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Synthesis of β-Methylsulfonylated N-Heterocycles from Saturated Cyclic Amines with the Insertion of Sulfur Dioxide

Yan He, Jintao Yang, Qimeng Liu, Xinying Zhang, Xuesen Fan

2020The Journal of Organic Chemistry27 citationsDOI

Abstract

)-H methylsulfonylation of inactivated cyclic amines with the promotion and participation of inorganic sodium metabisulfite and dicumyl peroxide (DCP) has been developed. Notably, bifunctional DCP acted not only as an oxidant to promote the dehydrogenation but also as a methyl radical to participate in the sulfone formation. With this protocol, a number of β-methylsulfonylated tetrahydropyridines, tetrahydroazepines, and pyrroles were obtained in a facile one-pot manner.

Topics & Concepts

ChemistryDehydrogenationBifunctionalSulfur dioxideSodium metabisulfiteCyclohexanoneSulfoneOrganic chemistrySulfurPeroxideHydrogen peroxideCatalysisMedicinal chemistryCombinatorial chemistrySulfur-Based Synthesis TechniquesChemical Synthesis and ReactionsCatalytic C–H Functionalization Methods
Synthesis of β-Methylsulfonylated N-Heterocycles from Saturated Cyclic Amines with the Insertion of Sulfur Dioxide | Litcius