Site-Selective Late-Stage Aromatic [18 F]Fluorination via Aryl Sulfonium Salts

Abstract

Site-selective functionalization of C-H bonds in small complex molecules is a long-standing challenge in organic chemistry. Herein, we report a broadly applicable and site-selective aromatic C-H dibenzothiophenylation reaction. The conceptual advantage of this transformation is further demonstrated through the two-step C-H [¹⁸ F]fluorination of a series of marketed small-molecule drugs.

Keywords: 18F labeling; C−H functionalization; fluorination; late-stage functionalization; radiochemistry.