反应详情

To a microwave vial charged with 1-chloro-N-(4-methoxybenzyl)-N-(thiazol-2-yl)isoquinoline-6-sulfonamide (Intermediate JJJ) (87 mg, 0.194 mmol), (2-hydroxy-4-(trifluoromethyl)phenyl)boronic acid (40 mg, 0.194 mmol), potassium carbonate (134 mg, 0.971 mmol) and Pd(Ph3P)4 (22.45 mg, 0.019 mmol) was added Dioxane (971 μl) and Water (324 μl) and irradiated at 100° C. for 30 min affording conversion to desired product as the primary species. The organic layer was decanted, the aqueous rinsed with EtOAc and the combined organics dried under reduced pressure. The crude material was used without further purification. m/z (ESI) 572.3 (M+H)+

1. customirradiated at 100° C. for 30 min