反应详情

温度

95 °C

To a 150 mL screw-cap vessel under nitrogen was added 5-bromo-4,7-diazaindole (1.0 g, 5.05 mmol), 4-bromo-2-fluorophenyl boronic acid (1.33 g, 6.06 mmol), Pd(dppf)Cl2.CH2Cl2 (0.2 g, 0.24 mmol), K2CO3 (2.09 g, 15.2 mmol), 1,4-dioxane (35 mL) and water (13 mL). The mixture was sparged with nitrogen for 10 minutes, the vessel capped and the reaction heated at 95° Celsius for 24 hours. The reaction was then cooled to rt, diluted with ethyl acetate (200 mL) and washed with water (1×100 mL) and brine (1×100 mL). The organic layer was dried with Na2SO4 and evaporated to dryness. The crude product was purified by HPLC giving the title compound (515 mg, 35%). MS (ESI): mass calcd. for C12H7BrFN2, 290.98; m/z found, 292.0 [M+H]+.

1. customTo a 150 mL screw-cap vessel under nitrogen
2. customThe mixture was sparged with nitrogen for 10 minutes
3. customthe vessel capped
4. temperatureThe reaction was then cooled to rt
5. additiondiluted with ethyl acetate (200 mL)
6. washwashed with water (1×100 mL) and brine (1×100 mL)
7. dry with materialThe organic layer was dried with Na2SO4
8. customevaporated to dryness
9. customThe crude product was purified by HPLC