Recent Advances in Tandem CH Activation and Named Reactions Toward Structurally Diverse Small‐Molecule Heterocycles: Synergistic Effects and Mechanistic Insights

Transition‐metal‐catalyzed chelation‐assisted CH activation has emerged as an important tool in modern organic synthesis. Small‐molecule heterocyclic compounds, owing to their distinctive electronic properties and spatial configurations, exhibit diverse pharmacological effects. Consequently, research on their synthetic methodologies has garnered substantial attention from both academia and industry. In recent years, researchers have developed a series of tandem strategies integrating CH activation with classical named reactions, providing novel approaches for the efficient construction of heterocyclic frameworks. This review summarizes recent advances in transition‐metal‐catalyzed tandem CH activation/named reaction strategies in facilitating heterocycle assembly, while providing in‐depth mechanistic analysis of the tandem processes.