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Paper | Regular issue | Vol 92, No. 3, 2016, pp.470-484
Published online, 2nd February, 2016
DOI: 10.3987/COM-15-13387
■ An Efficient and Convenient Synthesis of Acyl CoA: Monoacylglycerol Acyltransferase 2 Inhibitor, 2-[2-(4-tert-Butylphenyl)ethyl]-N-[4-(3-cyclopentylpropyl)-2-fluorophenyl]-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide

Tsuyoshi Busujima* and Hiroaki Tanaka

*Medicinal Chemistry 3, Taisho Pharmaceutical Co., Ltd., 1-403 Yoshino-cho Kita-ku Saitama 331-9530, Japan

Abstract

An efficient and convenient synthesis of MGAT2 inhibitor, 2-[2-(4-tert-butylphenyl)ethyl]-N-[4-(3-cyclopentylpropyl)-2-fluorophenyl]-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide (1), is reported. The optimized route consists of an effective chlorosulfonylation and debromination, resulting in an increase in the total yield from 6.8% to 45%, compared with our previous method. This synthetic approach enabled the synthesis of 1 to be scaled-up to a multi-gram scale.