反应详情

A mixture of 3-(4-methyl-3-oxopiperazin-1-yl)azetidine-1-carboxylic acid tert-butyl ester (211 mg, 0.78 mmol) and TFA (2 mL) in DCM (4 mL) was stirred at room temperature for 2 h. The reaction mixture was loaded onto an Isolute® SCX-2 cartridge which was washed with MeOH/DCM and the product eluted with 2M NH3/MeOH affording 4-Azetidin-3-yl-1-methylpiperazin-2-one as a white solid (125 mg, 95%). 1H NMR (CDCl3, 300 MHz): δ 3.63 (m, 4 H); 3.37-3.27 (m, 3 H); 3.03 (s, 2 H); 2.96 (s, 3 H); 2.58 (t, J=5.6 Hz, 2 H); 2.13-1.97 (m, 1 H).

1. washwas washed with MeOH/DCM
2. washthe product eluted with 2M NH3/MeOH