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The interplay between copper catalysts and molecular oxygen provides the opportunity to control the promiscuous catalytic behaviors in aerobic Csp3–H bond oxidations without using stoichiometric amounts of oxidants. This mini-review aims to cover the Cu-catalyzed aerobic benzylic and α-carbonyl Csp3–H oxidations and that of the carbon next to an amine group in the past five years. The development of tandem multicomponent reactions employing aerobic Csp3–H bond oxidations will be discussed to highlight the controlled catalyst behaviors and the catalyst interactions between multiple reaction components.

Graphical abstract: Recent advances in the copper-catalyzed aerobic Csp3–H oxidation strategy

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