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Short Paper | Regular issue | Vol 83, No. 5, 2011, pp.1145-1151
Published online, 25th March, 2011
DOI: 10.3987/COM-11-12175
Feasible Synthesis of the GPR40 Antagonist by Constructing 2-Thiouracil Ring via Acid Mediated Cyclization

Yongfeng Zhao and Jiayu Liao*

*Department of Bioengineering, Bourns College of Engineering, University of California at Riverside, 900 University Avenue, Riverside, CA 92521, U.S.A.

Abstract

GW1100 is an antagonist of GPR40 identified by high throughput screening recently. The feasible synthesis of GW1100 has been developed in mild conditions. The key step involves the cyclization of the 2-thiouracil heterocycle under acidic conditions at room temperature.