Copper-mediated C−H functionalization has emerged as a powerful strategy for the selective modification of nitrogen-containing molecules, offering significant advancements in organic synthesis. This review provides a comprehensive overview of recent developments in copper-catalyzed C−H functionalization reactions of amines, imines, and amides, from 2013 to present, emphasizing their synthetic applications and mechanistic insights. It also discusses the impact of these methodologies on the construction of complex molecular architectures, including pharmaceuticals and natural products. This review aims to provide valuable guidance for researchers seeking to leverage copper-mediated strategies in their synthetic endeavors by creating current knowledge and identifying future directions. We have highlighted the new bonds formed through C−H functionalizations for the convenience of readers.

铜介导的 C-H 官能团化已成为选择性修饰含氮分子的强大策略，为有机合成提供了重大进展。本文全面概述了 2013 年至今铜催化的胺、亚胺和酰胺的 C-H 官能化反应的最新进展，强调了它们的合成应用和机理见解。它还讨论了这些方法对复杂分子结构（包括药物和天然产物）构建的影响。本综述旨在通过创造当前知识和确定未来方向，为寻求在合成工作中利用铜介导策略的研究人员提供有价值的指导。为了方便读者，我们重点介绍了通过 C-H 官能团化形成的新键。