Patent ID: 8212021
Filing Date: 2012-07-03
Classification: A61P,C07H

Abstract:
1. A process for the preparation of a 5-azacytosine nucleoside compound of formula I: wherein R 1 is hydrogen, hydroxy or halogen; R 2 is hydrogen or halogen comprising: a. reacting 5-azacytosine with a silylating agent to produce a reaction mixture containing a silylated 5-azacytosine of formula II: wherein each of R b. coupling the silylated 5-azacytosine of formula II with a protected D-ribofuranose of formula III: c. converting the protected 5-azacytosine nucleoside of formula (IV) to the 5-azacytosine nucleoside of formula (I); wherein prior to the step of b), the silylated 5-azacytosine compound is isolated in a solid form from the reaction mixture of the step a).