专利号:US-11999757-B2 优先权日:2017-11-01 标 题:Synthesis of boronate ester derivatives and uses thereof 发明人:BOYER SERGE HENRI; HECKER SCOTT J; VERZIJL GERARDUS K M; HERMSEN PETRUS J 权利人:MELINTA SUBSIDIARY CORP 摘要:Disclosed herein are methods for the preparation of boronate derivatives in the synthesis of antimicrobial compounds and uses thereof. Disclosed herein includes method of making a compound of Formula (B) by reducing the ketone group of the keto-ester compound of Formula (A), and the reduction can be performed using a Ruthenium based catalyst system or using an alcohol dehydrogenase bioreduction system.
专利号:US-2025101006-A1 优先权日:2022-01-31 标题:Process for the synthesis of pyrazolyl derivatives useful as anti-cancer agents 发明人:BAENZIGER MARKUS; GALLOU FABRICE; GUO FENGFENG; HÄNGGI RUDOLF; HAN ENJIAN; JORDINE GUIDO; LI JIALIANG; LIU WEIPENG; MIAO BUKEYAN; RONG SHAOFENG; SANTANDREA ERNESTO; SCHIRNER PAUL BERND; SHEN XIAODONG; WANG CAN; ZHANG HAO 权利人:NOVARTIS AG 摘要:The invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially KRAS G12C inhibitors. The present invention provides a direct enantioselective chemical manufacturing method of making Compound A, or a pharmaceutically acceptable hydrate or solvent thereof: (I). The invention provides a process for preparing Intermediate B6* comprising reacting Intermediate B4* with Intermediate B5* in an atroposelective coupling reaction, using a chiral catalyst.
专利号:US-7399773-B2 优先权日:2001-01-09 标 题 :Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid and phenylamide 发明人:NELSON JADE DOUGLAS; PAMMENT MICHAEL GERARD 权利人:WARNER LAMBERT CO 摘要:An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide by a novel synthesis is described where methyl cyanoacetate is converted in eight operations or fewer to the desired product, as well as other valuable intermediates used in the process.
专利号:US-8835658-B2 优先权日:2012-12-28 标 题:Asymmetric synthesis of norcantharidin analougus by alkynylation of oxabenzonorbornadienes and their anticancer activities 发明人:CHAN ALBERT SUN-CHI; FAN BAOMIN; WANG JUN; LIN CHENGYUAN; HUANG CHAO; YANG QINGJING; XU JIANBIN; BIAN ZHAOXIANG; LU AIPING; HU JUN 权利人:UNIV HONG KONG BAPTIST; UNIV YUNNAN NATIONALITIES 摘要:The present invention relates to a type of norcantharidin analogues and a method to synthesis such norcantharidin analogues by transition metal-catalyzed alkynylation of 7-oxabenzonorbornadienes. The present invention also relates to the use of such norcantharidin analogues in manufacture of a medicament for the treatment of cancer tumors.
专利号:US-2009088576-A1 优先权日:2006-01-30 标题:Process for the Stereoselective Preparation of Alcohols From Alpha, Beta-Insaturated Compounds 发明人:HEROLD PETER; STUTZ STEFAN; MAH ROBERT; STOJANOVIC ALEKSANDAR; LYOTHIER ISABELLE; BEHNKE DIRK; SPINDLER FELIX; BAPPERT ERHARD 权利人:HEROLD PETER; STUTZ STEFAN; MAH ROBERT; STOJANOVIC ALEKSANDAR; LYOTHIER ISABELLE; BEHNKE DIRK; SPINDLER FELIX; BAPPERT ERHARD 摘要:A process for the synthesis of an alcohol of formula (I), using as intermediate a compound of formula (V).
专利号:US-2008207950-A1 优先权日:2004-12-22 标 题:Enantioselective Synthesis of a Sterically Hindered Amine 发明人:BERENS ULRICH; MALAN CHRISTOPHE; KIRNER HANS JURG 权利人:CIBA SC HOLDING AG 摘要:Compounds of the formula (I) wherein R is phenyl, or phenyl substituted by Cl, Br, C 1 -C 4 alkyl or CF 3 ; R 1 is H or methyl or ethyl; R 2 is H or methyl or acyl; R 3 is H or methyl; R′ 4 is —CH 3 or â•?CH 2 ; may be obtained in high enantiopurity by hydrogenation of a compound of the formula (II) wherein R and R 3 are as in formula (I); A is acyl; and R 4 is —CH 3 or â•?CH 2 ; in the presence of a chiral Rhodium or Ruthenium catalyst. Residues R 1 as methyl or ethyl and/or R 2 as H or methyl may subsequently be introduced without racemization by deacylation and optional alkylation.