3,4-二甲氧基苯乙酰胺置于甲烷磺酸,盐酸羟胺,Sodium Iodide,Potassium Hydroxide体系中,用 N,N-二甲基甲酰胺,甲苯,丁酮 用作溶剂,化学反应 40.25H,反应生成7,8-二甲氧基-3-(3-碘代丙基)-1,3-二氢-2H-3-苯并氮杂卓-2-酮 参考文献: An Improved Process For The Synthesis Of Ivabradine And Its Pharmaceutically Acceptable Salts[fr] Procédé Amélioré Pour La Synthèse De L'Ivabradine Ou De Ses Sels Pharmaceutiquement Acceptables 标题: An Improved Process For The Synthesis Of Ivabradine And Its Pharmaceutically Acceptable Salts[fr] Procédé Amélioré Pour La Synthèse De L'Ivabradine Ou De Ses Sels Pharmaceutiquement Acceptables 摘要:本文披露了一种改进的伊维布地定及其药用盐的制备过程.该发明更具体地披露了关键中间体的合成,即(S)-N-[(4,5-二甲氧基苯并环丁-1-基)-甲基]-N-(甲基)胺盐酸盐(化学式-Ii)和3-(3-碘丙基)-7,8-二甲氧基-1,3-二氢-2H-3-苯并啶-2-酮(化学式-Iii),以及其在伊维布地定及其药用盐的工业合成中的应用.
专利号:US-8927708-B2 优先权日:2013-03-26 标 题 :Process for the synthesis of 7,8-dimethoxy-1,3-dihydro-2H-3-benzazepin-2-one compounds, and application in the synthesis of ivabradine 发明人:LE FLOHIC ALEXANDRE 权利人:SERVIER LAB 摘要:Process for the synthesis of the compound of formula (I): n nwherein R represents a para-methoxybenzyl (PMB) group or the following group:n n nApplication in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.
专利号:US-8779122-B2 优先权日:2012-11-08 标 题:Process for the synthesis of (2E)-3-(3,4-dimethoxyphenyl)prop-2-enenitrile, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:CARRANZA MARIA DEL PILAR; GARCIA ARANDA MARIA ISABEL; GONZALEZ JOSÉ LORENZO; SANCHEZ FRÉDÉRIC 权利人:SERVIER LAB 摘要:Process for the synthesis of the compound of formula (I): n nApplication in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
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-7064200-B2 优先权日:2004-04-13 标题 :Process for the synthesis of 1,3,4,5-tetrahydro-2H-3-benzazepin-2-one compounds, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:LERESTIF JEAN-MICHEL; LECOUVE JEAN-PIERRE; SOUVIE JEAN-CLAUDE; BRIGOT DANIEL 权利人:SERVIER LAB 摘要:Process for the synthesis of compounds of formula (I): n nwherein R 1 and R 2 , which may be the same or different, each represent a linear or branched (C 1 –C 8 )alkoxy group or form, together with the carbon atom carrying them, a 1,3-dioxane, 1,3-dioxolane or 1,3-dioxepane ring.n n Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid, and hydrates thereof.
专利号:US-8859763-B1 优先权日:2013-05-17 标题 :Process for the synthesis of 3,4-dimethoxybicyclo[4.2.0]OCTA-1,3,5-triene-7-carbonitrile, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:VAYSSE-LUDOT LUCILE; LE FLOHIC ALEXANDRE; VAULTIER MICHEL; PUCHEAULT MATHIEU; KAMINSKI THOMAS 权利人:SERVIER LAB 摘要:Process for the synthesis of the compound of formula (I): n nApplication in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
专利号:US-8779123-B2 优先权日:2012-12-06 标题:Process for the synthesis of 3-(2-bromo-4,5-dimethoxyphenyl)propanenitrile, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:CARRANZA MARIA DEL PILAR; GARCIA ARANDA MARIA ISABEL; GONZALEZ JOSÉ LORENZO; SANCHEZ FRÉDÉRIC 权利人:SERVIER LAB 摘要:Process for the synthesis of the compound of formula (I): n nApplication in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
参考标题:Process For The Synthesis Of 3-(2-Bromo-4,5-Dimethoxyphenyl)Propanenitrile, And Application In The Synthesis Of Ivabradine And Addition Salts Thereof With A Pharmaceutically Acceptable Acid 摘要:Process For The Synthesis Of The Compound Of Formula (I): Application In The Synthesis Of Ivabradine, Addition Salts Thereof With A Pharmaceutically Acceptable Acid And Hydrates Thereof.