Process for the preparation of pure citalopram

Details Process for the preparation of pure citalopram Process for the preparation of pure citalopram

C - Chemistry, Metallurgy

07

D

C07D 307/87 (2006.01) A61K 31/343 (2006.01) A61P 25/24 (2006.01)

Patent

CA 2359810

A process for the preparation of citalopram of formula (I) in which a compound of formula (II) wherein Z is iodo, bromo, chloro or CF~3-(CF~2)~n-SO~2-O- n being 0, 1, 2, 3, 4, 5, 6, 7 or 8, is subjected to a cyanide exchange reaction in which the group Z is exchanged with cyanide by reaction with a cyanide source; the resultant crude citalopram product is optionally subjected to some initial purification and the crude citalopram base is subsequently subjected to a film distillation process; the resulting citalopram product is then optionally further purified and worked up and isolated as the base or a pharmaceutically acceptable salt thereof.

L'invention concerne un procédé de préparation de citalopram de formule (I) dans lequel un composé de formule (II) dans laquelle Z représente iodo, bromo, chloro ou CF3-(CF2)n-SO2-O- n étant 0, 1, 2, 3, 4, 5, 6, 7 ou 8, se caractérise en ce que le composé de formule (II) est soumis à une réaction d'échange de cyanure dans laquelle le groupe Z est échangé avec du cyanure en réaction avec une source de cyanure; le produit citalopram brut obtenu est éventuellement soumis à quelques purifications initiales et la base de citalopram brut est ensuite soumise à un processus de distillation de film; le produit citalopram obtenu est ensuite éventuellement purifié, préparé et isolé tout comme la base ou un sel acceptable sur le plan pharmaceutique de ce produit.

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