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Historically, precious metals have dominated C\u2500H amination chemistry but often suffer from limitations, including high cost, toxicity, and limited availability. In contrast, copper\u2010based reactions offer several advantages: it is cost\u2010effective, less toxic, earth\u2010abundant, biocompatible, and environmentally benign, while minimizing the formation of undesired byproducts. This transformation enables the streamline synthesis of pharmacologically relevant heterocycles and alkaloids, offering access to bioactive molecules with enhanced therapeutic potential. This review highlights recent advances in design, mechanistic insights, and synthetic applications of copper\u2010mediated C\u2500H amination in medicinal chemistry. Particular emphasis is placed on its role in the construction of complex nitrogen frameworks and its integration into drug discovery and development. 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