Radiosynthesis of 18 F-Labeled Arenesulfonyl Fluorides through Two-Bond Construction with [ 18 F]Fluoride.

A novel 18 F labeling strategy was developed to directly construct aryl-SO 2 - 18 F from arenediazonium tosylates with a SO 2 source and [ 18 F]fluoride. This approach is compatible with a wide range of substrates and enabled the production of 18 F-labeled drug-like derivatives through late-stage 18 F fluorination, representing a significant advance in the radiosynthesis of 18 F-labeled arenesulfonyl fluorides. A reactive 18 F labeling synthon, bearing a maleimide-based prosthetic group, allowed for the generation of 18 F-labeled temperature-sensitive biomolecules containing cysteine residues via maleimide-cysteine chemistry.