专利号:US-10337033-B2 优先权日:2016-12-30 标 题 :Carbonyl reductase oligomers and their application in synthesis of chiral alcohols 发明人:ZHANG RONGZHEN; XU YAN; LI KUNPENG 权利人:ZHANG RONGZHEN; XU YAN; LI KUNPENG; UNIV JIANGNAN 摘要:Disclosed are methods for the synthesis of chiral alcohols by Sortase A-mediated oxidoreductase oligomers, which relates to the field of biocatalysis. In the present disclosure, oxidoreductase oligomers were used as biocatalysts for chiral alcohol preparation. Compared to wild-type enzymes, the oxidoreductase oligomers significantly improved catalytic activity and thermal stability. The sortase A-mediated oxidoreductase oligomers had 6-8 folds improvement in specific activity over that of the wild-type enzymes. The oligomers displayed a T m value 6-12° C. higher than that of the wild-type, suggesting the sortase A-mediated oxidoreductase oligomers significantly improved thermostability of the enzymes. The oxidoreductase oligomers catalyzed asymmetric transformation to produce (S)-1-phenyl-1,2-ethanediol or (R)-1-phenethyl alcohol within 3-6 hr, with an optical purity of 98%-100% and a yield of 98%-99%.
专利号:US-6384228-B2 优先权日:1998-05-26 标题 :Method for synthesis of halopyridyl-azacyclopentane derivative and intermediate thereof 发明人:NODE MANABU; NAKAMURA DAISAKU; FUJIWARA TOSHIO; ICHIHASHI SHOGO 权利人:NIHON MEDIPHYSICS CO LTD 摘要:The present invention relates to a method for synthesis of an optically active halopyridyl-azacyclo-pentane derivative and the intermediate thereof which comprises preparing an optically active allene-1,3-dicarboxylic acid ester derivative from an optically active acetonedicarboxylic acid ester derivative and then proceeding through a 7-azabicyclo[2.2.1]heptane derivative to obtain the objective product.
专利号:US-6469133-B2 优先权日:1999-12-13 标题 :Process for the preparation of polymers of dimeric cyclic esters 发明人:BAKER GREGORY L; SMITH III MILTON R 权利人:UNIV MICHIGAN STATE 摘要:The present invention provides a process for the direct synthesis of high melting polymers made from dimeric cyclic esters. In particular, the present invention provides a process for synthesis of polylactic acid (PLA) from racemic materials such as racemic lactide and polymandelide from mandelide. The process further provides racemic metal organic ligand catalysts such as racemic salbinap that catalyzes the polymerization of racemic dimeric cyclic ester monomers to a polylactide stereocomplex. Polymandelide and mixed dimeric cyclic esters are also prepared in the presence of low amounts of water.
专利号:US-2009093630-A1 优先权日:2007-09-21 标题:Chiral synthesis of diazepinoquinolines 发明人:MEGATI SREENIVASULU; BHANSALI SHILPA; DEHNHARDT CHRISTOPH; DESHMUKH SUBODH; FUNG PETER; MACEWAN MICHAEL; TINDER ROBERT J 权利人:WYETH CORP 摘要:The present invention relates to improved methods of resolution and recrystallization for synthesizing compounds useful as 5HT 2C agonists or partial agonists, including intermediates thereto.
专利号:US-8168828-B2 优先权日:2007-06-25 标题 :Process for the preparation of pregabalin 发明人:SATYANARAYANA REDDY MANNE; THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; SATYANARAYANA REVU 权利人:SATYANARAYANA REDDY MANNE; THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; SATYANARAYANA REVU; MSN LAB LTD 摘要:The present invention encompasses novel intermediates of pregabalin, namely 3-cyano-5-methyl hexanamide (28) and 3-(amino methyl)-5 methyl hexanamide (29), and processes for their preparation. The invention also encompasses a process for converting the novel pregabalin intermediates into pregabalin, Formula (I): The present invention further provides a cost effective method for the synthesis of (S)-pregabalin, which involves the recovery of mandelic acid and tartaric acid used in the resolution process and recycling them, increasing the yields of the final product formed, which substantially reduced the cost of the production.
专利号:US-5097051-A 优先权日:1989-02-10 标题 :Cyclic triketone compounds and trimethylsilyloxy butadiene compounds and their use in the preparation of daunomycinone derivatives 发明人:SCHEEREN JOHAN W; DEBIE JOANNES F M; DEVOS DIRK 权利人:PHARMACHEMIE BV 摘要:The invention provides novel cyclic triketone compounds of the formulae wherein S is H, alkyl or alkoxy and R* is a group of the formule wherein R<1> is methyl and R2 is an alkyl group containing at least 2 carbon atoms, or R<1> is an alkyl group having 1-4 carbon atoms and R<2> is an aryl group, a hetero aryl group, a -CH2OR min , a -CH2N @@ group, a -CH2SR sec group or a -CH2CH=CH2 group, wherein R min and R sec are alkyl groups having 1-4 carbon atoms. These compounds can be used for preparing daunomycinone and derivatives thereof. Daunomycinone is used for preparing daunomycin and adriamycin. By introducing chirality at C-1 of ring A in the preparation of said novel compounds by using a novel diene of formula (1) in a Diels-Alder reaction for said preparation, the chirality of C-3 is established in the subsequent reaction with LiC IDENTICAL CSi(CH3)3 in the synthesis of daunomycinone and derivatives thereof. This last reaction leads to the desired compound wherein OH at C-3 and OR at C-1 are in the cis-position with respect to each other.