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Short Paper | Regular issue | Vol 100, No. 7, 2020, pp.1072-1083
Published online, 25th May, 2020
DOI: 10.3987/COM-20-14262
Synthesis of Lesinurad via a Multicomponent Reaction with Isocyanides and Disulfides

Yaoqi Li and Zhihua Sun*

*College of Chemistry and Chemical Engineering, Shanghai University of Engineering Science, 333 Longteng Rd., Songjiang, Shanghai, 201620, China

Abstract

An efficient synthesis of Lesinurad, a selective uric acid reabsorption (URAT1) inhibitor, is described in this article. The route to synthesis of Lesinurad avoids the use of thiophosgene and the formation of thiols. The key reaction in this synthesis is construction of the 1,2,4-triazole ring in 72% yield. The title product is obtained in 45% yield over 5 steps.