反应详情

温度

30 °C

Potassium carbonate (254 mg, 1.846 mmol, 2.0 eq), Pd2(dba)3 (84 mg, 0.0923 mmol, 0.1 eq) and tri-tert-butylphosphonium tetrafluoroborate (13 mg, 0.046 mmol, 0.05 eq) were added to a solution of (1-(5-bromopyrimidin-2-yl)-3-(methylthio)-1H-indol-6-yl)(morpholino)methanone (400 mg, 0.923 mmol, 1.0 eq) and (1-methyl-1H-pyrazol-4-yl)boronic acid (140 mg, 1.108 mmol, 1.2 eq) in THF/water (20 mL, 4:1) stirred under an argon atmosphere at 30° C. The reaction mixture was stirred at the same temperature for 2 h and the cooled to ambient temperature and diluted with ethyl acetate (10 mL). The mixture was filtered through a pad of celite, washed with water, dried over sodium sulfate and evaporated. The residue was purified by column chromatography [100-200 mesh, 2% methanol in dichloromethane]. White solid. Yield: 380 mg (95% of theory)

1. stirringThe reaction mixture was stirred at the same temperature for 2 h
2. temperaturethe cooled to ambient temperature
3. filtrationThe mixture was filtered through a pad of celite
4. washwashed with water
5. dry with materialdried over sodium sulfate
6. customevaporated
7. customThe residue was purified by column chromatography [100-200 mesh, 2% methanol in dichloromethane]