Transition-metal-free arene C-H functionalization for the synthesis of sulfoximines
Wenbo Zhang1, XinYu Li1, Yanchuan Zhao2
1State Key Laboratory of Chemo and Biosensing, College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China. gaobing@hnu.edu.cn.
Abstract:
A transition-metal-free C-H functionalization method has been developed for the synthesis of aryl sulfoximines. This two-step protocol involves the 3,5-dimethyl-4-isoxazolyliodonium salt as an intermediate. The iodonium salt is obtained with high site selectivity from arenes via C-H activation, and is then converted into sulfoximines through a ligand coupling at the hypervalent iodine center with sulfinamides. The process is mild and does not require transition metals, enabling the late-stage incorporation of chiral sulfonimidoyl groups into drug candidates.
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