Patent ID: 7365188
Filing Date: 2008-04-29
Classification: A61P,C07H

Abstract:
1. A process for producing a N 4 -acyl-5′-deoxy-5-fluorocytidine compound of formula: wherein R 2 is alkyl, cycloalkyl, aralkyl, aryl, or alkoxy, said process comprising: (a) admixing 5-fluorocytosine of formula:  with a first silylating agent in the presence of an organic acid catalyst to produce a first silylated compound; (b) admixing the first silylated compound with a 2,3-diprotected-5-deoxy furanoside of formula:  to produce a coupled product,  wherein (c) admixing the coupled product with a second silylating agent to produce a second silylated compound, wherein the second silylating agent may be the same as or different from the first silylating agent; (d) acylating the second silylated compound with an acylating agent of formula:  to produce an acylated product, wherein (e) adding at least one base to the acylated product to selectively remove a covalently linked silyl moiety and the hydroxy protecting groups, R