Process for preparing purine derivatives

Details Process for preparing purine derivatives Process for preparing purine derivatives

C - Chemistry, Metallurgy

07

D

C07D 473/18 (2006.01)

Patent

CA 2243972

Process for preparing the L-monovaline ester of 2-(2-amino-1,6-dihydro-6- oxo-purin-9-yl)-methoxy-1,3-propanediol and its pharmaceutically acceptable salts. The present process relates to an improved process whereby ganciclovir is esterified with an L-valine derivative to provide a di-valine ganciclovir intermediate. Removal of one of the valine groups with a lower alkyl amine, benzylamine or benzyl methylamine provides the mono-valine ester compound of Formula I, (see formula I) These products are of value as antiviral agents with improved absorption.

L'invention concerne un procédé et de nouveaux intermédiaires pour préparer l'ester L-monovaline de 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)-méthoxy-1,3-propanediol et ses sels pharmaceutiquement acceptables. Le présent procédé concerne un procédé amélioré selon lequel le ganciclovir est estérifié avec un dérivé de L-valine pour fournir un intermédiaire du di-valine ganciclovir. L'élimination des groupes de valine avec un alkylamine inférieur, un benzylamine ou un benzyle méthylamine donne le composé d'ester mono-valine selon la formule I. Ces produits sont très utiles comme agents antiviraux et présentent une absorption améliorée.

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