloaded 111 g (0.50 mol) of syrup of 1-allylcarbamate (the product of example 1) in 280 ml of methanol. Then the reactor was added 9.5 g pTSA, 53 g (0.5 mol) of benzaldehyde and 67 g (0.50 mmol) of 2,4-dimethylbenzaldehyde. A clear solution was stirred 48 hours, during which we observed formation of a significant amount of white precipitate. The powder was isolated by filtration and washed with 250 ml of a 1M aqueous solution of NaOH. Then the powder is suspended in water and neutralized to pH 7 with a small amount of NaOH. The suspension was heated to boiling, then filtered. The white powder was washed 7×500 ml of boiling water. The washed powder was dried overnight. Then the powder was stirred in 500 ml of cyclohexane was heated to boiling, filtration is ovale and washed 2× 250 ml of boiling cyclohexane. Selected white powder was dried in a vacuum oven and got to 38.4 g of the product, TPL 234-236°C. the Standard analyses of the obtained product showed that it consists of a mixture of 1,3-O-(benzylidene):2,4-O-(2,4-dimethylbenzylidene)-1-allylbromide and 1,3-O-(2,4-dimethylbenzylidene):2,4-O-benzylidene-1-allylcarbamate (85%), 1,3:2,4-bis(benzylidene)-1-allylcarbamate (5%), and 1,3:2,4-bis(2,4-dimethylbenzylidene)-1-allylcarbamate (10%). Example 18 Three-1,3:2,4:5,6-benzylidene-1-allylboronic 111 g (0.50 mol) of syrup of 1-allylcarbamate (the product of example 1) was dissolved in 111 g of water. The solution was mixed with 50 g of ice. While cooling in an ice bath to this solution was slowly added to 90 ml of 93% sulfuric acid so that the temperature was below 20°C. Then was added 106 g (1.0 mol) of benzaldehyde. In the formed dark pink suspension. The reaction mixture was left overnight at room temperature. The obtained yellow solid was collected by filtration and neutralized with 10% NaOH solution. The solid is washed with boiling water, then cooled methanol and received a white solid, TPL 216-218°C. GC-MS analysis indicated the presence of two diastereomers that differ only by a carbon atom in the methane that is attached to the oxygen atoms in position 5 and 6 carbon allylamino fragment. The carbon atom in the methane may be attended by the e or R, or in the S-conformation) in the ratio of 24:76.1H-NMR (500 MHz, DMSO-d6, ppm): 2,43-of 2.45 (t, 2H), 3.95 to to 4.52 (m, 7H), 5,10-5,20 (DD, 2H), 5,72 (s, 1H), 5,79 (s, 1H), of 5.89 (s, 1H), 5,86-of 5.92 (m, 1H), was 7.36-to 7.50 (m, 15 NM).13C-NMR (125 MHz, DMSO-d6, ppm): 34,2; 67,0; 69,6; 70,3; 73,3; 76,9; 77,6; 99,0; 99,1; 102,8; 109,3; 117,6; 126,0; 126,6; 128,0; 128,1; 128,2; 128,6; 128,7; 129,2; 134,0; 137,8; 138,2; 138,4. Example 19 Bis-1,3:2,4-(3'-bromo-4'-ethylbenzamide)-1-allylboronic/mono-2,4-(3'-bromo-4'-ethylbenzamide)-1-allylboronic One litre 3-necked flask equipped with a mechanical stirrer, a glass lid and a hole for gas was purged with argon for 10 minutes. To this flask was added 335,2 ml of 0,4M methanol solution of 1-allylcarbamate (30,07 g, 134,1 mmol)(product of example 1) and 60,00 g (281,6 mmol) 3-bromo-4-ethylbenzaldehyde. After mixing the reagents for 10 minutes was added 42 ml of HCl (12M) for catalysis reactions. After 2 minutes after addition of HCl was observed in the precipitate, and the solution began to acquire a pinkish hue. After 3 hours of reaction pinkish hue was largely disappeared, and increased the number pinkish-white solids. Contents quickly mixed, and every 8-12 hours spent monitoring the completion of the reaction by GC-MS. After 48 hours, during which formed a significant number of not quite white precipitate, the reaction was suppressed by adding 54,00 g (962,5 mmol) of potassium hydroxide [prior the nutrient dissolved in deionized H 2O], receiving the mixture with a final pH of 12-13. The crude solids were isolated by vacuum filtration through a Buchner funnel and washed with 800 ml of boiling deionized H2O. removal of unreacted sugar product was dried over night, crushed into a fine powder and suspended in 1000 ml of deionized H2O. Suspended mixture was brought to boiling and stirred for 30 minutes. The solids were filtered off through a Buchner funnel and then washed with boiling deionized H2O (3×1000 ml). To remove residual aldehyde of the above-mentioned procedure was repeated, using boiling methanol as a wash solvent. After drying overnight GC-MS-analysis of the solids indicated the presence of a mixture of mono:dibenzylideneacetone [eur36, 85 g; crude yield of 44.5%]. To separate this mixture of the crude white solid was ground into a fine powder, stirred in boiling solvent mixture of 50:50 (CH3HE:deionized H2O) for 1 hour, subjected to hot filtration through a Buchner funnel and dried in vacuum, obtaining 27,99 g soft white powder [exit allocated DBS 33,8%]. The analysis showed that this product is a (19a) bis-1,3:2,4-(3'-bromo-4'-ethylbenzamide)-1-allylboronic [see below]. After conditioning in the course the e night in flushing solvent, used in the final treatment procedure DBS, it was observed the formation of a gelatinous white precipitate [50:50, SN3HE:deionized H2O]. This precipitate was isolated by vacuum filtration through a Buchner funnel and dried in vacuum, obtaining of 7.48 g of a white solid [MBS]. The analysis showed that this product is a (19b) mono-2,4-(3'-bromo-4'-ethylbenzamide)-1-allylboronic [see below]. (19a). The results of the analysis for bis-1,3:2,4-(3'-bromo-4'-ethylbenzamide)-1-allylcarbamate [C37H32About6Br2]: Selected white powder was dried in a vacuum oven (<10-1mm Hg) at 90°C for 18 hours and got 27,99 g soft white powder, TPL 268,2-268,6° [in argon atmosphere]. Purity was >98,3%, which was confirmed by GC-MS.1H-NMR (500 MHz, DMSO-d6that δ ppm): 1,15 (dt, 6N, -CH2WithN3); 2,42 (TDD, 2H, -allylic methylene); 2,70 (DQC, 4H,- N2CH3); 3,44 (width, m, 1H), 3,61 (width, DQC, 1H), 3,74 (width, m, 1H), 3,84 (width, d, 2H), 4,10 (width, m, 2H), 4,43 (t, 1H, 2°-HE), the 4.90 (d, 1H, 1°-HE), 5,14 (width, KVM, 2H, -CH=CN2); 5,63 (s, 1H, acetal); 5,67 (s, 1H, acetal); 5,88 (m, 1H,- N=CH2); 7,38 (width, m, 4H, aromatic); 7,58 (width, s, 1H, aromatic), 7.62mm (width, d, 1H, aromatic).13C-NMR (500 MHz, DMSO-d6that δ ppm): 14,25 (-CH2WithH3); 28,50 (-WithH2CH3) 34,29 (allyl); 62,60; 67,73; 68,86; 70,84; 77,03; 77,53; 97,83 (acetal); 97,94 (acetal); 117,49 (-CH=WithH2); 122,81; 122,88; 125,64; 125,78; 129,49; 129,62; 129,72; 129,89; 134,13 (-WithN=CH2); 138,33; 138,45; 142,91; 142,97. (19b). The results of the analysis for mono-2,4-(3'-bromo-4'-ethylbenzamide)-1-allylcarbamate [C18H25About6Br]: Selected white powder was dried in a vacuum oven (<10-1mm Hg) at 70°C for 18 hours and got 7,58 g soft white powder, TPL 199,8-200,5° [in argon atmosphere]. Purity was >96% [content DBS <4%], which was confirmed by GC-MS.1H-NMR (500 MHz, DMSO-d6that δ ppm): to 1.16 (t, 3H, -CH2WithN3); 2,10 (m, 1H, -allylic methylene); 2.40 a (width, m, 1H, -allylic methylene); 2,70 (q, 2H,- N2CH3); to 3.41 (m, 1H), 3,47 (width, d, 1H), 3,57 (width, m, 1H), 3,62 (width, d, 1H), 3,74 (width, DM, 2H), 3,88 (width, d, 1H), 4,34 (d, 1H, 1°-HE), and 4.40 (t, 1H, 2°-HE), 4,70 (d, 1H, 1°-HE), 4,78 (d, 1H, 1°-HE), 5,03 (width, m, 2H, -CH=CN2); of 5.50 (s, 1H, acetal); 5,91 (width, m, 1H,- N=CH2); of 7.36 (width, m, 2H, aromatic); to 7.67 (width, d, 1H, aromatic).13C-NMR (500 MHz, DMSO-d6that δ ppm): 14,26 (-CH2WithH3); 28,49 (-WithH2CH3); 37,89 (-allyl); 60,51; 62,70; 67,15; 69,15; 79,54; 82,33; 98,84 (acetal); 116,33 (-CH=WithH2); 122,88; 125,99; 129,42; 130,10; 135,92 (-WithN=CH2); 138,56; 142,87. Example 20 The mixture of bis-1,3:2,4-(4'-ethylbenzamide is)-1-allylcarbamate, 12-hydroxystearate acid and lauryl sodium In the cleaned 250-ml odnogolosy flask with rod stirrer was loaded to 9.50 g of bis-1,3:2,4-(4'-ethylbenzamide)-1-allylcarbamate (example 2), 0,250 g 12-hydroxystearate acid, 0,250 g of lauryl sodium and 60 g of methanol. The mixture was boiled under reflux for one hour under stirring. The reaction mixture was cooled to room temperature. The methanol is evaporated at the rotary evaporator, then dried in a vacuum oven at 80°C for 2 hours, getting 9,62 g of the product as a white solid. TPL 203-204°C. Example 21 Bis-1,3:2,4-(3',4'-dimethylbenzylidene)-1-metalcored 2,3,4,6-Tetra-O-benzyl-D-glucono-1,5-lactone (21A) 27 g of 2,3,4,6-Tetra-O-benzyl-D-glucopyranose (50 mmol) was dissolved in 153 ml of DMSO, obtaining a clear solution. Then was added dropwise 102 ml of acetic anhydride. The obtained clear solution was left over night at room temperature for mixing. After 17 hours the GC-MS analysis indicated the disappearance of the lactone and the emergence of a new connection. The yellow solution was poured into 600 ml of water and placed overnight in a separating funnel. The precipitated oil was passed through a column of silica gel, elwira first with cyclohexane, followed by a gradual increase in polarity by adding acetone to the ex long while the ratio of the final eluent cyclohexane:acetone did not reach 2:1. The appropriate fractions were collected and evaporated to obtain a light syrup, 25,2 g; yield 94%. IR (ν cm-1) 2867, 1752. 3,4,5,7-Tetra-O-benzyl-1-deoxy-D-gluco-heptanophenone (21b) 18 g (33 mmol) of compound 21A was dissolved in 200 ml of anhydrous THF under nitrogen atmosphere. The solution was cooled to -78°and a syringe was added 45 ml of MeLi (1.6 m, 72 mmol). After incubation for 1 hour at -78°the reaction was suppressed by a solution of 7 g of NH4Cl 200 ml of H2O. TLC indicated the absence of the original substance, but found a new spot corresponding to the formed product. The mixture was extracted with 3×150 ml of ethyl acetate, washed with saturated salt solution and dried over Na2SO4. After evaporation got a thick light yellow oil, which was turned into a white solid (17.6 g, yield 95%) with TPL 92-93°C.1H-NMR (300 MHz, CDCl3) δ: of 1.41 (s, 3H, CH3); 2,58 (s, 1H, HE); 3,35-to 3.38 (d, 1H); 3,65-and 3.72 (m, 3H); 3,93-to 3.99 (m, 2H); 4,50-of 4.95 (m, 8H, 4-CH2); 7,14 and 7.36 (m, 20N).13C-NMR (CDCl3) δ: 26,59; 68,81; 71,55; 73,42; 74,85; 75,58; 75,68; 78,42; 83,18; 83,63; 97,36; 127,58; 127,65; 127,74; 127,82; 127,84; 127,91; 128,28; 128,32; 128,36; 128,41; 137,87; 138,21; 138,25; 138,64. 1,3,4,5-tetrakis-benzyloxyethyl-2,6-diol (s+s') To the clear solution 5,54 g (10 mmol) of compound 21b in 60 ml of THF was added 0.5 g (12.5 mmol) of 95% LiAlH4. The mixture of toulali for 4 hours in an ice bath for mixing. TLC indicated the disappearance of all starting compounds and the appearance of two very closely spaced spots. The reaction was carefully suppressed 2N HCl, after which the reaction mixture was extracted with ethyl acetate. The combined organic phase washed with aqueous NaHCO3then with saturated salt solution and dried over sodium sulfate. After evaporation of the solvent was obtained a colorless syrup (5.5 g, yield 99%). Attitude 1,048-1,069 ppm (doublet, C): 1,170-1,191 ppm (doublet, C') was 45%:55%, which was confirmed by NMR. Heptane-1,2,3,4,5,6-hexol (21d+21d') To a solution of 2.4 g (4.3 mmol) of the compound C in 100 ml of ethanol was added 0.6 g of 5% Pd-C. the Mixture was first made at an initial hydrogen pressure of 63 psi. After 6 hours the catalyst was filtered and washed with a mixture of methanol and water. The combined solution was evaporated to obtain white solids, of 0.80 g, yield: 95%.1H-NMR (300 MHz, D2O) δ: 1,186-1,237 (two doublet, 3H), 3,537-3,988 (m, 7H). Bis-1,3:2,4-(3',4'-dimethylbenzylidene)-1-metalcored (21) To a solution of the 4.65 g (24 mmol) of the compound 21d+21d' in 100 ml of acetic acid was added 4.77 g (36 mmol) of 3,4-dimethylbenzaldehyde. The mixture was left over night at room temperature for mixing. The obtained gel was neutralized by adding CON-H2O. White solid (4,2 g) was collected by filtration and suspended in boiling water. A suspension of p which has Dorgali hot filtration and the solid is washed 7× 100 ml of boiling water. Then the solid is suspended in 50 ml of boiling methanol and again filtered. Received 2,30 g of dry white solid with a yield of 25%. GC-MS analysis indicated a purity of 98.3%. Melting point: 259-261°C.1H-NMR (300 MHz, DMSO-d6) δ: 1,23-1,25 (doublet, 3H), 2.21 are of 2.23 (m, N), 3,40-4,80 (m, N), 5,55-5,59 (doublet, 2H), 7,10-7,22 (m, 6N). Example 22 Composition containing various amounts of acetals of examples 2-21, co-supplementation of 0.05 wt.% Irganox 1010, 0.1 wt.% Irgafos168 and 0.08 wt.% calcium stearate) and in the rest of its mass, a homopolymer of polypropylene or a statistical copolymer of polypropene (containing 3% ethylene), were subjected to dry mixing in a mechanical stirrer, was extrudible through a single-screw extruder at 240°and was granulated. Plate (thickness 1.27 mm) were made by injection moulding pellets at 220°C. Were measured value TC and the percentage of turbidity, and the results of these measurements are presented in table 2. Millad 3988® is a registered trademark of Milliken and Company of Spartanburg, South Carolina. Millad 3988® is a commercially available bleaching agent containing bis(3,4-dimethyl-benzylidene)("DMDBS") and described in U.S. patent No. 5049605.
In some applications of the invention to the polymer resin may be added to the composition of nucleation agents at a concentration of about 0.005 to 3 wt.%. In other applications can be used in a concentration of from about 0.01 to 1 wt.%. In other applications, use concentration of from about 0.025 to 0.5 wt.%. song. Concentrates containing up to 50 wt.% agents nucleation in the resin, can also be obtained for the mixture with an additional amount of resin before molding. Usually concentrates, provided the 33 wt.% or less nucleation agents in the resin, are commercially available. This resin can be extruded a second time just prior to the processing of obtaining the finished product, for example, injection molding, pneumoperitoneum by extrusion, injection molding injection blow, pneumoperitoneum with extraction, direct pressing, centrifugal molding, extrusion obtaining shaped articles by extrusion with receiving sheets, hot molding, extrusion obtaining films and extrusion with getting oriented films. The gel formation and analysis Solid gels containing substituted Aldine derivatives according to the invention can also be obtained well-known and simple methods. In particular, appropriate organic solvents combined with additives in certain concentrations and thoroughly mix. Then the obtained mixture is heated to a temperature of approximately 170°F (77° (C) to 300°F (149° (C)as shown below, with stirring, for 5-120mm minutes. The resulting solution was poured into the melt to obtain a gel form. Below is a list of solvents is not exhaustive, and to obtain gels with substituted aldaniti derivatives according to the invention can be used solvents other types, and just below lists the solvents, which which are preferred for use in these purposes. To establish the fact of gel formation and determination of its hardness, and the hardness of all of the formed gels, the following samples were analyzed empirically and touch. The results are presented in table 3.
Thus, substituted Aldine derivatives according to the invention have excellent gelling properties in the presence of certain solvents, but not limited to, depending on their concentration. For any medium-specialist it is obvious that the discussion presented in this description is given only of illustration the x purposes and should not be construed as limiting the broader aspects of the invention, which are included in the scope of representative variants of the invention. The present invention is also described in the claims attached below. 1. Connection where n is 0, 1 or 2; Ar1and Ar2independently selected from the group consisting of unsubstituted aryl groups, and aryl groups substituted by substituents selected from the group consisting of alkyl groups, alkenyl groups, etkinlik groups, alkoxygroup, carboxypropyl and halogen; and R is selected from the group consisting of alkenyl groups, alkyl groups, alkoxygroup, hydroxyalkyl groups and alkylhalogenide groups. 2. The compound according to claim 1, where n=0. 3. The compound according to claim 1, where n=1. 4. The compound according to claim 1, where n=2. 5. The compound according to claim 1, where R represents allyl. 6. The compound according to claim 1, where R represents propyl. 7. The use of compounds according to claim 1 as an agent of nucleation polyolefin-containing composition. 8. The compound according to claim 1, where R is selected from the following compounds: CH3; -CH2CH3; -CH2CH2CH3; -CH2CH2CH2CH3; -CH2CH=CH2; -CH(CH3)CH=CH2; -CH2SN-X-CH2-X'; CH2CH2-X-CH2-CH3; -CH2SN-X"'-CH2HE; -CH-HE-HF-HE-CH2Is HE, where X, X', X ' Is X'", if they are present, are independently selected halide group. 9. The connection of claim 8, where Ar1and Ar2independently selected from the group of substituted benzaldehydes, including benzaldehyde, 4-ethylbenzaldehyde, 4-isobutylbenzene, 4-fluoro-3-methylbenzaldehyde, 5,6,7,8-tetrahydro-2-naphthaldehyde, 3-methylbenzaldehyde, 4-propylbenzamide, 4-butylbenzaldehyde, 4-methoxybenzaldehyde, 3-chlorobenzaldehyde, 3,4-dimethylbenzaldehyde, 3,5-differentally, 3-fermentology, 4-fermentology, 3-bromo-4-fermentology, 3-methyl-4-methoxybenzaldehyde, 2,4,5-trimethylbenzaldehyde, 4-chloro-3-fermentology, 4-methylbenzaldehyde, 3-bromobenzaldehyde, 4-methoxybenzaldehyde, 3,4-dichlorobenzaldehyde, 4-fluoro-3,5-dimethylbenzaldehyde, 2,4-dimethylbenzaldehyde, 4-bromobenzaldehyde, 3-ethoxybenzaldehyde, 4-allyloxymethyl, 3,5-dimethylbenzaldehyde, 4-chlorobenzaldehyde, 3-methoxybenzaldehyde, 4-(trifluoromethyl)benzaldehyde, 2-naphthaldehyde, 4-isopropylbenzaldehyde, 3,4-diethoxybenzene, 3-bromo-4-ethoxybenzaldehyde, piperonal, 3,4-dimethoxybenzaldehyde, 4-carboxybenzoyl, 3-Gex-1-universalized and 2-chlorobenzaldehyde. 10. The connection according to claim 9, where the specified Ar1and Ar2both represent 4-propylbenzamide. 11. Molded or cast polyolefin product containing the compound according to claim 1. any according to claim 1, representing 1,3:2,4 diacetyl substituted alditha. 13. Connection where n is 1; R represents alkenylphenol or alkyl group; each of R1, R2, R3, R4and R5independently selected from the group consisting of hydrogen, alkyl groups, etkinlik groups, alkoxygroup, carboxypropyl and Halogens. 14. The connection indicated in paragraph 13, where the specified R is selected from the following compounds: CH3; -CH2CH3; -CH2CH2CH3; -CH2CH2CH2CH3; -CH2CH=CH2; -CH(CH3)CH=CH2. 15. The connection 14, where R is a-CH2CH=CH2. 16. The connection 14, where R is a-CH2CH2CH3. 17. The connection indicated in paragraph 13, where one of the R1, R2, R3, R4and R5represents alkyl. 18. Acetal substituted Aldata having the structure presented in claim 1, obtained by reaction of compounds (a) and (b), namely: (a) substituted aldinga connection where n is 0, 1 or 2; R is selected from the group consisting of alkenyl groups, alkyl groups, alkoxygroup, hydroxyalkyl groups and alkylhalogenide; and (b) at IU is e 1 mol of substituted or unsubstituted benzaldehyde 1 mol of substituted aldinga connection where specified benzaldehyde is a where each of R1, R2, R3, R4and R5independently selected from the group consisting of hydrogen, alkyl groups, alkenyl groups, etkinlik groups, alkoxygroup, carboxypropyl and Halogens. 19. The method of obtaining subjected to nucleation or brightened polyolefin composition, where the method includes mixing the polyolefin composition with the compound having the structure where n is 0, 1 or 2; Ar1and Ar2independently selected from the group consisting of unsubstituted aryl groups, and aryl groups substituted by substituents selected from the group consisting of alkyl groups, alkenyl groups, etkinlik groups, alkoxygroup, carboxypropyl and halogen; and R is selected from the group consisting of alkenyl groups, alkyl groups, alkoxygroup, hydroxyalkyl groups and alkylhalogenide groups. 20. The method according to claim 19, where the specified R is selected from the following compounds: CH3; -CH2CH3; -CH2CH2CH3; -CH2CH2CH2CH3; -CH2CH=CH2; -CH(CH3)CH=CH2.
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