Selective S-arylation of Sulfenamides with Arynes: Facile Access to Sul-filimines

Sulfilimines, the aza-analogues of sulfoxides, are of increasing interests in medicinal and agrochemical research programs. However, the development of efficient routes for their synthesis remains relatively unexplored. In this study, we report a transition metal-free, selective S-arylation reaction between sulfenamides and arynes, enabling the facile preparation of structurally diverse sulfilimines under mild and redox-neutral condition in good yields. The application value of our method was further demonstrated by scale-up synthesis, downstream derivatization, and robustness screen.