Transition‐Metal‐Catalyzed Synthesis of Spiro Compounds through Activation and Cleavage of C−H Bonds

Abstract Spirocyclic compounds represent an imperative class of naturally occurring substances characterized by their potential biological properties. They receive much attention as scaffolds in modern drug discovery programs and widespread applications in asymmetric organic synthesis as chiral catalysts and ligands because of their structural rigidity and excellent stereochemical recognition. With the advent of C−H activation/annulation, their synthesis enters into a new dimension with the formation of novel spiro cycles. The present review highlights the advances in transition‐metal‐catalyzed synthesis of spirocyclic compounds triggered by C−H bond activation.