Abstract: | Strained ring systems are regarded as privileged coupling partners in directed C?H bond functionalization and have emerged as a potential research area in organic synthesis. The inherent ring strain in these systems acts as a driving force, allowing the facile construction of diversified structural scaffolds via integrating C?H activation and ring‐scission. The mechanistic underpinnings allows the implementation of a plethora of C?H bonds across plentiful organic substrates, including the less reactive alkyl ones. Considering the synthetic space, this area will foster developments of novel synthetic methods in chelation guided C?H functionalization. This review will focus on recent developments in transition‐metal catalyzed chelation assisted concomitant C?H activation and ring scission of strained rings to attain molecular complexity. |