反应详情

Benzylpiperazine (1.3 mL, 8.4 mmol), BINAP (0.43 g, 0.69 mmol), Pd2 dba3 (0.32 g, 0.35 mmol), cesium carbonate (3.25 g, 9.76 mmol) were added to a degassed solution of 7-bromo-5-fluoro-benzofuran-2-carboxylic acid ethyl ester (2.0 g, 6.97 mmol) in toluene (50 mL). The mixture was heated at reflux over night. After cooling, the mixture was filtered through a pad of celite and washed with dichloromethane. The filtrate was concentrated under reduced pressure. The product was purified by flash chromatography (SiO2; hexane/EtOAc, 7/3). Yield: 1.6 g (60%).

1. temperatureThe mixture was heated
2. temperatureat reflux over night
3. temperatureAfter cooling
4. filtrationthe mixture was filtered through a pad of celite
5. washwashed with dichloromethane
6. concentrationThe filtrate was concentrated under reduced pressure
7. customThe product was purified by flash chromatography (SiO2; hexane/EtOAc, 7/3)