Guoling Huang, Zhibo Zhao, Zhenghao Huang, Huarui Zhu, Xunbo Lu
In this study, we describe a strategy for benzylic C(sp 3 )–H activation that enables C–S bond formation through a copper-mediated sulfimidation. Leveraging readily available methylarenes under oxidative conditions, the method provides a complementary route to benzylic sulfilimines directly from simple C(sp 3 )–H precursors. It is applicable to a representative range of sulfenamides and methylarenes, amenable to scale-up, and typically delivers benzylic sulfilimines in moderate yields.