Process for preparing ganciclovir derivatives

Details Process for preparing ganciclovir derivatives Process for preparing ganciclovir derivatives

C - Chemistry, Metallurgy

12

P

C12P 17/18 (2006.01) C07D 473/32 (2006.01) A61K 31/7076 (2006.01)

Patent

CA 2547307

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) Image in high yield and purity. These products are of value as antiviral agents with improved absorption.

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