Cobalt-Catalyzed Three-Component Synthesis of α-Substituted N-Sulfonyl Amines via C(sp2)–H Bond Activation

Abstract Herein, we report a three-component synthesis of α-substituted N-sulfonyl amines from aryl aldehydes, primary sulfonamides, and (hetero)arenes as readily available building blocks. This method is based on the direct functionalization of (hetero)arenes via a cobalt-catalyzed C(sp2)–H bond activation. It enables the modular synthesis of highly substituted sulfonamides as interesting scaffolds for pharmaceutical applications in good yields with a high degree of structural diversity. The applicability of this method in the context of pharmaceutical research was demonstrated by the late-stage modification of active pharmaceutical ingredients and drug-like compounds. Overall, this process offers an interesting and atom-economical alternative to classical approaches for the preparation of α-arylated amines, such as the Petasis reactions or similar processes based on organometallic reagents.