F.i.s. Fabbrica Italiana Sintetici S.p.a.

Claudio Dal Santo

Pierluigi Padovan

Andrea Castellin

Siro Serafini

Lorenzo Caruana

An improved and well reproducible process for the preparation of Enclomiphene citrate having needle shaped crystal habit is provided. It is also related to a solid form of Enclomiphene citrate.

Process for the preparation of enclomiphene citrate having needle shaped crystal habit

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. 

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Sarego, Italy

Claudio Dal Santo