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

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.