专利号:US-7452994-B2 优先权日:2001-09-12 标 题 :Synthesis of enantiomerically pure amino-substituted fused bicyclic rings 发明人:MCEACHERN ERNEST J; BRIDGER GARY J; SKUPINSKA KRYSTYNA A; SKERLJ RENATO T; YANG WEN 权利人:ANORMED INC 摘要:This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepares the racemic amino-substituted fused bicyclic ring system via nitrosation. In addition, the present invention describes the enzymatic resolution of a racemic mixture to produce the (R)- and (S)-forms of amino-substituted fused bicyclic rings as well as a racemization process to recycle the unpreferred enantioner. Further provided by this invention is an asymmetric synthesis of the (R)- or (S)-enantiomer of primary amino-substituted fused bicyclic ring systems.
专利号:WO-2008132128-A3 优先权日:2007-04-27 标 题:Synthesis of a pharmaceutically active compound 发明人:WIESENHOEFER WOLFGANG; BUYLE OLIVIER; CALLENS ROLAND; GIRE ROMAN; POUSSET CYRILLE; JEANNIN LAURENT 权利人:SOLVAY; WIESENHOEFER WOLFGANG; BUYLE OLIVIER; CALLENS ROLAND; GIRE ROMAN; POUSSET CYRILLE; JEANNIN LAURENT 摘要:Process for the manufacture of UK- 427,857 ( Maraviroc ) which comprises a step wherein enantiopure (S)-3-amino-3-phenylpropan-1-ol is manufactured from a mixture of its enantiomers by crystallizing or precipitating from a solution containing the mixture of enantiomers of 3-amino-3-phenylpropan-1-ol, an enantiopure resolving agent and a solvent, a diastereomeric salt or complex of 3-amino-3-phenylpropan-1-ol with the resolving agent, said salt or complex being enriched in the (S)-enantiomer of 3-amino-3-phenylpropan-1-ol. Difluorocyclohexan oic acid derivatives useful in the process can be obtained by a process comprising subjecting an oxocyclohexanoic acid ester to reaction with an activated fluorocarboxylic acid derivative and fluorinating the obtained intermediate to obtain a difluorocyclo hexanoic acid ester.
专利号:US-10533028-B2 优先权日:2014-09-04 标 题:Ruthenium complexes and their uses as catalysts in processes for formation and/or hydrogenation of esters, amides and related reactions 发明人:MILSTEIN DAVID; HU PENG; FOGLER ERAN; RAO JAI ANAND GARG NARAYANA 权利人:YEDA RES & DEV 摘要:The present invention relates to novel Ruthenium complexes of formulae A1-A4 and their use, inter alia, for (1) dehydrogenative coupling of alcohols to esters; (2) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones), or polyesters); (3) preparing amides from alcohols and amines—(including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or polymerization of amino alcohols and/or forming cyclic dipeptides from p-aminoalcohols; (4) hydrogenation of amides (including cyclic dipeptides, polypeptides and polyamides) to alcohols and amines; (5) hydrogenation of organic carbonates (including polycarbonates) to alcohols or hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (6) dehydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e., synthesis of amides from esters and amines); (8) acylation of alcohols using esters; (9) coupling of alcohols with water and a base to form carboxylic acids; and (10) preparation of amino acids or their salts by coupling of amino alcohols with water and a base. The present, invention further relates to the use of certain known Ruthenium complexes for the preparation of amino acids or their salts from amino alcohols.
专利号:WO-2025050656-A1 优先权日:2023-09-04 标 题 :Method and biomaterial for total biosynthesis of paclitaxel precursor substance baccatin iii, and use 发明人:YAN JIANBIN; JIANG BIN; SUN YAPING; HUANG SANWEN 权利人:AGRICULTURAL GENOMICS INST AT SHENZHEN CHINESE ACADEMY OF AGRICULTURAL SCIENCES SHENZHEN BRANCH GUAN; AGRICULTURAL GENOMICS INST CHINESE ACADEMY OF AGRICULTURAL SCIENCES 摘要:A method and a biomaterial for the total biosynthesis of a key paclitaxel precursor substance baccatin III, and the use. The biological enzyme composition used in the method comprises taxane 9α-hydroxylase (T9αH) and taxane C4-C20 oxetane-forming enzyme (TOT). The core ingredients of the biosynthetic pathway of baccatin III are identified, and an artificial synthesis route for baccatin III is constructed, which pave the way for the efficient development of a green and low-carbon production pathway for taxane products such as paclitaxel by means of synthetic biology.
专利号:WO-2011161690-A1 优先权日:2010-06-23 标题:Processes for the preparation of (+)-n,n-dimethyl-2-[1-(naphthalenyloxy) ethyl] benzene methanamine and intermediates thereof 发明人:MOHAN RAO DODDA; KRISHNA REDDY PINGILI; JITHENDER AADEPU; VENUGOPAL BINGI 权利人:SYMED LABS LTD; MOHAN RAO DODDA; KRISHNA REDDY PINGILI; JITHENDER AADEPU; VENUGOPAL BINGI 摘要:The present invention relates to processes for the preparation of S(+)-N,N-dimethyl-2-[1-(naphthalenyloxy)ethyl]benzene methanamine and intermediates thereof. More particularly the present invention relates to preparation of the compound 3(S)-(+)-N,N-dimethylamino-3-phenyl propanol useful as intermediate in the synthesis of pharmaceutically active compounds.
摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 88. 摘要:Barsegyan, Y. A.; Vil’, V. A.; Tomkinson, N. C. O.; Terent’ev, A. O., Science of Synthesis Knowledge Updates, (2022) 1, 264.