Palladium-catalyzed denitrogenation/vinylation of benzotriazinones with vinylene carbonate

Abstract

Herein, a novel Pd-catalyzed denitrogenation/vinylation of benzotriazinones using vinylene carbonate as the vinylation reagent is reported. This transformation demonstrates an unprecedented skeletal editing approach, effectively converting NN to CC fragments <i>in situ</i> and synthesizing a collection of isoquinolinones with broad-spectrum functional group tolerance. Moreover, the quite concise reaction system and late-stage modification of bioactive molecules comprehensively underscore the practical potential of this protocol.