Abstract Nitrogen‐containing heterocyclic compounds are the core skeletons of many natural products, bioactive molecules and drugs, and the transition metal‐catalyzed hydrazine‐directed C−H bond activation/annulation reactions is one of the effective methods for the synthesis of nitrogen‐containing heterocyclic compounds. In this review, the important research progress of transition metal‐catalyzed hydrazine‐directed C−H bond activation reactions for the synthesis of nitrogen‐containing heterocyclic compounds is reviewed according to the size of the constructed nitrogen‐containing heterocycles, and the substrate scope and reaction mechanism are discussed in detail, and the limitations and future development prospects are summarized and outlooked.