首页> 外国专利> Procedure for the synthesis of 3 - 3 - (7S) - 3,4 - dimetoxibiciclo 4.2.0 octa - 1,3,5 - triennium 2008-2010 - 7 - il methyl} (methyl) amino propyl - 7.8 - Dimethoxy - 1,3,4,5 - tetrahydro - 2H - 3 - benzazepin - 2 - One (Combination).

Procedure for the synthesis of 3 - 3 - (7S) - 3,4 - dimetoxibiciclo 4.2.0 octa - 1,3,5 - triennium 2008-2010 - 7 - il methyl} (methyl) amino propyl - 7.8 - Dimethoxy - 1,3,4,5 - tetrahydro - 2H - 3 - benzazepin - 2 - One (Combination).

机译:合成3-[3-[[(7S)-3,4-二甲双胍[4.2.0] octa-1,3,5-三年期2008-2010-7-il]甲基}(甲基)氨基]的合成程序丙基]-7.8-二甲氧基-1,3,4,5-四氢-2H-3-苯并ze庚因-2-一(组合)。

摘要

Preparing (P1) ivabradine (I) involves reductive amination reaction of 4-(7,8-dimethoxy-2-oxo-1,2,4,5-tetrahydro-benzo[d]azepin-3-yl)-butyraldehyde (V) with ((S)-3,4-dimethoxy-bicyclo[4.2.0]octa-1(6),2,4-trien-7-ylmethyl)-methyl-amine (VI) in the presence of an iron-based catalyst, optionally in the presence of trimethylamine N-oxide, under dihydrogen pressure of 1-20 bars, in an organic solvent or mixture of organic solvents, at 25-100[deg] C. ACTIVITY : Cardiant; Vasotropic; Antianginal. No biological data given. MECHANISM OF ACTION : None given.
机译:制备(P1)伊伐布雷定(I)涉及4-(7,8-二甲氧基-2-氧代-1,2,4,5-四氢-苯并[d] a嗪-3-基)-丁醛(V的还原胺化反应) )与((S)-3,4-二甲氧基-双环[4.2.0] octa-1(6),2,4-三烯-7-基甲基)-甲基胺(VI)在铁-碱催化剂,任选地在三甲胺N-氧化物存在下,在1-20 bar的二氢压力下,在有机溶剂或有机溶剂的混合物中,温度为25-100℃。变压性抗心绞痛。未提供生物学数据。作用机理:未给出。

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