(2-Methoxy-4-(trifluoromethyl)phenyl)boronic acid → 4-fluoro-1-(2-methoxy-4-(trifluoromethyl)phenyl)-N-(1,2,4-thiadiazol-5-yl)isoquinoline-6-sulfonamide

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Reaction Steps

The title compound was prepared in an analogous manner to that of EXAMPLE 228, except that 1-chloro-N-(2,4-dimethoxybenzyl)-4-fluoro-N-(1,2,4-thiadiazol-5-yl)isoquinoline-6-sulfonamide and (2-methoxy-4-(trifluoromethyl)phenyl)boronic acid were used as the coupling partners. The final compound was purified via column chromatography (RediSep Gold 12 g silica gel column, gradient elution 0-10% MeOH:DCM) to afford 4-fluoro-1-(2-methoxy-4-(trifluoromethyl)phenyl)-N-(1,2,4-thiadiazol-5-yl)isoquinoline-6-sulfonamide as an off-white solid. 1H NMR (400 MHz, DMSO-d6) δ=8.76 (s, 1H), 8.49 (d, J=9.3 Hz, 2H), 8.00 (d, J=8.4 Hz, 1H), 7.81 (d, J=8.4 Hz, 1H), 7.64-7.42 (m, 3H), 3.75 (s, 3H). m/z (ESI) 485.0 (M+H)+.

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