Method for the preparation of 2'-deoxy-2',2'-difluorocytidine

Details Method for the preparation of 2'-deoxy-2',2'-difluorocytidine Method for the preparation of 2'-deoxy-2',2'-difluorocytidine

C - Chemistry, Metallurgy

07

H

C07H 19/04 (2006.01)

Patent

CA 2577449

This invention relates to an improved method for stereoselectively preparing 2¢~-deoxy-2¢~,2¢~-difluorocytidine of formula (I), which comprises the steps of reacting a 1-halo ribofuranose compound of formula (III) with a nucleobase of formula (IV) in a solvent to obtain a nucleoside of formula (II) with removing the silyl halide of formula (V) produced during the reaction; and deprotecting the nucleoside of formula (II) to obtain 2¢~-deoxy-2¢~,2¢~- difluorocytidine of formula (I).

Méthode améliorée de préparation stéréosélective de 2'-deoxy-2',2'-difluorocytidine représentée par la formule (I) et consistant à effectuer la réaction d'un composé de 1-halo-ribofuranose représenté par la formule (III) avec une nucléobase représentée par la formule (IV) dans un solvant afin d'obtenir un nucléoside représenté par la formule (II) et à extraire l'halogénure de silyle représenté par la formule (V) produit pendant la réaction, puis à déprotéger le nucléoside (formule II), de manière à obtenir 2-'deoxy-2'2' difluorocytidine (formule I).

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