DOI: 10.1021/acs.joc.6c01009 ISSN: 0022-3263

Copper/Iron-Cocatalyzed Synthesis of Functionalized Quinazolines from gem -Difluoroalkenes and Amidines

Yang Feng, Yanpeng Zhang, Xiangxiang Yan, Ying Fu, Zhengyin Du

Abstract

A novel and efficient method for synthesizing functionalized acyl quinazolines has been developed via CuCl2·2H2O/FeBr3-cocatalyzed cascade cyclization of amidines with readily accessible gem-difluoroalkenes. The reaction proceeds in DMF under an air atmosphere, affording diversely substituted acyl quinazolines in moderate yields. This annulation strategy, based on dual C–F bond cleavage, represents a valuable alternative for constructing cyclization products, offering advantages in synthetic efficiency and substrate availability.

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