Direct one step dehydrogenative C-H sulfonimidation of unfunctionalized arenes: A conveneient protocol to emerging medicinal chemistry motifs without prefunctionalized arenes

[Display omitted] •Sulfonimidamides and sulfoximines are emerging medicinal chemistry motifs.•Direct one step sulfonimidation of unfunctionalized arenes in a dehydrogenative C-H activation manner is achieved.•A simple protocol to access sulfonimidate esters and sulfonimidamides is demonstrated. Recently new sulfur moieties such as sulfonimidamides are emerging as indispensable bioisosters in medicinal chemistry and agrochemistry programs due to their important biological and physiological properties. But, most available synthetic protocols start from thiol derivatives or from their precursor halides via multi-step procedures. Also, all these protocols involve harsh oxidation conditions. This is a big discouraging factor for medicinal chemists to explore these high medicinal value motifs in drug discovery programs. We herein report a facile synthesis of sulfonimidates and sulfonimidamides by direct sulfonimidation of unfinctional arenes [direct C-H activation to C-S(=O)(=NH) functionalization], thus providing a convenient protocol to incorporate emerging high medicinal value moieties in drug discovery programs. We further demonstrated the applications of tBuON-sulfonimidate esters as useful synthons in synthesis of sulfonimidamides.