Process for preparing...

C - Chemistry – Metallurgy – 07 – H

Patent

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C07H 19/073 (2006.01) C07H 19/06 (2006.01)

Patent

CA 2207617

This invention provides a process for preparing gemcitabine hydrochloride which comprises deblocking .beta.-1-(2'-deoxy-2',2'-difluoro-3',5'-di-O-benzoyl-D-ribofuranosyl)-4- aminopyrimidin-2-one with a catalytic amount of an alkylamine in the presence of methanol or ethanol in an environment essentially free of water, treating the resulting solution with hydrochloric acid and an antisolvent; and recovering the resulting solid gemcitabine hydrochloride.

Cette invention concerne un procédé de préparation de chlorhydrate de gemcitabine, procédé consistant à débloquer beta -1-(2'-désoxy-2',2'-difluoro-3',5'-di-O-benzoyl-D-ribofuranosyl)-4-aminopyrimidine-2-one avec une quantité catalytique d'une alkylamine en présence de méthanol ou d'éthanol dans un environnement totalement exempt d'eau; à traiter la solution obtenue avec l'acide chlorhydrique et un antisolvant; et à récupérer le chlorhydrate de gemcitabine solide obtenu.

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