Abstract:

Using DMF as solvent, 3,3′-diaminobenzidine and aromatic aldehydes as starting materials, and KI as catalyst, six new bisbenzimidazoles were synthesized in the presence of air. The structures of the compounds were characterized by means of FTIR, ¹H NMR, ¹³C NMR, MS and elemental analysis. The optimal synthetic conditions were investigated. When the temperature was 150 ℃ and the reaction time was 12 h, the six compounds were obtained with yields in the range of 58.4% to 98.0%. The new method with readily available catalyst is advantageous to conventional synthetic process of bisbenzimidazoles due to its less steps, simpler operations, easier postprocessings and higher yields. The anti-tumor activities of the target compounds were preliminarily examined via MTT method on Bel-7402 cell in vitro, and they exhibited certain inhibition activities.

Key words: Bisbenzimidazoles, Synthesis, Characterization, Anti-cancer activity