Transition metal-catalyzed direct functionalization of C–H bonds has recently emerged as a powerful strategy for the construction of carbon–carbon and carbon–heteroatom bonds. Among various metals employed, base metal copper has attracted significant attention owing to its relatively low cost, abundance, and versatile reactivity. This review aims to comprehensively summarize the recent advances in copper-mediated (both stoichiometric and catalytic) chelation-assisted functionalization of unactivated C–H bonds.