2,2,2-Trifluoroethanol → (R)-2-amino-1-(3,3-difluoro-azetidin-1-yl)-propan-1-one

Participants

Reaction Conditions

Reaction Steps

A 5 ml microwave vial was charged with [(R)-2-(3,3-difluoro-azetidin-1-yl)-1-methyl-2-oxo-ethyl]-carbamic acid tert-butyl ester (170 mg, 0.64 mmol) and 2,2,2-trifluoroethanol (2.4 ml, 32.9 mmol). The vial was flushed with argon, sealed and heated at 150° C. under microwave irradiation for 3 h. The reaction mixture was concentrated to afford 102 mg (97%) of (R)-2-amino-1-(3,3-difluoro-azetidin-1-yl)-propan-1-one as a brown oil which was used without further purification.

Provenance & Evidence