Patent · US Active

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

US8426612B2 · kind B2 · utility

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35Claims
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Key dates

Filing dateNov 9, 2009
Grant dateApr 23, 2013
Priority date
Expiry dateJan 7, 2030

Classification

  • Technology area (CPC A)Human Necessities
  • CPC primaryA61P25/06
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

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.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.