1637results about How to "High optical purity" patented technology

An objective of the present invention is to provide methods for efficiently producing (S)-1-(3,4-dimethoxyphenyl)-2-propanol at a high optical purity. Another objective is to provide novel reductases which reduce 3,4-dimethoxyphenylacetone, using NADPH as a coenzyme, to produce (S)-1-(3,4-dimethoxyphenyl)-2-propanol with a high optical purity.The inventors found that a 3,4-dimethoxyphenylacetone-reducing enzyme present in Torulaspora delbrueckii is a novel carbonyl reductase that reduces various carbonyls. This novel enzyme reduces 3,4-dimethoxyphenylacetone in a reduction reaction to produce (S)-1-(3,4-dimethoxyphenyl)-2-propanol with a high optical purity and at a high yield. Furthermore, the inventors isolated a DNA that encodes the present enzyme, and generated a recombinant bacterium which highly expresses the present enzyme. Thus, the present inventors established a simple and highly economical method of obtaining optically active alcohols with a high optical purity and at a high yield.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

The present invention provides compounds represented by formulas II and IV. The invention further provides uses of the compound represented by the formula II in synthesis of brivaracetam, and a synthesis method. According to the present invention, the used raw materials are easy to obtain and have low price, and the high optical-purity brivaracetam can be prepared. The formulas II and IV are defined in the specification.

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.

The present invention relates to chiral salen catalysts and a process for preparing chiral compounds from racemic epoxides by using them. More particularly, the present invention is to provide chiral salen catalysts and its use for producing chiral compounds such as chiral epoxides and chiral 1,2-diols economically in high yield and high optical purity by performing stereoselective hydrolysis of racemic epoxides, wherein the chiral salen catalyst comprises a cationic cobalt as a center metal of chiral salen ligand and counterions having weak nucleophilic property to resolve disadvantages associated with conventional chiral salen catalysts, and can be used continuously without any activating process of used catalysts because it does not loose a catalytic activity during the reaction process.