反应详情

To a solution of 1-benzyl-4-aminopiperidine (1.13 g) in dichloromethane (10 ml) were added a solution of 4-fluorobenzoyl chloride (0.99 g) in dichloromethane (1 ml) and diisopropylethylamine (1.09 ml) under cooling on an ice-water bath. The mixture was warmed to ambient temperature slowly under stirring. The mixture was diluted with dichloromethane and washed with water, saturated aqueous sodium hydrogen carbonate, water, and brine. After drying with magnesium sulfate, the solvents were removed under reduced pressure. A residue was purified by column chromatography (silica gel 100 ml, dichloromethane:methanol=15:1). After rinse with diisopropyl ether-n-hexane (1:1), N-(1-benzylpiperidin-4-yl)-4-fluorobenzamide (1.31 g) was obtained.

1. temperatureunder cooling on an ice-water bath
2. washwashed with water, saturated aqueous sodium hydrogen carbonate, water, and brine
3. dry with materialAfter drying with magnesium sulfate
4. customthe solvents were removed under reduced pressure
5. customA residue was purified by column chromatography (silica gel 100 ml, dichloromethane:methanol=15:1)
6. washAfter rinse with diisopropyl ether-n-hexane (1:1)