反应详情

A mixture of 3-(2,2-dimethylmorpholin-4-yl)azetidine-1-carboxylic acid tert-butyl ester (492 mg, 1.82 mmol) and TFA (5 mL) in DCM (10 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 4-Azetidin-3-yl-2,2-dimethylmorpholine as a white solid (302 mg, 97%). 1H NMR (CDCl3, 300 MHz): δ 3.73 (t, J=4.8 Hz, 2 H); 3.64-3.51 (m, 4 H); 3.18-3.11 (m, 1 H); 2.23 (t, J=4.8 Hz, 2 H); 2.23-2.07 (m, 1 H); 2.06 (s, 2 H); 1.25 (s, 6 H).

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