反应详情

Benzylic amine salt 112e (0.78 g, 1.7 mmol), N,N'-bis-BOC-pyrazole carboxamidine 122f (0.51 g, 1.5 mmol), and Et3N (0.23 mL, 17 mmol), were stirred in THF (5 mL) at room temperature for 44 h. After evaporation of solvent, the product was isolated by chromatography on silica gel, eluting with 30% to 50% EtOAc in hexane, to yield a yellow solid (0.81 g) following solvent evaporation. IR(KBr) cm-1 3328, 2338, 1760, 1726. 1H NMR(300 MHz, CDCl3): 11.54 (br, 1H), 8.60 (br, 1H), 7.91 (m, 2H), 7.74 (d, 1H, J-16 Hz), 7.54-6.81 (m, 6H), 5.95 (s, 1H), 4.75 (s, 2H), 4 . 72 (d, 2H, J=6 Hz), 3.96 (s, 3H), 3.81 (s, 3H), 1.51 (s, 9H), 1.47 (s, 9H). MS (NH3): 598 (base, M+H).

1. customAfter evaporation of solvent
2. customthe product was isolated by chromatography on silica gel
3. washeluting with 30% to 50% EtOAc in hexane