反应详情

cis-3-Methoxycarbonyl-5-[N-(1-(4-cyanobenzyl)-1H-imidazol-5-yl)acetylamino]piperidine (35.3 mg, 0.093 mmol), benzaldehyde (32.5 uL, 0.278 mmol), and sodium cyanoborohydride (17.5 mg, 0.278 mmol) was dissolved in MeOH (2 mL) and stirred overnight at ambient temperature. The solution was concentrated under reduced pressure and chromatographed (silica gel, 0.5-2% MeOH/CH2Cl2 with NH4OH) to give the title compound. 1H NMR (CDCl3) δ 7.62 (d, 2H, J=8 Hz), 7.52 (s, 1H), 7.11-7.31 (m, 7H), 6.99 (s, 1H), 6.25 (br s, 1H), 5.24 (s, 2H), 3.86-3.96 (m, 1H), 3.65 (s, 3H), 3.29 (s, 2H), 2.48-2.83 (m, 8H), 2.13-2.24 (m, 1H), 1.83-1.95 (m, 1H), 1.50-1.65 (m, 1H). FAB MS 486 (M+1)

1. concentrationThe solution was concentrated under reduced pressure
2. customchromatographed (silica gel, 0.5-2% MeOH/CH2Cl2 with NH4OH)