反应详情

1-Chloroethyl chloroformate (90 μL, 0.84 mmol) was added to a solution of 1-benzhydryl-3-((3-methylthiophen-2-yl)methoxy)azetidine (290 mg, 0.83 mmol) in dichloromethane (9 mL) at 0° C. The reaction mixture was stirred 3 hours, then 30 minutes at room temperature. Ethanol (9 mL) was added and the reaction mixture was stirred at 35° C. for an additional 3 hours. After concentration to dryness, the crude was triturated in pentane to give a yellow solid (200 mg, quantitative) which was used in the next step without further purification.

1. custom30 minutes
2. customat room temperature
3. stirringthe reaction mixture was stirred at 35° C. for an additional 3 hours
4. concentrationAfter concentration to dryness
5. customthe crude was triturated in pentane
6. customto give a yellow solid (200 mg, quantitative) which
7. customwas used in the next step without further purification