反应详情

1,3-Dibenzylpiperidin-4-one (3, R1B=H, Z=benzyl) (3.98 g, 13.96 mmol) was added to a solution of sodium methoxide (0.83 g, 15.36 mmol) in 80 mL of methanol and stirred at ambient temperature for 45 min. The contents were cooled to 0° C. and methylvinyl ketone (1.74 mL, 20.94 mmol) was added over 30 min. The contents were allowed to warm to ambient temperature and stir for 18 h. Concentrated HCl (1.55 mL) was added, the contents were stirred for a further 5 min and the solvents were evaporated to give a brown oil which was triturated in diethyl ether to give the title compound, 1.90 g. LC-MS: RT=2.26 min. (M+H)+ 332.

1. temperatureThe contents were cooled to 0° C.
2. temperatureto warm to ambient temperature
3. stirringstir for 18 h
4. stirringthe contents were stirred for a further 5 min
5. customthe solvents were evaporated
6. customto give a brown oil which
7. customwas triturated in diethyl ether