反应详情

A mixture of 4-[methyl(tetrahydrofuran-3-yl)amino]piperidine-1-carboxylic acid tert-butyl ester (132 mg, 0.46 mmol) and TFA (2 mL) in DCM (5 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 Methyl(piperidin-4-yl)(tetrahydro-furan-3-yl)amine as a white solid (84 mg, quant.). 1H NMR (CDCl3, 300 MHz): δ 3.98-3.91 (m, 1H); 3.88-3.83 (m, 1H); 3.80-3.73 (m, 1H); 3.61-3.53 (m, 1H); 3.42-3.35 (m, 1H); 3.26-3.14 (m, 2H); 2.71-2.53 (m, 2H); 2.57-2.46 (m, 1H); 2.23 (s, 3H); 2.05-1.97 (m, 1H); 1.93-1.77 (m, 1H); 1.78-1.72 (m, 2H); 1.64-1.49 (m, 2H).

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