专利号:US-2011130591-A1 优先权日:2009-06-03 标 题:Steroselective synthesis of certain trifluoromethyl-substituted alcohols 发明人:FANDRICK DANIEL R; REEVES JONATHAN T; SONG JINHUA J 权利人:BOEHRINGER INGELHEIM INT 摘要:A process for synthesis of a compound of Formula (X) n n n n n n n n n n wherein:n R 1 is an aryl group substituted with one to three substituent groups,n wherein each substituent group of R 1 is independently C 1 -C 5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, halogen, carboxy, cyano, or trifluoromethyl,n wherein each substituent group of R 1 is optionally independently substituted with one to three substituents selected from C 1 -C 3 alkyl, C 1 -C 3 alkoxy, phenyl, and alkoxyphenyl; and n n R 2 and R 3 are each independently C 1 -C 5 alkyl.
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-2024010638-A1 优先权日:2020-11-13 标题:Improved synthesis of crac channel inhibitors 发明人:STAUDERMAN KENNETH; DUNN MICHAEL; OLMSTEAD KAY 权利人:CALCIMEDICA INC 摘要:Provided herein is an improved synthetic method for the production of CRAC channel inhibitors. The synthetic method provides a method for producing highly pure CRAC channel inhibitors for clinical testing.
专利号:US-9328061-B2 优先权日:2012-03-01 标题:Simple organic molecules as catalysts for practical and efficient enantioselective synthesis of amines and alcohols 发明人:HOVEYDA AMIR H; SILVERIO DANIEL L; PILYUGINA TATIANA; TORKER SEBASTIAN; ROBBINS DANIEL 权利人:TRUSTEES BOSTON COLLEGE 摘要:The present invention provides organic molecules and methods thereof for reactions between organoboron reagents and double bonds, such as imines or carbonyls, to stereoselectively provide chiral products including amines and alcohols, entities useful for the preparation of biologically active molecules.
专利号:US-2012289733-A1 优先权日:2011-05-11 标 题 :Novel borate derivatives and their applications 发明人:HEISE GLENN L; MYSLINSKA MALGORZATA 权利人:HEISE GLENN L; MYSLINSKA MALGORZATA; ANDERSON DEV CO 摘要:Borates, compositions comprising chiral (cyclic and acyclic) and achiral (cyclic and acyclic) borates; chiral (cyclic and acyclic) and achiral (cyclic and acyclic) biborates; and methods for their synthesis. Additionally, a significantly improved synthetic protocol for the synthesis of wide range of boronates starting from borates or biborates and Grignard or organolithium reagents that can be used for kilo lab and commercial scale production.
专利号:WO-2023143605-A1 优先权日:2022-01-31 标 题:Process for the synthesis of pyrazolyl derivatives useful as anti-cancer agents
摘要:Delvos, L. B.; Oestreich, M., Science of Synthesis Knowledge Updates, (2017) 1, 70. 摘要:Vaultier, M.; Pucheault, M., Science of Synthesis Knowledge Updates, (2012) 4, 311. 摘要:Naka, H.; Saito, S., Science of Synthesis Knowledge Updates, (2010) 4, 73. 摘要:Littke, A., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 239. 摘要:Miyagishi, H. V.; Nagaki, A., Science of Synthesis: Knowledge Updates, (2024) 1, 206.