Rhodium-catalyzed C-H bond activation alkylation and cyclization of 2-arylquinazolin-4-ones. 2018

Minhao Lou, and Zhihong Deng, and Xuechun Mao, and Yang Fu, and Qin Yang, and Yiyuan Peng
Key Laboratory of Functional Small Organic Molecule, Ministry of Education, Jiangxi Province's Key Laboratory of Green Chemistry, Jiangxi Normal University, Nanchang, Jiangxi 330022, China. yypeng@jxnu.edu.cn.

An efficient method for the synthesis of isoquinolino[1,2-b]quinazolin-8-one derivatives and 12-methyl-12H-isoindolo[1,2-b]quinazoline-10-one derivatives is described herein. With rhodium catalysis, the desired products are obtained through a sequence reaction of C-H activation-based alkenylation and intramolecular aza-Heck-type cyclization. The developed method has a wide range of substrate tolerance under mild conditions and provides an alternative for the structural elaboration of quinazoline compounds.

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