Abstract
Abstract 2‐Pyridone, 2‐pyrone, and their benzo‐fused congeners are privileged heterocyclic scaffolds that are widely found in natural products and drug molecules. The late‐stage functionalization of CH bonds in these heterocyclic scaffolds has been an important research area in synthetic organic chemistry as they provide straightforward and easy access to valuable bioactive derivatives. This article outlines transition metal‐catalyzed CH functionalizations of 2‐pyridones, 2‐pyrones, and their benzo‐fused congeners. It can be classified into several major categories in terms of the methodologies involved: (i) intermolecular CH functionalization without the directing groups, (ii) intermolecular CH functionalization using directing groups, and (iii) intramolecular CH functionalization.
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