反应详情

To a solution of 3-bromo-1-tosylindole (105 mg, 0.3 mmol) and anhydrous piperazine (258 mg, 3.0 mmol) in toluene (4.5 mL) was added palladium acetate (13.4 mg, 0.055 mmol), BINAP (40.3 mg, 0.065 mmol), and cesium carbonate (318 mmol, 0.9 mmol), and the resulting mixture was refluxed for 6 hours. The reaction solution was cooled to room temperature and the precipitated salt was separated by filtration, and the filtrate was concentrated to afford a crude product. The crude product was purified by column chromatography on a silica gel (eluent; ammonia-saturated chloroform) to afford the title compound (69 mg, yield: 65%) as a colorless viscous oil.

1. temperaturethe resulting mixture was refluxed for 6 hours
2. customthe precipitated salt was separated by filtration
3. concentrationthe filtrate was concentrated
4. customto afford a crude product
5. customThe crude product was purified by column chromatography on a silica gel (eluent; ammonia-saturated chloroform)