反应详情

温度

80 °C

A mixture of methyl 3-(4-bromophenyl)-2,2-dimethyl-3-phenylpropanoate (250 mg, 0.72 mmol), piperidine (3 mL), palladium acetate (32 mg, 0.144 mmol), 2-(di-tert-butylphosphino)-biphenyl (87 mg, 0.29 mmol), and sodium tert-butoxide (166 mg, 1.73 mmol) in toluene (5 ml) was heated at 80° C. for 1.5 h. The reaction mixture was cooled to room temperature, the solid was removed by filtration, and the filtrate was concentrated in vacuo. The crude product was purified by silica gel flash chromatography using 10% ethyl acetate in hexanes to give methyl 2,2-dimethyl-3-phenyl-3-(4-(piperidin-1-yl)phenyl)propanoate as a white solid (207 mg, 82%). LC/MS (m/z) 352.24 [(M+H)+]; HPLC Rt: 2.448 min.

1. temperatureThe reaction mixture was cooled to room temperature
2. customthe solid was removed by filtration
3. concentrationthe filtrate was concentrated in vacuo
4. customThe crude product was purified by silica gel flash chromatography