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A Brønsted acid-catalyzed addition of 2-alkylazaarenes to in situ generated N-sulfonylimines through selective C(sp3)–H bond functionalization has been developed. This protocol provides an atom- and step-economic approach to α-substituted sulfonamides.

Graphical abstract: 3-Component synthesis of α-substituted sulfonamides via Brønsted acid-catalyzed C(sp3)–H bond functionalization of 2-alkylazaarenes

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