反应详情

温度

100 °C

453 mg (1.25 mmol) 7-bromo-6-fluoro-2-(4-methoxy-benzyl)-2H-isoquinolin-1-one (313), 432 mg (3.125 mmol) K2CO3 and 190.5 mg (1.56 mmol) phenylboronic acid were dissolved in 12.5 mL toluene. Under Argon, 72 mg (0.062 mmol) Pd(Ph3)4 were added and the solution was stirred at 100° C. After complete conversion, the solvent is removed i. vac. and saturated sodium bicarbonate solution is added. The aqueous solution is extracted three times with dichloromethane and the organic layers are dried with MgSO4. After evaporation, the crude product is purified by preparative HPLC. Rt=1.80 min (Method C). Detected mass: 360.4 (M+H+).

1. customAfter complete conversion, the solvent is removed i
2. additionand saturated sodium bicarbonate solution is added
3. extractionThe aqueous solution is extracted three times with dichloromethane
4. dry with materialthe organic layers are dried with MgSO4
5. customAfter evaporation
6. customthe crude product is purified by preparative HPLC