专利号:US-9090560-B2 优先权日:2013-09-04 标 题 :Process for microwave assisted synthesis of N-methyl pyrrolidone 发明人:KHATRI PRAVEEN KUMAR; JAIN SUMAN LATA; CHATERJEE ALOK KUMAR; BIR SAIN 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to a process for microwave assisted synthesis of N-methyl pyrrolidone (NMP). Particularly the process relates to the synthesis of N-methyl succinimide or corresponding analogs by using microwave irradiation which on hydrogenation in the presence of a hydrogenating catalyst gives N-methyl pyrrolidone. Compared to the conventional heating microwave process requires less energy inputs and reduces the reaction time drastically from 5-6 h to 2-5 min.
专利号:WO-2019202611-A1 优先权日:2018-04-21 标题:An improved process for the synthesis of ivabradine and its pharmaceutically acceptable salts 发明人:NANDEPU Venkateswara Rao; BOPPANA DURGA PRASAD 权利人:METROCHEM API PVT 摘要:: Disclosed herein is an improved process for the preparation of Ivabradine and pharmaceutically acceptable salts thereof. The invention more particularly disclosesthe synthesis of key intermediates viz.,(S)-N-[(4,5-dimethoxybenzocydobut-l-yl)-methyl]-N- (methyl)amine hydrochloride of Formula-II and 3-(3-Iodopropyl)-7,8-dimethoxy-1,3-dihydro-2H-3-benzapin-2-one of Formula-III, and its use in industrial synthesis of Ivabradine and pharmaceutically acceptable salts thereof.
专利号:WO-2023019298-A1 优先权日:2021-08-20 标 题:Improved method of synthesis of 1-(3',4'-methylene dioxyphenyl)-2-(methylamino) propane (mdma) 发明人:O'MALLEY WILLIAM IAN; WYNNE PAUL MICHAEL 权利人:MIND MEDICINE AUSTRALIA LTD 摘要:The present invention relates to an improved method of synthesis of 1-(3',4'-methylenedioxyphenyl)-2-(methylamino)propane (MDMA) that is of sufficient purity that it can be used for pharmaceutical applications. In particular the present invention provides a method of synthesising MDMA comprising the steps of (a) condensation of piperonal and nitroethane in the presence of a catalysing base to form 1-(3',4'-methylenedioxyphenyl)-2-nitroprop-1-ene (MDP-2-nitropropene), (b) oxidative hydrolysis of MDP-2-nitropropene to form 1-(3',4'methylenedioxyphenyl)-propan-2-one (MDP2P), and (c) reductive amination of MDP2P to 1-(3',4'-methylenedioxyphenyl)-2-(methylamino)propane (MDMA).
专利号:US-5665877-A 优先权日:1993-12-07 标题:Synthesis of bisindolylmaleimides 发明人:FAUL MARGARET M; JIROUSEK MICHAEL R; WINNEROSKI II LEONARD L 权利人:LILLY CO ELI 摘要:The present invention provides a novel synthesis of the compounds of Formula (I): ##STR1## The compounds are produced in high yield and without utilizing expensive chromatographic separations. The synthesis is particularly advantageous because it is stereoselective.
专利号:US-5541347-A 优先权日:1993-12-07 标 题 :Synthesis of bisindolylmaleimides 发明人:FAUL MARGARET M; JIROUSEK MICHAEL R; WINNEROSKI II LEONARD L 权利人:LILLY CO ELI 摘要:The present invention provides a novel synthesis of the compounds of Formula (I): ##STR1## The compounds are produced in high yield and without utilizing expensive chromatographic separations. The synthesis is particularly advantageous because it is stereoselective.
专利号:US-12240835-B2 优先权日:2018-09-18 标题:Substituted benzamides as intermediates in the synthesis of inhibitors of tyrosine kinase enzymatic activity 发明人:ROMERO F ANTHONY; KIRSCHBERG THORSTEN A; HALCOMB RANDALL; XU YINGZI 权利人:TERNS PHARMACEUTICALS INC 摘要:Provided herein are compounds, preferably compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and/or symptomology of the disease. Intermediates such as compounds of Formula (S23), which are useful in the synthesis of compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, are also provided.
摘要:Demchuk, O. M.; Stankevič, M.; Pietrusiewicz, K. M., Science of Synthesis Knowledge Updates, (2015) 1, 360. 摘要:Kodak Company Reports., 21MAY1971 摘要:Cui, H.; An, B.; Zhang, X., Science of Synthesis: Dearomatizations, (2026) . 参考文献:10.1007/bf00717730 摘要:Lange R, Lameijer W, Slijkhuis C, de Kaste D. Pharmaceutical analysis of the oral iron chelator deferiprone (DMHP, L1). International Journal of Clinical Pharmacy. 1996 Jul;18(4):142–7. doi: 10.1007/bf00717730.