反应详情

温度

90 °C

PdCl2(dppf) dichloromethane adduct (0.017 g, 0.02 mmol) was added to a suspension of 5-bromo-3-iodo-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-pyrazolo[3,4-b]pyridine (0.185 g, 0.41 mmol), phenylboronic acid (0.050 g, 0.41 mmol) and Na2CO3 (0.064 g, 0.61 mmol) in dimethylether (“DME”)/EtOH/H2O (5:2:1, 8 mL). The reaction mixture was purged with argon for 10 minutes and then heated to 90° C. under argon for 2 hours. The reaction mixture was cooled to room temperature and concentrated. The crude product was purified by column chromatography, eluting with hexanes/ethyl acetate (50:1) to give 5-bromo-3-phenyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-pyrazolo[3,4-b]pyridine (0.080 g, 49%) as an oil.

1. customThe reaction mixture was purged with argon for 10 minutes
2. temperatureThe reaction mixture was cooled to room temperature
3. concentrationconcentrated
4. customThe crude product was purified by column chromatography
5. washeluting with hexanes/ethyl acetate (50:1)