反应详情

To a mixture of N-[1-(4-amino-2-fluoro-phenyl)-piperidin-4-yl]-2-ethyl-N-phenyl-butyramide (0.30 mmol) and TEA (2.0 mmol) in DCM (10 mL) was added 2-ethyl-butyryl chloride (1.0 mmol). After 16 h, the mixture was washed with H2O (10 mL). The organic layer was concentrated and the residue was purified by PTLC to provide the title compound (45 mg, 31%). MS (ESI): mass calcd. for C29H40FN3O2, 481.31. m/z found, 482.4 [M+H]+. 1H NMR (CDCl3): 7.50-7.35 (m, 5H), 7.15-7.03 (m, 2H), 6.86 (t, J=8.8, 1H), 4.90-4.72 (m, 1H), 3.44-3.30 (m, 2H), 2.80-2.67 (m, 2H), 2.30-1.30 (m, 14H), 0.95 (t, J=7.3, 6H), 0.80 (t, J=7.2, 6H).

1. washthe mixture was washed with H2O (10 mL)
2. concentrationThe organic layer was concentrated
3. customthe residue was purified by PTLC