Manyi Chen, Zeyi Wang, Zhangjie Zhou, Xinxin Wang, Pengfei Zhang, Jun Xu
Herein, we describe an efficient ortho C-H sulfonylation of 8-aminoquinoline-tethered benzoic acid derivatives using N-sulfonyl-aminophthalimide (NSAPI) as the sulfonylating source. Mechanistic investigations support a radical process, wherein cleavage of the ortho C(sp2)-H bond is rate-determining. The active copper species is regenerated by atmospheric oxygen, allowing for low catalyst loading and broad substrate/functional group tolerance.