专利号:US-2017327504-A1 优先权日:2014-10-30 标 题:Synthesis of Substituted 1H-Pyrazolo[3,4-D]Pyrimidines 发明人:ROSE CHRISTOPHER; SILBERGER HERBERT; SCHREINER ERWIN; FELZMANN WOLFGANG; MARAS NENAD 权利人:SANDOZ AG 摘要:The present invention refers to the synthesis and intermediates of substituted bicyclic compounds by using a central 1H-pyrazolo[3,4-d]pyrimidine of formula (I), which is assembled starting from 4,6-dichloropyrimidine carboxylic acid. The invention in particular refers to the synthesis of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one(ibrutinib) and its synthesis intermediates.
专利号:US-7973175-B2 优先权日:2005-09-28 标 题 :Synthesis of renin inhibitors involving a cycloaddition reaction 发明人:MICKEL STUART J; MARTERER WOLFGANG 权利人:NOVARTIS AG 摘要:The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula III, n nwherein R, R 1 , and R′ are as defined in the specification, or a salt thereof, and a compound of formula IVn n nwherein R, R 1 , R 2 and R′ are as defined in the specification, and processes of manufacturing these.
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-2024208926-A1 优先权日:2021-03-24 标题:New process for the synthesis of 5-{5-chloro-2-[(3s)-3-[(morpholin-4-yl)methyl]-3,4-dihydroisoquinoline-2(1h)- carbonyl]phenyl}-1,2-dimethyl-1h-pyrrole-3-carboxylic acid derivatives and its application for the production of pharmaceutical compounds 发明人:PIN FRÉDÉRIC; PETHÖ BÃ?LINT 权利人:SERVIER LAB; NOVARTIS AG 摘要:The present invention relates to a new process for preparing 5-{5-chloro-2-[(38)-3-[(morpholin-4-yl)methyl]-3.4-dihydr oisoquinoline-2(1H)-carbonyl]phenyl}-1,2-dimethyl-1/H-pyrrole-3-carboxylic acid derivatives and its application for the production of pharmaceutical compounds.
专利号:US-5218097-A 优先权日:1988-12-07 标题:Process for the preparation of protected mono-sugar and oligo-sugar halides 发明人:ERNST BEAT 权利人:CIBA GEIGY CORP 摘要:The reaction of protected monosaccharides or oligosaccharides or protected monosaccharide and oligosaccharide derivatives containing an anomeric hydroxyl group with secondary α-haloenamines affords high yields of protected glycosyl halides, which are valuable intermediates for the introduction of sugar groups in the synthesis of oligosaccharides, glycolipids or glycopeptides.
专利号:US-9035070-B2 优先权日:2010-07-30 标 题 :Process for the preparation of 1-aryl-pyrazol-3-one intermediates useful in the synthesis of sigma receptors inhibitors 发明人:BARTRA SANMARTI MARTÃ?; BERENGUER MAIMO RAMON; MEDRANO RUPEREZ JORGE; GARCIA GOMEZ JORGE; ARIZA PIQUER JAVIER 权利人:BARTRA SANMARTI MARTÃ?; BERENGUER MAIMO RAMON; MEDRANO RUPEREZ JORGE; GARCIA GOMEZ JORGE; ARIZA PIQUER JAVIER; ESTEVE QUÃ?MICA S A 摘要:The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.