专利号:US-11512303-B2 优先权日:2017-05-27 标 题 :Engineered polypeptides and their applications in the synthesis of beta-hydroxy-alpha-amino acids 发明人:CHEN HAIBIN; BONG YONG KOY; XU QING; ZHOU AMENG; SHEN TIANRAN; YANG JIADONG; YANG ZHUHONG 权利人:ENZYMASTER NINGBO BIO ENG CO LTD 摘要:The present invention provides engineered polypeptides that are useful for the asymmetric synthesis of β-hydroxy-α-amino acids under industrial-relevant conditions. The engineered polypeptides disclosed in this invention were developed through directed evolution based on the ability of catalytic synthesis of (2S, 3R)-2-amino-3-hydroxy-3-(4-nitrophenyl) propanoic acid. The present disclosure also provides polynucleotides encoding engineered polypeptides, host cells capable of expressing engineered polypeptides, and methods of producing β-hydroxy-α-amino acids using engineered polypeptides. Compared to other processes of preparation, the use of the engineered polypeptides of the present invention for the preparation of β-hydroxy-α-amino acids results in high purity of the desired stereoisomers, mild reaction conditions, low pollution and low energy consumption. So, it has good industrial application prospects.
专利号:US-5684130-A 优先权日:1995-06-05 标题 :Process for synthesis of organic compounds using magnetic particles 发明人:SUCHOLEIKI IRVING 权利人:SOLID PHASE SCIENCES CORP 摘要:This invention provides a process for the synthesis of a defined chemical entity, i.e., any desired chemical compound, in high yield using a solid support comprising a magnetic particle, in organic solvents. In general, a sequence of chemical synthetic steps are required to prepare the defined chemical entity bound to the particle. The particle comprises a resin bearing a high concentration of substituent pendant functional groups, to which the first reagent employed in the synthetic sequence binds; in subsequent reaction steps further reagents react with the growing chemical intermediate bound to the pendant functional groups until the defined chemical entity is obtained. The particle also comprises smaller paramagnetic or superpara-magnetic particles incorporated within the resin. The magnetic particle therefore responds to imposed magnetic field gradients, permitting ease of manipulation in steps involving removal of organic solvent.
专利号:US-5399721-A 优先权日:1990-01-12 标题:Synthesis of optically pure 4-aryl-2-hydroxytetronic acids 发明人:HOPPER ALLEN T; WITIAK DONALD T 权利人:UNIV OHIO STATE RES FOUND 摘要:The present invention relates to a method for synthesis of optically pure stereogenically labile 4-aryl-2-hydroxytetronic acids from an optically pure aldehyde. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase. the invention further relates to the pharmaceutical use of such compounds in the treatment of coronary artery diseases, especially in the treatment and/or prevention of atherosclerosis.
专利号:WO-2012089181-A1 优先权日:2010-12-30 标题 :O-substituted (2r,3r)-3-(3-hydroxyphenyl)-2-methyl-4-pentenoic acids and a method of obtaining the same 发明人:VLASAKOVA RUZENA; HAJICEK JOSEF; ZEZULA JOSEF 权利人:ZENTIVA KS; VLASAKOVA RUZENA; HAJICEK JOSEF; ZEZULA JOSEF 摘要:The compounds of general formula II are new and represent important intermediates in the synthesis of tapentadol. In the synthesis of tapentadol of formula I and its pharmaceutically acceptable salts, O-protected (2R,3R)-acids of general formula II, in step A, are reacted in an inert organic solvent with an activating agent, optionally in presence of a catalyst or a base; in step B, the obtained compounds of general formula V, wherein R has the above mentioned meaning and X stands for chlorine or alkoxycarbonyloxyl group O-CO-OR 1 or pivaloyloxyl O-CO-t-Bu group, wherein R 1 is methyl or ethyl, are reacted with dimethylamine or its salts optionally in presence of a base; in step C, the obtained N, N-dimethylamides of general formula VI, wherein R has the above mentioned meaning, are reduced by means of hydride agents in a suitable solvent; in step D, the produced alkeneamines of general formula VII, wherein R has the above mentioned meaning, are hydrogenated on a metal catalysts in a suitable solvent; and, finally, in step E, the produced alkaneamines of general formula VIII, wherein R has the above mentioned meaning, are O-dealkylated by means of dealkylating agents, and, if required, the obtained tapentadol is converted by the action of a pharmaceutically acceptable acid to respective salts, e.g. hydrochloride.
专利号:US-2001047100-A1 优先权日:2000-04-26 标 题:Chiral imidazoyl intermediates for the synthesis of 2-(4-imidazoyl)-cyclopropyl derivatives 发明人:KJAERSGAARD HANS JOERGEN; PHILLIPS JIM; ALI SYED M 摘要:Novel intermediates useful in the preparation of optically active H 3 histamine receptor antagonist 2-(4-imidazoyl)-cyclopropyl derivatives are disclosed.
专利号:US-6140529-A 优先权日:1998-10-22 标 题 :Synthesis of optically active cyclohexylphenylglycolate esters 发明人:BAKALE ROGER P; LOPEZ JORGE L; MCCONVILLE FRANCIS X; VANDENBOSSCHE CHARLES P; SENANAYAKE CHRIS HUGH 权利人:SEPRACOR INC 摘要:A process for the preparation of optically active cyclohexylphenylglycolate esters is described. The process utilizes carboxylic acid activation to couple (R)- or (S)-cyclohexylphenylglycolic acid (CHPGA) with 4-N,N-diethylamino butynol or other propargyl alcohol derivatives. The preparation of the hydrochloride salt is also described. In addition, a resolution process employing tyrosine methyl ester enantiomers for preparing a single enantiomer of CHPGA from racemic CHPGA is disclosed.