反应详情

A 25 mL round-bottomed flask was charged with a solution of 3-(4-hydroxy-4-methylpiperidin-1-yl)azetidine-1-carboxylic acid tert-butyl ester (0.2 g, 0.74 mmol) in DCM/TFA (3 mL/3 mL). The reaction mixture was stirred for 4 h at room temperature. The reaction mixture was loaded onto an Isolute® SCX-2 cartridge. The cartridge was washed with MeOH and the desired product was eluted using 2 M NH3 in MeOH to give 1-Azetidin-3-yl-4-methylpiperidin-4-ol as a colourless oil (0.107 g, 85%). 1H NMR (CDCl3, 400 MHz) δ 3.61 (t, J=7.3 Hz, 2 H); 3.54 (t, J=7.3 Hz, 2 H); 3.29-3.15 (m, 1 H); 3.04 (s, 2 H); 2.40 (d, J=10.8 Hz, 2 H); 2.30-2.18 (m, 2 H); 1.67-1.56 (m, 4 H); 1.23 (s, 3 H).

1. washThe cartridge was washed with MeOH
2. washthe desired product was eluted