Photocatalytic N‐Alkylation of NH‐Sulfoximines via Anti‐Markovnikov Hydroamination of Alkenes

Abstract

AbstractSulfoximines, the isoelectronic with sulfones, represent a class of alternative and intriguing motifs in both discovery program and agrochemistry. N‐Alkylation on imines could significantly improve their bioactivities, but the lack of general method has hindered their further uptake by medicinal chemistry and drug development. Herein, we present a mild photocatalytic anti‐Markovnikov hydroamination of alkenes to construct N‐alkylated sulfoximines with broad substrate tolerance on primary, secondary and tertiary alkyl substituents as well as a diverse range of sulfoximines. The mechanistic studies support the photocatalytic pathway, and demonstrate that the alkene radical cation rather than the iminium radical serves as the key intermediate in the transformation.