Method of preparing esomeprazole and salts thereof

Details Method of preparing esomeprazole and salts thereof Method of preparing esomeprazole and salts thereof

C - Chemistry, Metallurgy

07

D

C07D 401/12 (2006.01) A61P 1/04 (2006.01)

Patent

CA 2616119

Optically pure esomeprazole and its salt can be simply prepared by dissolving (S)-(-)-binol, a weak base and the racemic form of omeprazole in a mixture of a water-compatible organic solvent and water at a high temperature, cooling the mixed solution to crystallize the inclusion complex of esomeprazole and (S)-(-)-binol, and removing the (S)-(-)-binol moiety from the crystallized inclusion complex.

Selon l'invention, on peut préparer d'une manière simple de l'ésoméprazole optiquement pur ainsi que ses sels en dissolvant (S)-(-)-binol, une base faible et la forme racémique d'oméprazole dans un mélange d'eau et de solvant organique compatible avec l'eau à une température élevée, en refroidissant la solution mélangée afin de cristalliser le complexe d'inclusion d'ésoméprazole et de (S)-(-)-binol, et en évacuant la fraction (S)-(-)-binol du complexe d'inclusion cristallisé.

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