Synthesis of...

C - Chemistry – Metallurgy – 07 – D

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C07D 403/06 (2006.01)

Patent

CA 2756234

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.

La présente invention porte sur la synthèse de 3-{[(2R)-1-méthylpyrrolidin-2-yl]méthyl}-5-[2-(phénylsulfonyl)éthyl]-1H-indole, un médicament appelé élétriptan, ou de ses sels. En particulier, la présente invention porte sur un procédé pour la synthèse d'élétriptan ou de ses sels, comprenant les étapes suivantes : a) la salification de l'intermédiaire de formule (6), à l'aide d'un acide dicarboxylique, pour obtenir un sel dérivé; b) éventuellement, la purification dudit sel brut obtenu selon l'étape a), par cristallisation dans un solvant, pour obtenir un sel purifié de l'intermédiaire de formule (6); c) la conversion dudit sel de l'intermédiaire de formule (6) selon l'étape a) ou dudit sel purifié selon l'étape b) en un intermédiaire de formule (10); d) la conversion de l'intermédiaire de formule (10) en élétriptan ou son sel.

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