biostudies-literatureUnknown9(8)Griffiths RJGlaxoSmithKlineA transition metal-free strategy for the dehydrogenative β-sulfonylation of tertiary cyclic amines is described. N-Iodosuccinimide facilitates regioselective oxidative sulfonylation at C-H bonds positioned β to the nitrogen atom of tertiary amines, installing enaminyl sulfone functionality in cyclic systems. Mild reaction conditions, broad functional group tolerance and a wide substrate scope are demonstrated. The nucleophilic character of the enaminyl sulfone is harnessed, demonstrating potential application for scaffold diversification.Chemical science2295-2300https://www.ebi.ac.uk/biostudies/studies/S-EPMC5897885biostudies-literatureOxidative β-C-H sulfonylation of cyclic amines.PMC5897885Griffiths RJKong WCTalbot EPARichards SABurley GAWillis MCfalseOxidative β-C-H sulfonylation of cyclic amines.A transition metal-free strategy for the dehydrogenative β-sulfonylation of tertiary cyclic amines is described. N-Iodosuccinimide facilitates regioselective oxidative sulfonylation at C-H bonds positioned β to the nitrogen atom of tertiary amines, installing enaminyl sulfone functionality in cyclic systems. Mild reaction conditions, broad functional group tolerance and a wide substrate scope are demonstrated. The nucleophilic character of the enaminyl sulfone is harnessed, demonstrating potential application for scaffold diversification.2018-01-01T00:00:00Z2018 Feb2025-04-04T13:34:26.192Z2019-03-26T23:36:06ZS-EPMC58978852971970310.1039/c7sc04900e