反应详情

(S)-4-tert-butyloxazolidine-2,5-dione (1.59 g, 10.12 mmol) and azetidine hydrochloride (0.946 g, 10.12 mmol) were combined in ethanol (5 mL) in a 2 mL microwave vial. The vial was capped and subjected to microwave irradiation at 150° C. for 10 min. The reaction was concentrated under reduced pressure and azeotroped with twice with toluene (5 mL) to provide the desired (S)-2-amino-1-(azetidin-1-yl)-3,3-dimethylbutan-1-one as a brown oil (1.7 g, 99%) that was used without further purification. LCMS (+ESI) m/z: 171.1 [M+H]+.

1. customThe vial was capped
2. customirradiation at 150° C. for 10 min
3. concentrationThe reaction was concentrated under reduced pressure
4. customazeotroped with twice with toluene (5 mL)