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:US-8476426-B2 优先权日:2011-02-14 标题 :Process for the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:PEGLION JEAN-LOUIS; DESSINGES AIMEE 权利人:PEGLION JEAN-LOUIS; DESSINGES AIMEE; SERVIER LAB 摘要:Process for the synthesis of ivabradine of formula (I): n nand addition salts thereof with a pharmaceutically acceptable acid.
专利号:EP-2017267-A1 优先权日:2007-07-16 标 题:Synthesis of statins 发明人:KOPITAR GREGOR; MRAK PETER; OSLAJ MATEJ 权利人:LEK PHARMACEUTICALS 摘要:The process for synthesis of statins is presented where the intermediate intermediate (4 R ,6 S )-6-(dialkoxymethyl)tetrahydro-2 H -pyran-2,4-diol which already possesses the desired stereochemistry corresponding to final statin is prepared by an aldolaze.
专利号:EP-2465936-A1 优先权日:2010-12-20 标题 :Enzymatic synthesis of statins and intermediates thereof 权利人:LEK PHARMACEUTICALS 摘要:The present invention discloses a process for preparing an active pharmaceutical ingredient (API) or intermediates thereof, notably particular step in the synthesis of an intermdiate useful for example in the preparation of statins, by using an enzyme capable of catalyzing oxidation or dehydrogenation. The invention further provides an expression system effectively translating said enzyme. In addition, the invention relates to a specific use of such enzyme for preparing API or intermediate thereof, and in particular for preparing statin or interemediate thereof.
专利号:US-8471045-B2 优先权日:2007-04-03 标题 :Synthesis of statins 发明人:CASAR ZDENKO; MESAR TOMAZ; KOPITAR GREGOR; MRAK PETER; OSLAJ MATEJ 权利人:CASAR ZDENKO; MESAR TOMAZ; KOPITAR GREGOR; MRAK PETER; OSLAJ MATEJ; LEK PHARMACEUTICALS 摘要:The process for the synthesis of statins featuring the use of an early intermediate (4R,6S)-6-(dialkoxymethyl)tetrahydro-2H-pyran-2,4-diol which already possesses the desired stereochemistry corresponding to the final statin.
专利号:US-12006315-B2 优先权日:2022-03-25 标题 :Intermediate useful for the synthesis of TGF-beta inhibitors and a method of preparing TGF-beta inhibitors using the same 发明人:LEE SEUNG HO 权利人:MEDPACTO INC 摘要:The present invention provides an intermediate for synthesizing a TGF-β inhibitor represented by Chemical Formula 1 and an improved method for preparing the TGF-β inhibitor represented by Chemical Formula 1 using the same. The preparation method according to the present invention can not only allow inexpensive and safe reagents to be used, but also simplify the synthesis steps and purification methods to improve the reaction yield, thereby maximizing the production efficiency of the TGF-β inhibitor represented by Chemical Formula 1 to be used usefully for mass production.
摘要:Schneider, C.; Sickert, M., Science of Synthesis Knowledge Updates, (2017) 3, 398. 摘要:Burns, N. Z.; Jacobsen, E. N., Science of Synthesis: Stereoselective Synthesis, (2011) 2, 793. 摘要:Yliniemelä-Sipari, S. M.; Piisola, A.; Pihko, P. M., Science of Synthesis: Asymmetric Organocatalysis, (2012) 1, 59. 摘要:Yliniemelä-Sipari, S. M.; Piisola, A.; Pihko, P. M., Science of Synthesis: Asymmetric Organocatalysis, (2012) 1, 64. 摘要:Suzuki, K.; Takikawa, H., Science of Synthesis: Asymmetric Organocatalysis, (2012) 1, 601.