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1644results about How to "High optical purity" patented technology

Process for preparing optically active compounds

This document describes a novel and practically excellent process for the preparation of optically active compounds, such as optically active alcohols or amines which are useful for various applications, for example, as synthetic intermediates of pharmaceuticals, liquid crystal materials, and reagents for optical resolution, wherein a hydrogen transfer type asymmetric reduction is carried out in the presence of both a transition metal complex and an optically active nitrogen compound or a transition metal complex having an optically active nitrogen compounds as an asymmetric ligand, and a hydrogen-donating organic or inorganic compound.
Owner:ASAHI KASEI PHARMA +4

Resin Composition and Molded Article Comprising the Same

A resin composition in which a polylactic acid resin (A) 95-5 wt %, an aromatic polycarbonate resin (B) 5-95 wt %, and, with respect to 100 wt parts of the total of the (A) and the (B), at least one compatibilizer selected from a polymer compound containing an acrylic resin or styrene resin unit as a graft (C), a polymer compound to which a glycidyl compound or an acid anhydride is grafted or copolymerized (D) and an oxazoline compound, an oxazine compound and a carbodiimide compound (E) are compounded.
Owner:TORAY IND INC

Method for preparing clopidogrel and its derivatives

The present invention relates to a method for preparing Clopidogrel and its derivatives. More particularly, the present invention is a method for preparation of (S)-2-Clopidogrel and its derivatives, which are active inhibitors of platelet aggregation, from an optically active (S)-2-chlorophenyl glycine alkyl ester through hydrolysis of racemic 2-chlorophenylglycine alkyl esters using an enzyme. The present invention employs a simple procedure to prepare Clopidogrel and its derivatives. Because no chiral resolving agents are used except for a small amount of enzyme, the cost of preparation can be reduced. In addition, the present invention is suitable for synthesizing highly optical-active Clopidogrel and its derivatives on a large scale by using optically active (S)-2-chlorophenylglycine alkyl ester obtained in high yield as an intermediate, and is also environmentally friendly since no highly toxic reagents are employed.
Owner:ENZYTECH LTD

Resin Composition and Molded Article Composed of the Same

A resin composition comprising a polylactic acid-based resin (A) and methacrylic resins (B), wherein the methacrylic resins having at least (a) a difference of 10° C. or more in glass transition temperature or (b) a difference of 3% or more in syndiotacticity; it is preferred that at least one of the methacrylic resins (B) is a methacrylic resin having a weight average molecular weight of 50,000 to 450,000, a glass transition temperature of 110° C. or higher and a syndiotacticity of 40% or more, and that the resin composition further contains a multilayer structure polymer formed as particles each consisting of a core layer and one or more shell layers covering it (C) A molded article made of said resin composition.
Owner:TORAY IND INC

Carbonyl reductase, gene and mutant and application thereof to asymmetrical reduced carbonyl compound

The invention discloses a novel carbonyl reductase, a gene, a mutant thereof, a recombinant expression vector containing the gene and the mutant, a recombinant expression transformant, a recombinase preparation method, and applications of the carbonyl reductase and recombinase to preparation of active chiral alcohols with a chiral carbonyl compound before asymmetrical reduction. The carbonyl reductase is derived from candida glabrata, is applied to preparation of a plurality of optically-active chiral alcohols such as (R)-chloromandelic acid methyl ester, (R)-2-hydroxy-4-phenyl ethyl butyrate, (R)-4-chlorin-3-phenyl ethyl butyrate and the like. Compared with other preparation methods, a product prepared through the method has high concentration, does not require additionally or slightly adding any expensive coenzyme, has high optical purity, and has the advantages of mild reaction conditions, easiness and convenience for operating, easiness for amplifying and the like, and has a good industrial application prospect in the production of clopidogrel, L-carnitine and perindopril antihypertensive medicinal intermediates.
Owner:EAST CHINA UNIV OF SCI & TECH

Novel intermediate for synthesizing treprostinil diethanolamine and method for preparing the same

The present invention relates to a method for treprostinil diethanolamine synthesis. The present invention also relates to a novel intermediate used in the method for treprostinil diethanolamine synthesis. The novel intermediate is shown in the following formula (II):wherein R1 and R2 are described in the description.
Owner:EVERLIGHT CHEMICAL INDUSTRIAL CORPORATION

Method for producing L-lactic acid by Bacillus coagulans CGMCC No.2602

A method for producing L-lactic acid by Bacillus coagulans CGMCC No.2602 belongs to the technical field of microorganisms. In the invention, Bacillus coagulans CGMCC No.2602 is adopted, and under the condition of no oxygen supply, starchiness hydrolyzed sugar or dextrose is fermented by a semicontinuous intermittent fermentation way or an inter-sugar-compensating fermentation way to generate L-lactic acid with high optical purity. The invention has the advantages that the gemma property of the Bacillus coagulans is stable, and the L-lactic acid obtained by inoculating and fermenting the starchiness hydrolyzed sugar has high optical purity and rate of conversion of sugar and acid and short fermentation period; in addition, the semicontinuous intermittent fermentation way saves the time for preparing seeds by a continuous reladling and subculturing method, shortens the fermentation period, enhances the fermentation strength and obtains the L-lactic acid with both relatively high rate of conversion of sugar and acid and purity.
Owner:江苏省苏微微生物研究有限公司

Preparation method of dezocine

The invention provides a preparation method of dezocine, which has the following advantages: (1) when an intermediate which is dezocine-1 is used as a raw material to prepare another intermediate which is dezocine-2, the obtained oxidants are acid peroxide, alcohol peroxide or hydrogen peroxide which have low cost and are easy to obtain and post-process; (2) when the intermediate which is dezocine-2 is used as a raw material to prepare an intermediate which is dezocine-3, the obtained bases are bases which have low cost and are easy to obtain; (3) when an intermediate which is dezocine-6 is used as a raw material to prepare an intermediate which is dezocine-6b, an optically pure chiral organic acid and an racemic intermediate which is the dezocine-6 react for generate a pair of diastereomeric salts, and then the pair of diastereomeric salts are separated through recrystallization to obtain the intermediate which is the dezocine-6 with high optical purity; and (4), the operation is simple and efficient, the reaction condition is mild, and the used reagents are cheap, readily available, highly safe and suitable for industrial mass production.
Owner:JIANGSU HAICI BIOLOGICAL PHARMA CO LTD OF YANGTZE RIVER PHARMA GRP +1

Method for preparing (S)-(4-chlorphenyl)-(pyridine-2-yl)-methanol by utilizing microbial catalysis

The invention relates to a method for preparing (S)-(4-chlorphenyl)-(pyridine-2-yl)-methanol by utilizing microbial catalysis, and belongs to the technical field of biological catalysis. According to the method, 4-chlorphenyl-(pyridine-2-yl)-ketone is subjected to asymmetrical reduction by utilizing kluyveromycessp (CCTCCM 2011385) whole cells to synthesize the (S)-(4-chlorphenyl)-(pyridine-2-yl)-methanol. The method comprises the following steps of: sieving a microbe which has high-stereoselectivity carbonyl reductase activity on a prochiral ketone substrate, determining a series of conditions of asymmetrical reduction reaction, such as reaction temperature, pH, the concentration of cells, the concentration of the substrate and reaction time and additives (including various secondary solvents, polyethyleneglycol (PEG), phosphates and the like), wherein the enantiomer excess value and yield of the (S)-(4-chlorphenyl)-(pyridine-2-yl)-methanol serving as a product can reach 86.7 percent e.e and 92.1. The product is separated and extracted initially by silicagel column chromatography, so that the purity of the separated product is 99.2 percent, and the extraction yield is 56.7 percent.
Owner:JIANGNAN UNIV

Asymmetric synthesis method of (+)-tanshinol

The invention relates to an asymmetric synthesis method of (+)-tanshinol, which comprises the following steps: carrying out Knoevenagel condensation on the raw material heliotropin, hydrolyzing for ring opening to obtain beta-(3,4-3,4-methylenedioxyphenyl)pyruvic acid, carrying out key asymmetric reduction reaction to obtain R-beta-(3,4-dibenzyloxyphenyl)-alpha-hydracrylic acid, and finally, deprotecting to obtain the (+)-tanshinol. The method has the advantages of accessible raw material and high optical purity of the product, is simple to operate, and can implement large-scale preparation.
Owner:FOURTH MILITARY MEDICAL UNIVERSITY

Preparation method of brivaracetam

The invention provides a method for synthesizing brivaracetam. Raw materials used in the method are available and inexpensive, a preparation process avoids appearance of chiral isomers difficult to separate, purification means such as column chromatography purification and the like adverse to industrial amplification production is avoided, a synthesis process is not involved with expensive and toxic heavy metal and chiral ligands, and a product brivaracetam with high quality and high optical purity can be obtained.
Owner:SUZHOU PENGXU PHARM TECH CO LTD +1

Preparation method for optical activity active 3-amino butanol and optical activity 3-amino butyric acid

The present invention discloses a preparation method for optical activity active 3-amino butanol and optical activity 3-amino butyric acid. The optical activity active 3-amino butanol preparation method comprises: in a solvent, under effects of a hydroboration reduction agent and a Lewis acid, carrying out a reduction reaction on a compound represented by a formlu 65 to produce a compound represented by a formlu 14. The optical activity active 3-amino butyric acid preparation method comprises: carrying out a hydrolysis reaction on a compound represented by a formlu 64 to produce a compound represented by a formlu 65. According to the present invention, the preparation method has characteristics of cheap and easily-available raw materials, simple operation, short process route, no hazard of raw materials, high yield, little waste production, environment protection, high raw material conversion rate, high product chemical purity and high product optical purity, and the industrialization is easily achieved. The formulas 64, 65 and 14 are defined in the instruction.
Owner:JIANGXI LONGLIFE BIO PHARM CO LTD +1

Method for preparing high optical purity pitavastatin calcium raw material drug

The invention relates the method of preparing the raw material of high optical purity pravastatin calcium. The method comprises the following steps: adding the 2- cyclopropyl-4-(4- fluorophenyl)-3-quinoline aldehyde II and (3R)-3- alkoxy silane-5- carbonyl-6- triphenyl phosphor heptene acid ester III in dissolvent, getting (E)-7- [2-2- cyclopropyl-4-(4- fluorophenyl)-3- chinoline]-5- carbonyl-(3R)-3- alkoxy silane-6- triphenyl phosphor heptene acid ester IV, removing the protection of IV, getting (E)-7- [2-2- cyclopropyl-4-(4- fluorophenyl)-3- chinoline]-5- carbonyl-(3R)- hydroxyl -6- triphenyl phosphor heptene acid ester V, deacidizing it in the mixture dissolvent of alcohol and ether with NaBH4 or KBH4 at -100-0Deg.C, getting (E)-7- [2-2- cyclopropyl-4-(4- fluorophenyl)-3- chinoline]-(3R, 5S)- dihydroxy -6- triphenyl phosphor heptene acid ester VI, hydrolyzing it with alkali, and getting pravastatin calcium. The material is used to prepare HMG-CoA reductase inhibiting agent.
Owner:CHINA RESOURCES DOUBLE CRANE PHARMA COMPANY

Method for catalyzing dynamic kinetic resolution of arylamine via racemization catalyst

The invention discloses a method for catalyzing dynamic kinetic resolution of arylamine via a racemization catalyst, comprising the following steps of: 1) adding p-chlorophenol, n-pentanoic acid, dicyclohexylcarbodiimide and 4-dimethylamino-pyridine, and carrying out mixing, filtration, drying, concentration and column chromatography to obtain a pentanoic acid p-chlorophenyl ester acyl donor; 2) carrying out coprecipitation on magnesium chloride solution and aluminum chloride solution and carrying out water-heat treatment to obtain chloridion intercalated hydrotalcite, adding the chloridion intercalated hydrotalcite in lauryl sodium sulfate aqueous solution, and carrying out backflow, cooling, centrifugation, water washing, acetone washing and drying to obtain a carrier; 3) adding palladium salt and the carrier, and carrying out heating, ascorbic acid addition, centrifugation, water washing, acetone washing and freeze-drying to obtain the racemization catalyst; and 4) adding arylamine, the acyl donor, lipase and the racemization catalyst in toluene and placing in a stainless steel reactor to add hydrogen so as to obtain amide. The method provided by the invention is used for catalyzing the dynamic kinetic resolution of arylamine, has rapid reaction rate, low temperature, high conversion rate and high product optical purity, and has great application value.
Owner:ZHEJIANG UNIV

Carbonyl reductase, gene and applications of carbonyl reductase in asymmetric reduction of prochiral carbonyl compound

The invention discloses applications of carbonyl reductase being as a catalyst in the preparation of chiral alcohol by asymmetric reduction of a prochiral carbonyl compound, and a gene, protein and a mutant of the carbonyl reductase. The invention also provides a recombinant expression vector and a recombinant expression transformant containing the gene of the carbonyl reductase. When the carbonyl reductase disclosed by the invention is utilized for catalyzing the asymmetric reduction reaction of the prochiral carbonyl compound, the reaction conditions of the asymmetric reduction are moderate, the operation process is simple and convenient, and the amplification is easy; and the chiral alcohol product prepared by the asymmetric reduction reaction is high in concentration and optical purity. Therefore, the carbonyl reductase has a good industrial application and development prospect in the preparation of the optically pure chiral alcohol.
Owner:EAST CHINA UNIV OF SCI & TECH

New benzocyclobutane, preparation method thereof and application thereof

The invention relates to new benzocyclobutane, a preparation method thereof and application thereof. The invention provides a new preparation method for (1S)-4, 5-dimethoxy-1-(methyl-amino-methyl)-benzocyclobutane serving as a key intermediate of ivabradine hydrochloride and addition salt thereof, and meanwhile provides a new benzocyclobutane compound which is an intermediate for preparing the (1S)-4, 5-dimethoxy-1-(methyl-amino-methyl)-benzocyclobutane. In addition, the invention also provides a method for preparing the new benzocyclobutane compound, and meanwhile provides a method for splitting an intermediate product during preparing the new benzocyclobutane compound.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI +1

Preparation method of key intermediate of rosuvastatin calcium side chain

The invention provides a preparation method of a key intermediate of a rosuvastatin calcium side chain, comprising the following steps: using (S)-4-chlorine-3-hydroxybutanoate as an initial raw material; and preparing the key intermediate through four-step reactions of condensation, reduction, hydroxy group protection and condensation. The reaction process is simple to operate, the products in each step are easy to separate and purify, the purification and separation step is carried out without a silicagel column, and the yield is more than 80 percent, therefore, the intermediate with higher chemical purity and optical purity can be obtained. The GC determination shows that the chemical purity is more than or equal to 99.5 percent and the optical purity is more than or equal to 99.2 percent ee.
Owner:LUNAN PHARMA GROUP CORPORATION

Synthetic methods of chiral aryloxy propanol amine compounds and salts thereof

The invention relates to a synthesis method of chiral aryloxy propanol amine compound and salts thereof, which pertains to chemical pharmacy field. The method of the invention takes chiral source (R or S) halogenated propylene oxide and phenol compound as initial raw materials, (R or S) aryloxy propanol amine compound of high optical purity is obtained through etherification reaction and amination reaction, and the method of the invention can be applied to the preparation of various salts or compounds through salt forming reaction. The products of the invention usually has the characteristics of retarder of beta adrenoceptor and can be used as medicaments for curing diseases such as high blood pressure, angina pectoris, cardiac neurosis, arrhythmia and glaucoma, etc.
Owner:HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY

Intermediate for synthesizing treprostinil diethanolamine and method for preparing the same

The present invention relates to a method for treprostinil diethanolamine synthesis. The present invention also relates to a novel intermediate used in the method for treprostinil diethanolamine synthesis. The novel intermediate is shown in the following formula (II):wherein R1 and R2 are described in the description.
Owner:EVERLIGHT CHEMICAL INDUSTRIAL CORPORATION

Non-enantioselective prepn process of emtricitabine

The present invention discloses non-enantioselective preparation process of emtricitabine. The preparation process includes condensation of glyoxalic acid as the initial material and 2, 5-dihydroxy-1, 4-dithiane under the asymmetric induction of optically active alcohol ester to obtain trans-5-hydroxy-1, 3-oxythiacyclopentane-2-carboxylate; halogenating and coupling with silylated 5-flucytosine, and reducing to obtain initial product; reaction with salicylic acid to form salt, purification and separation to obtain optically pure emtricitabine. The present invention has mild reaction condition, simple operation, low cost, less environmental pollution and high product purity reaching medicinal standard, and is suitable for industrial production. The product is used in treating hepatitis B and AIDS.
Owner:葛建利

High optical purity copolymer film

The invention relates to a high optical purity toughened copolymer film or coating. The copolymer is a graft or block copolymer, preferably acrylic, preferably produced by a controlled radical polymerization having an extremely low degree of particulate contamination and excellent optical properties. The film or coating is preferably formed by solvent-casting on a temporary substrate or solvent-coating on a permanent substrate.
Owner:TRINSEO EURO GMBH

Process for producing optically active 2-substituted carboxylic acid

The present invention relates to a process for efficiently producing an optically active 2-bromocarboylic acid and an optically active 2-sulfonyloxycarboxylic acid, which are important in the production of medicinal compounds and so forth. An optically active 2-sulfonyloxycarboxylic acid ester is subjected to deprotection under acid conditions to obtain an optically active 2-sulfonyloxycarboxylic acid. A metal bromide is caused to act on the acid to brominate it with configuration inversion at position 2 to thereby produce an optically active 2-bromocarboxylic acid. The resultant optically active 2-bromocarboxylic acid is isolated / purified by subjecting it to a step in which the acid is crystallized and separated as a salt with a base. Thus, an optically active 2-bromocarboxylic acid having a high chemical purity and high optical purity can be produced.
Owner:KANEKA CORP

High-purity lactide and preparation method thereof

The invention discloses high-purity lactide and a preparation method thereof. The preparation method comprises the steps of raw material addition, free water removal, polycondensation, depolymerization, distillation and secondary distillation. The raw material addition step refers to that a catalyst is added into L-lactic acid or D-lactic acid, wherein the catalyst is one or more of zinc oxide, stannous oxide and stannous octoate. In the preparation process, the use of an organic solvent, N2 and inert gas and environmental pollution are avoided, the vacuum degree is moderate, purification loss is reduced, the production cost is reduced, and the method is suitable for industrial production. The L-lactide or D-lactide product prepared by the method is high in yield, optical purity and quality, the yield is more than or equal to 97 percent, and the optical purity of the purified lactide is 99.45 percent or above.
Owner:SHANDONG SHOUGUANG JUNENG GOLDEN CORN CO LTD
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