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

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