2-Cyano-4-(trifluoromethyl)phenylboronic acid → 1-(2-cyano-4-(trifluoromethyl)phenyl)-N-(2,4-dimethoxybenzyl)-N-(thiazol-2-yl)isoquinoline-6-sulfonamide

Participants

Reaction Steps

The titled compound was prepared in an analogous manner to that of INTERMEDIATE DD, except that 1-chloro-N-(2,4-dimethoxybenzyl)-N-(thiazol-2-yl)isoquinoline-6-sulfonamide (Intermediate OOO) and (2-cyano-4-(trifluoromethyl)phenyl)boronic acid were used as the coupling partners. The material was purified via silica gel column chromatography (12 g, gradient elution 0 to 50% EtOAc:Heptane) to afford 1-(2-cyano-4-(trifluoromethyl)phenyl)-N-(2,4-dimethoxybenzyl)-N-(thiazol-2-yl)isoquinoline-6-sulfonamide as a light yellow solid. m/z (ESI) 629.3 (M+H)+.

Provenance & Evidence