Abstract
An I2-DMSO promoted remote difunctionalization reaction of anthranils is reported. This cross-coupling process realizes simultaneous N1- and C5-dicarbonylation of anthranils with a highly atom- and step-economy. The mechanism involves the copper-catalyzed N–O bond cleavage of anthranils and the construction of a new C–C and a C–N bond respectively. The transformation proceeds smoothly in gram-scale, and the product of the reaction could be transformed into other valuable heterocyclic structures.
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