Trifluoroacetic acid → 4-(Azetidin-3-yl)piperazin-2-one

Participants

Reaction Steps

A mixture of 3-(3-oxopiperazin-1-yl)azetidine-1-carboxylic acid tert-butyl ester (400 mg, 1.57 mmol) and TFA (3 mL) in DCM (6 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-ylpiperazin-2-one as a white solid (227 mg, 93%). 1H NMR (CDCl3, 300 MHz): δ 6.08 (s, 1 H); 3.63-3.56 (m, 3 H); 3.42-3.35 (m, 3 H); 3.31 (t, J=6.74 Hz, 1 H); 3.03 (s, 2 H); 2.59-2.51 (m, 2 H).

Provenance & Evidence