文摘
A series of benzimidazo[1,2-c]quinazolines have been synthesized via phenyliodine(III) diacetate (PIDA)-mediated intramolecular C–H bond cycloamination reaction. This method results in a direct oxidative C–N bond formation in a complex molecule by using a metal-free protocol. A plausible reaction mechanism was described on the basis of the experiments. Some new compounds were evaluated for their antitumor activity against HUH 7 and SK-HEP-1 hepatocarcinoma cell line. Among the compounds screened, 4m was found to be the most active compound against HUH 7.