首页> 外国专利> Synthesis of 3-{(2R) -1-methylpyrrolidin-2-yl methyl} -5- 2- (phenylsulfonyl) ethyl 1H-indole

Synthesis of 3-{(2R) -1-methylpyrrolidin-2-yl methyl} -5- 2- (phenylsulfonyl) ethyl 1H-indole

机译:3-{[((R)-1-甲基吡咯烷-2-基]甲基]}-5- [2-(苯磺酰基)乙基] 1H-吲哚的合成

摘要

The present invention refers to the synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole, a drug known by the name Eletriptan, or of its salts. In particular, the present invention regards a process for the synthesis of Eletriptan or of its salt, comprising the following steps: a) Salifying the intermediate of Formula (6), using a dicarboxylic acid to obtain a derived sa b) Optionally, purifying said raw salt obtained according to step a) by solvent crystallization to obtain a purified salt of the intermediate of Formula (6); c) Converting said salt of the intermediate of formula (6) according to step a) or said purified salt according to step b) into an intermediate of formula (10); d) Converting the intermediate of Formula (10) into Eletriptan or its salt.
机译:本发明涉及3-{[((2R)-1-甲基吡咯烷基-2-基]甲基} -5- [2-(苯磺酰基)乙基] -1H-吲哚的合成,该药物被称为Eletriptan,或其盐。特别地,本发明涉及一种合成依曲曲坦或其盐的方法,其包括以下步骤:a)使用二羧酸将式(6)的中间体盐化以获得衍生的盐; b)任选地,通过溶剂结晶纯化根据步骤a)获得的所述粗盐,以获得式(6)的中间体的纯化盐; c)将根据步骤a)的式(6)的中间体的所述盐或根据步骤b)的所述纯化的盐转化为式(10)的中间体; d)将式(10)的中间体转化成依曲曲坦或其盐。

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