反应详情

温度

100 °C

To a solution 5-bromo-3-(1-{[3-(dimethylamino)propyl]sulfonyl}-4-piperidinyl)-1H-indazole-7-carboxamide (Intermediate 8) (20 mg, 0.04 mmol) in dioxane/water (1:1, 5 mL) was added {4-[(trifluoromethyl)oxy]phenyl}boronic acid (30 mg, 0.12 mmol), potassium carbonate (40 mg), and Pd(dppf)Cl2 (8 mg). The reaction mixture was heated at 100° C. for 1800 seconds. The contents of the vial were partitioned between ethyl acetate and water. The organic phase was washed with water, dried over MgSO4, filtered, and concentrated to give 0.62 g of a yellow solid. This was purified via silica gel chromatography using 20% ethyl acetate/pentane as the mobile phase to give the title compound (5 mg, 23%).

1. customThe contents of the vial were partitioned between ethyl acetate and water
2. washThe organic phase was washed with water
3. dry with materialdried over MgSO4
4. filtrationfiltered
5. concentrationconcentrated