Process for preparing ganciclovir derivatives

Details Process for preparing ganciclovir derivatives Process for preparing ganciclovir derivatives

C - Chemistry, Metallurgy

07

D

C07D 473/18 (2006.01) C12P 17/18 (2006.01)

Patent

CA 2246164

Process and novel intermediates for preparing the L-monovaline ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)-methoxy-1,3- propanediol (ganciclovir) and its pharmaceutically acceptable salts. The present process and monoester intermediates provide for monoesterification by an L-valine derivative, resulting in a monocarboxylate-monovalinate which is then selectively hydrolyzed under basic or enzymatic conditions to give the monovaline ester of ganciclovir, of formula (I) (See Formula I) in high yield and purity. 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-purine-9-yl)-méthoxy-1,3-propanediol (ganciclovir) et ses sels pharmaceutiquement acceptables. Le présent procédé et les intermédiaires monoester assurent la mono-estérification par un dérivé de L-valine, ce qui donne un monocarboxylate-monovalinate. Ce dernier produit est ensuite hydrolysé sélectivement dans des conditions basiques ou enzymatiques pour donner l'ester monovaline de ganciclovir en grande quantité et avec une pureté élevée. Ces produits sont très utiles comme agents antiviraux et présentent une absorption améliorée.

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