反应详情

温度

100 °C

To a solution of N-(2-bromo-3,6-dimethylthieno[2,3-b]pyridin-4-yl)-3-chlorobenzenesulfonamide (Example 77) (80 mg, 0.185 mmol) in 1,4-dioxane (2 mL) and water (1 mL) was added 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)isoxazole (36.1 mg, 0.185 mmol), bis(triphenylphosphine)palladium(II) chloride (13.01 mg, 0.019 mmol), and potassium carbonate (90 mg, 0.649 mmol) and the reaction mixture heated at 100° C. using a microwave reactor for 1.5 h. The reaction mixture was then filtered through celite, washing with DCM (30 mL) and the filtrate evaporated to dryness. The resulting material was then purified by MDAP (acidic conditions), to afford the title compound (4.67 mg). LCMS (A) m/z: 420 [M+1]+, Rt 1.09 min (acidic).

1. customfor 1.5 h
2. filtrationThe reaction mixture was then filtered through celite
3. washwashing with DCM (30 mL)
4. customthe filtrate evaporated to dryness
5. customThe resulting material was then purified by MDAP (acidic conditions)