反应详情

1-Chloroethyl chloroformate (136 μL, 1.25 mmol) was added to a solution of 1-benzhydryl-3-(3,3,3-trifluoropropoxy)-azetidine (400 mg, 1.19 mmol) in dichloromethane (10 mL) at 0° C. The reaction mixture was stirred for 1 hour. Ethanol (10 mL) was added and the reaction mixture was stirred for 1 hour at room temperature and for 2 hours at 45° C. After concentration to dryness, the crude mixture was triturated in petroleum ether (2×20 mL) to give a yellow oil (245 mg, quantitative) which was used in the next step without further purification.

1. stirringthe reaction mixture was stirred for 1 hour at room temperature and for 2 hours at 45° C
2. concentrationAfter concentration to dryness
3. customthe crude mixture was triturated in petroleum ether (2×20 mL)
4. customto give a yellow oil (245 mg, quantitative) which
5. customwas used in the next step without further purification