C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 473/18 (2006.01)
Patent
CA 2244680
Process for preparing the L-monovaline ester of 2-(2-amino-1,6-dihydro-6- oxo-purin-9-yl)-methoxy-1,3-propanediol of the formula I, (See formula I) and its pharmaceutically acceptable salts. The present process provides an N,O- bis- trityl intermediate of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)-methoxy-1,3- propanediol which allows for monoesterification by an L-valine derivative. These products are of value as antiviral agents with improved absorption.
L'invention concerne un procédé 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. Ce procédé permet d'obtenir un intermédiaire N,O-bis-trityl de 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)-méthoxy-1,3-propanediol qui assure la monoestérification par un dérivé de L-valine. Ces produits sont très utiles comme agents antiviraux et présentent une absorption améliorée.
Arzeno Humberto B.
Humphreys Eric R.
F. Hoffmann-La Roche Ag
Gowling Lafleur Henderson Llp
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