Cesium carbonate → 1-(2-(Cyanomethoxy)-4-(trifluoromethyl)phenyl)-N-(4-methoxybenzyl)-N-(thiazol-2-YL)isoquinoline-6-sulfonamide

Participants

Reaction Conditions

Reaction Steps

To a vial charged with 1-(2-hydroxy-4-(trifluoromethyl)phenyl)-N-(4-methoxybenzyl)-N-(thiazol-2-yl)isoquinoline-6-sulfonamide (111 mg, 0.194 mmol) was added DMF (777 μl) and Cs2CO3 (190 mg, 0.583 mmol) and bromoacetonitrile (46.6 mg, 0.39 mmol) respectively. The mixture was heated to 60° C. overnight affording conversion to desired product fairly cleanly. The mixture was dried under reduced pressure and purified with a 25 g Interchim column (25 um silica) ramping EtOAc in heptane (0-100%, 10% DCM throughout) affording product as a light brown solid. m/z (ESI) 611.3 (M+H)+

Provenance & Evidence