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Published on: June 10, 2021
Iodine-Mediated C═C Double Bond Cleavage toward Pyrido[2,1-b]quinazolinones
Wei Hao1, Kailu Li1, Chenyang Ye1
1Green Catalysis Center and College of Chemistry, Zhengzhou University, Zhengzhou 450001, China.
Abstract:
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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