反应详情

温度

90 °C

Tetrakis(triphenylphosphine)palladium(0) (0.15 g, 0.13 mmol), 2-fluorophenylboronic acid (0.93 g, 6.64 mmol) and ethanol (40 mL) were added under an argon atmosphere to a mixture of 51b) (2.0 g, 5.3 mmol) in DME (40 mL) and 2M sodium carbonate solution (5.3 mL). The resulting mixture was heated at 90° C. for 3 h and then filtered through a pad of celite that was subsequently rinsed with dichloromethane (2×50 mL). The filtrate was concentrated and the remnant purified by column chromatography [100-200 mesh silica; dichloromethane/hexane=1:1]. White solid. Yield: 2.0 g (96% of theory). HPLC-MS (method 5): Rt=4.41 min; m/z [M+H]+=394

1. filtrationfiltered through a pad of celite that
2. washwas subsequently rinsed with dichloromethane (2×50 mL)
3. concentrationThe filtrate was concentrated
4. customthe remnant purified by column chromatography [100-200 mesh silica; dichloromethane/hexane=1:1]