反应详情

To a stirred solution of 1-benzhydryl-3-(4,4′-dichlorobenzhydryloxy)azetidine (35) (8.4 mmol) in dichloromethane (50 mL) was added 1-chloroethylchloroformate (16.9 mmol) dropwise at 0° C. and the reaction mixture was stirred at reflux for 6 hours. The reaction mixture was cooled to room temperature, concentrated in vacuo, then dissolved in methanol (50 mL) and stirred at room temperature for overnight. The reaction mixture was reduced in vacuo and triturated with diethyl ether (100 mL) to afford the desired product as a white solid (2.16 g, 74%).

1. temperatureat reflux for 6 hours
2. concentrationconcentrated in vacuo
3. dissolutiondissolved in methanol (50 mL)
4. stirringstirred at room temperature for overnight
5. customtriturated with diethyl ether (100 mL)