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Short Paper | Regular issue | Vol 102, No. 4, 2021, pp.743-749
Published online, 26th February, 2021
DOI: 10.3987/COM-21-14414
Synthesis of Anti-Insomnia Drug Suvorexant

Hongshun Yuan, Lei Guo,* and Xianhua Pan*

*School of Perfume and Aroma Technology, Shanghai Institute of Technology, 100 Haiquan Road, Shanghai, 201418, China.

Abstract

Suvorexant is the first dual orexin receptor antagonist for treating insomnia. Although numerous methods have been developed to construct suvorexant, a generally efficient, mild, facile synthesis platform for the conversion of simple starting material to this highly enantioselective scaffold via successive C–N bond forming steps remains in high demand. Here we report an efficient synthetic route without using chiral HPLC separation, resolution, enzyme catalysis or transition metal catalysis, and the total yield is up to 37%.