Abstract

AbstractA copper‐catalyzed aerobic oxidative annulation of amidines with dichloromethane was first demonstrated. Using this novel approach, 16 examples of symmetrical 2,4‐disubstitued 1,3,5‐triazines and 7 examples of unsymmetrical ones were obtained with up to 82% yields. Moreover, a D‐labeling experiment proved that dichloromethane was employed as the C1 building block and solvent. A primary kinetic isotope effect revealed that the C−H cleavage of dichloromethane might be a rate‐determining step. This protocol provides a novel strategy for the synthesis of heterocycles.magnified image

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