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Heterocycles. 2011 May 1;83(5):1145-1151.

Feasible Synthesis of Antagonist of GPR40 by Constructing 2-Thiouracil Ring viaAcid Mediated Cyclization.

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Department of Bioengineering, Bourns College of Engineering, University of California-Riverside, Riverside, CA 92507, USA.


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

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