Recent Trends in Copper-Catalyzed C−H Amination Routes to Biologically Important Nitrogen Scaffolds

Nitrogen‐containing heterocycles have found remarkable applications in natural product research, material sciences, and pharmaceuticals. Although the synthesis of this interesting class of compounds attracted the interest of generations of organic chemists, simple and straightforward assembly methods based on transition‐metal catalysis have regularly been elusive. The recent advancements in the development of C−H functionalization have helped in accomplishing the synthesis of a variety of complex heterocycles from simple precursors. This Focus Review summarizes the recent advances in one particular field: the copper‐catalyzed C−N bond formation reactions via C−H bond functionalization to furnish a comprehensive range of nitrogen heterocycles. Applicability and synthetic feasibility of a particular reaction represent major requirements for the inclusion in this review. The recent advancement in copper‐catalyzed C−H amination provided simple and straightforward routes with environmentally benign and scalable procedures for the synthesis of biologically relevant heterocycles. The mechanistic evolution of this method allowed for thorough understanding and subsequent development, which further delivered efficient protocols for the synthesis of various nitrogen scaffold including drug molecules. This review highlights the importance of copper catalysis and its recent applications of C−H amination reactions in the synthesis of a variety of heterocycles.