Abstract

Taking advantage of facilely available α-chloroketones as C(sp3)-based electrophilic partners and oxidized alkyne equivalents, we here present a novel CpxRh(III)-catalyzed enantioselective C–H [4 ​+ ​2] annulation of sulfoximines under mild and redox-neutral conditions to access S-chiral 1,2-benzothiazines. It represents the first example of such C(sp3)-electrophiles enabling enantioselective C–H functionalization.

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