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

A novel ¹⁸F labeling strategy was developed to directly construct aryl-SO₂-¹⁸F from arenediazonium tosylates with a SO₂ source and [¹⁸F]fluoride. This approach is compatible with a wide range of substrates and enabled the production of ¹⁸F-labeled drug-like derivatives through late-stage ¹⁸F fluorination, representing a significant advance in the radiosynthesis of ¹⁸F-labeled arenesulfonyl fluorides. A reactive ¹⁸F labeling synthon, bearing a maleimide-based prosthetic group, allowed for the generation of ¹⁸F-labeled temperature-sensitive biomolecules containing cysteine residues via maleimide-cysteine chemistry.