反应详情

A solution of 200 mg (0.551 mmol) of (2R*,4S*)-2-benzyl-1-(3,5-dichlorobenzoyl)-4-piperidinamine and 110 mg (0.606 mmol) of benzophenone in 5 ml of toluene are kept at reflux for 18 hours. The reaction mixture is then concentrated in a rotary evaporator and dissolved in 3 ml of methanol, and 69 mg (1.10 mmol) of sodium cyanoborohydride are added at RT. The reaction mixture is adjusted to pH=5 with 80 μl of acetic acid and stirred at RT for 68 hours. The title compound ##STR98## is obtained as white foam (120 mg, 41%). TLC: toluene/ethyl acetate (7:3) Rf =0.79, FD-MS: M+ =528,530; IR: 1630 cm-1.

1. temperatureat reflux for 18 hours
2. concentrationThe reaction mixture is then concentrated in a rotary evaporator
3. dissolutiondissolved in 3 ml of methanol