反应详情

A mixture of 3-(3,3-difluoropyrrolidin-1-yl)azetidine-1-carboxylic acid tert-butyl ester (193 mg, 0.74 mmol) and TFA (1 mL) in DCM (2 mL) was stirred at room temperature for 2 h. The reaction mixture was loaded onto an Isolute® SCX-2 cartridge, washed with MeOH/DCM and eluted with 2M NH3/MeOH affording 1-Azetidin-3-yl-3,3-difluoropyrrolidine as a white solid (122 mg, quant.). 1H NMR (CDCl3, 300 MHz): δ 3.63 (m, 4 H), 3.48 (m, 1 H), 2.87 (t, J=13.1 Hz, 2 H), 2.70 (t, J=7.0 Hz, 2 H) and 2.29 (m, 2 H)

1. washwashed with MeOH/DCM
2. washeluted with 2M NH3/MeOH