Progress in Transition‐Metal‐Catalyzed C–H Functionalization of 2‐Arylthiazoles and 2‐Arylbenzothiazoles

Heterocyclic compounds play a central role in modern organic chemistry, underpinning the structural frameworks of numerous bioactive molecules and functional materials. In particular, 2‐arylthiazoles and 2‐arylbenzothiazoles have emerged as privileged sulfur‐containing heteroarenes, valued for their diverse biological activities and favorable electronic properties. Their rigid, π‐conjugated architectures enable broad applications ranging from medicinal chemistry to optoelectronic materials. Consequently, efficient methods for their synthesis and selective structural modification are of considerable importance. While classical synthetic routes and cross‐coupling strategies provide access to these scaffolds, their reliance on prefunctionalized substrates and multistep sequences limits synthetic efficiency and late‐stage diversification. In response, transition‐metal‐catalyzed C–H functionalization has become a powerful alternative, allowing direct and atom‐economical modification of heteroarenes. Recent advances have addressed the inherent challenges of sulfur‐containing substrates, enabling precise regioselective and regiodivergent transformations. This review summarizes recent progress in transition‐metal‐catalyzed C–H functionalization of 2‐arylthiazoles and 2‐arylbenzothiazoles, highlighting key reaction modes, mechanistic insights, and representative applications.