反应详情

温度

130 °C

To a solution of 4-fluorobenzaldehyde (5 g, 40.2 mmol) in N,N-dimethylformamide (130 mL) was added potassium carbonate (8.35 g, 60.4 mmol) and 1-piperazin-1-ylethanone (10.3 g, 80.5 mmol) and the reaction was stirred at 130° C. for 16 hours. The reaction was then cooled to ambient temperature, diluted with EtOAc and washed with water (×2) and brine. The organic layer was then dried with MgSO4, concentrated and purified by silica gel column chromatography (0-10% methanol in dichloromethane) to give 4-(4-acetylpiperazin-1-yl)benzaldehyde (5.96 g, 64% yield). LCMS (m/z) ES+ 233 [M+1]+.

1. temperatureThe reaction was then cooled to ambient temperature
2. washwashed with water (×2) and brine
3. dry with materialThe organic layer was then dried with MgSO4
4. concentrationconcentrated
5. custompurified by silica gel column chromatography (0-10% methanol in dichloromethane)