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Note | Regular issue | Vol 68, No. 3, 2006, pp.521-530
Published online, 14th February, 2006
DOI: 10.3987/COM-05-10639
Synthesis of 2’-O-Methyl-5-alkynyl and alkenyl Substituted Uridine Derivatives to Screen for Inhibitors of HCV

Yili Ding,* Jean-Luc Girardet, Zhi Hong, Stephanie Z. Shaw, and Nanhua Yao

*Drug Discovery, Valeant Pharmaceuticals International, Inc., 3300 Hyland Avenue, Costa Mesa, CA 92626, U.S.A.

Abstract

Using Sonogashira and Heck coupling reactions, a series of 5-alkynyl and 5-alkenyl substituted 2’-O-methyluridine derivatives were synthesized in high yields. These compounds were used to screen for inhibitors of HCV, however none of them showed significant HCV inhibitory activity under 300 μM.