反应详情

To a microwave vial containing Na2CO3 (1.216 ml, 2.432 mmol), (6-fluoro-2-methoxypyridin-3-yl)boronic acid (0.166 g, 0.973 mmol) and 1-chloro-N-(pyrimidin-4-yl)isoquinoline-6-sulfonamide (0.26 g, 0.811 mmol) and Dioxane (4.05 ml) was added tetrakis(triphenylphosphine)palladium (0.094 g, 0.081 mmol) and purged with nitrogen and irradiated at 100° C. for 30 min. The reaction mixture was diluted with DMSO to dissolve the observed yellow ppt. Purification was done on reverse phase HPLC with 0.1% NH4OH in ACN and water as mobile phase to obtain 1-(6-fluoro-2-methoxypyridin-3-yl)-N-(pyrimidin-4-yl)isoquinoline-6-sulfonamide (133.2 mg, 0.324 mmol, 39.9% yield) as yellow solid; m/z (ESI) 412.0 (M+H)+.

1. custompurged with nitrogen
2. customirradiated at 100° C. for 30 min
3. additionThe reaction mixture was diluted with DMSO
4. dissolutionto dissolve the observed yellow ppt
5. customPurification