AN EFFICIENT AND CONVENIENT SYNTHESIS OF ACYL CoA: MONOACYLGLYCEROL ACYLTRANSFERASE 2 INHIBITOR, 2-[2-(4-tert-BUTYLPHENYL)ETHYL]-N-[4-(3-CYCLOPENTYL-PROPYL)-2-FLUOROPHENYL]-1,2,3,4-TETRAHYDROISOQUINO-LINE-6-SULFONAMIDE

摘要

An efficient and convenient synthesis of MGAT2 inhibitor, 2-[2-(4-tert-butylphenyl)ethyl]-N44-(3-cyclopentylpropy1)-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.