Intermediate and process for preparing of beta- anomer...

Details Intermediate and process for preparing of beta- anomer... Intermediate and process for preparing of beta- anomer...

C - Chemistry, Metallurgy

07

H

C07H 13/08 (2006.01) C07H 19/073 (2006.01)

Patent

CA 2598895

A highly stereoselective, simple and economical glycosylation process for preparation of .beta.-anomer enriched 21-deoxy-21,21-D-ribofuranosyl difluoronucleosides of formula (II), and physiologically acceptable slats thereof, in particular, the .beta.- enriched anomer of gemcitabine hydrochloride of formula (lib) in purity of >99% is provided through utilization of a novel trichloroacetimidate of formula (I).

L'invention concerne un procédé de glycosylation simple et économique, hautement stéréosélectif pour la préparation de 21-désoxy-21, 21-D-ribofuranosyl difluoronucléosides enrichis en anomères .beta. de formule (II), ainsi que de sels physiologiquement acceptables de ces derniers, et en particulier de l'anomère ß-enrichi de chlorhydrate de gemcitabine de formule (lIb) présentant une pureté supérieure à 99 % par utilisation d'un nouveau trichloroacétimidate de formule (I).

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