反应详情

A solution of benzimidazole-2-aldehyde 1 (0.5 mmol) and diamine 2 (0.5 mmol) in dimethylacetamide (4 mL) was stirred at 100° C. for 12 h. Solvent was evaporated and residue was purified by preparative HPLC to give benzimidazole derivative 3. 1H NMR (300 MHz, MeOH-d4): δ 2.52 (s, 3H), 2.85 (brs, 4H), 3.25 (brs, 4H), 7.05-7.15 (m, 2H), 7.25-7.35 (s overlapped with m, 2H), 7.60-7.75 (m, 4H); LCMS m/z 333 (M+H+), ELSD 99%.

1. customSolvent was evaporated
2. customresidue was purified by preparative HPLC