反应详情

4-Nitrophenyl (4R)-4-(3,4-difluorophenyl)-2-oxo-1,3-oxazolidine-3-carboxylate (169 mg, 0.465 mmol), N-{3-[1-(3-aminopropyl)-4-piperidinyl]phenyl}-2-methylpropanamide (141 mg, 0.465 mmol), K2CO3 (0.193 g, 1.39 mmol), CH2Cl2 (10 mL), and methanol (0.1 mL) were combined in a flask. The mixture was stirred overnight at room temperature, the solvent was removed in vacuo, and the residue was purified by chromatography [2.5% of NH3 (2.0 M in methanol) in CH2Cl2] to afford the desired product (26.1 mg, 10.6%): 1H NMR (400 MHz, CDCl3) δ 8.08 (t, 1H, J=5.5 Hz), 7.45 (S, 2H), 7.38 (d, 1H, J=8.6 Hz), 7.24–7.12 (m, 3H), 7.06 (m, 1H), 6.97.(d, 1H, J=8.6 Hz), 5.40 (dd, 1H, J=3.9–8.8 Hz); 4.71 (t, 1H, J=8.8 Hz), 4.23 (dd, 1H, J=4.4, 9.1 Hz), 3.32 (qt, 2H, J=6.1 Hz), 2.99. (d, 2H, J=11.0 Hz), 2.49 (qt, 2H, J=7.0 Hz), 2.41 (t, 2H, J=7.0 Hz), 1.99–1.97 (m, 2H), 1.82–1.68 (m, 6H), 1.23 (d, 6H, J=7.3 Hz); Anal. Calcd. for C28H34F2N4O4+HCl+0.185CHCl3: C, 57.6; H, 6.04; N, 9.54. Found: C, 58.5; H, 6.08; N, 9.47; ESMS m/e: 529.1 (M+H)+.

1. customthe solvent was removed in vacuo
2. customthe residue was purified by chromatography [2.5% of NH3 (2.0 M in methanol) in CH2Cl2]