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发明授权
US08426612B2 Synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5[2-(phenylsulfonyl)ethyl]-1H-indole 有权
3 - {[（2R）-1-甲基吡咯烷-2-基]甲基} -5 [2-（苯基磺酰基）乙基] -1H-吲哚

Synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5[2-(phenylsulfonyl)ethyl]-1H-indole
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 salt; 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.
摘要（中）：

本发明涉及合成名为Eletriptan的3 - {[（2R）-1-甲基吡咯烷-2-基]甲基} -5- [2-（苯基磺酰基）乙基] -1H-吲哚， 或其盐。 特别地，本发明涉及一种合成埃曲普坦或其盐的方法，包括以下步骤：a）使用二羧酸使式（6）的中间体盐化得到衍生的盐; b）任选地，通过溶剂结晶纯化根据步骤a）获得的所述生盐，得到式（6）中间体的纯化盐; c）根据步骤a）将所述式（6）的中间体的盐或根据步骤b）的所述纯化盐转化成式（10）的中间体; d）将式（10）的中间体转化成Eletriptan或其盐。

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