专利号:US-2025179012-A1 优先权日:2022-03-04 标 题:Synthesis of sulfur(vi) compounds and reagents for same 发明人:LOPCHUK JUSTIN MATTHEW; SHULTZ ZACHARY 权利人:H LEE MOFFITT CANCER CT & RES 摘要:This disclosure provides reagents and processes for the synthesis of organic compounds, more particularly reagents and processes for the asymmetric synthesis of sulfur (VI) containing organic compounds.
专利号:US-8697876-B2 优先权日:2010-04-02 标 题:Compositions and methods of synthesis of pyridinolypiperidine 5-HT1F agonists 发明人:CARNIAUX JEAN-FRANCOIS; CUMMINS JONATHAN 权利人:CARNIAUX JEAN-FRANCOIS; CUMMINS JONATHAN; COLUCID PHARMACEUTICALS INC 摘要:The present invention provides a novel polymorph of the hemisuccinate salt of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide (Form A) characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. This polymorph is useful in pharmaceutical compositions, for example, for the treatment and prevention of migraine. The invention also provides a process for the synthesis of pyridinoylpiperidine compounds of Formula I in high yield and high purity. In particular, the provides a process for the preparation of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide, its hemisuccinate salt and polymorph (Form A).
专利号:US-2011130567-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; TAN ZHULIN; QU BO; YEE NATHAN K; RODRIGUEZ SONIA 权利人:BOEHRINGER INGELHEIM INT 摘要:A process for stereoselective 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; n n R 2 and R 3 are each independently C 1 -C 5 alkyl; R 4 is C 1 -C 5 alkyl optionally independently substituted with one to three substituent groups,n wherein each substituent group of R 4 is independently C 1 -C 3 alkyl, hydroxy, halogen, amino, or oxo; and n R 5 is a heteroaryl group substituted with one to three substituent groups,n wherein each substituent group of R 5 is independently C 1 -C 5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, alkylsulfonylamino, aminosulfonyl, C 1 -C 5 alkylaminosulfonyl, C 1 -C 5 dialkylaminosulfonyl, halogen, hydroxy, carboxy, cyano, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, or C 1 -C 5 alkylthio wherein the sulfur atom is optionally oxidized to a sulfoxide or sulfone.
专利号:US-2010312013-A1 优先权日:2009-06-03 标 题:Steroselective synthesis of certain trifluoromethyl-substituted alcohols 发明人:FANDRICK DANIEL R; YEE NATHAN K; SONG JINHUA J; REEVES JONATHAN T 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:WO-2015177083-A1 优先权日:2014-05-19 标题 :STEREOSELECTIVE SYNTHESIS OF INTERMEDIATES IN THE PREPARATION OF ß-C-ARYLGLUCOSIDES 发明人:ZUPANCIC BORUT; SELIC LOVRO; CUSAK ANJA; RICHTER FRANK 权利人:LEK PHARMACEUTICALS 摘要:The invention belongs to the fields of pharmaceutical industry, and particularly to an improved stereoselective synthesis of intermediate compounds for the preparation of gliflozins, for example canagliflozin or structurally similar gliflozins. Gliflozins, such as canagliflozin, dapagliflozin, empagliflozin, or ipragliflozin, inhibit the sodium-dependent glucose cotransporter 2 (SGLT2) in the kidney and as such are useful in the treatment of type-2 diabetes.