Oxidative β-C-H sulfonylation of cyclic amines.

ABSTRACT: 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.

SUBMITTER: Griffiths RJ 

PROVIDER: S-EPMC5897885 | biostudies-literature | 2018 Feb

REPOSITORIES: biostudies-literature