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A transition-metal-free CC double bond cleavage reaction employing molecular iodine is described. In the presence of K2CO3 as the base, I2-mediated CC bond cleavage followed by intramolecular annulation of N-(2-vinylaryl)­pyridin-2-amine substrates produces pyrido­[2,1-b]­quinazolinones and related heterocyclic compounds. This reaction can be completed on a gram scale and has been successfully applied to the synthesis of compounds with important biological properties, including efflux pump inhibitory and antiallergic activities.

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A facile synthesis of novel dispiroheterocycles has been developed through one-pot [3+2] cycloaddition between isatins, amino acids, and aurones. Thirty different dispiroheterocycles were synthesized eusing this method which features mild conditions, convenient operation, and high efficacy. Evaluation of the bioactivity of these dispiroheterocyclic products revealed antiviral activity against tobacco mosaic virus (TMV).

A series of 1-azaaurone derivatives were designed and synthesized from 3,5-dimethoxyaniline and 2-chloroacetonitrile. Their structures were characterized by melting point, 1 H NMR, IR, and elemental analysis, as well as 13 C NMR. The target compounds were evaluated for antitumor activities against human hepatocellular liver carcinoma cell line (HepG-2) and human cervix carcinoma cell line (Hela) using methyl thiazolyl tetrazolium method. The results revealed that several 1-azaaurones exhibited strong proliferation inhibition efficacy against HepG-2 and Hela with an IC 50 range of 5.6-8.8 μg/mL without damaging normal cell.