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.