Synthesis of Benzimidazo[1,2-c]quinazolines via Metal-Free Intramolecular C–H Amination Reaction
2016
Shen, Chao | Wang, Lingfang | Wen, Ming | Shen, Hongyun | Jin, Jianzhong | Zhang, Pengfei
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.
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