Feasible synthesis of the GPR40 antagonist by contructing 2-thiouracil ring VIA acid mediated cyclization

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. © The Japan Institute of Heterocyclic Chemistry.