Chemoselective Radiosyntheses of Electron-Rich [¹⁸F]Fluoroarenes from Aryl(2,4,6-trimethoxyphenyl)iodonium Tosylates

Abstract

Hypervalent diaryliodonium salts have been used to produce various [¹⁸F]fluoroarenes. The iodonium salt approach as a labeling precursor has been established to equally afford complex ¹⁸F-fluorinated molecules. Because of the inherent two aryl ring system connected to a central iodine atom, safeguarding the chemoselectivity during radiofluorination using diaryliodonium salts is important. Herein, we introduce a superior chemoselective radiosynthesis of [¹⁸F]fluoroarenes using an aryl(2,4,6-trimethoxyphenyl)iodonium tosylate as a precursor for ¹⁸F-incorporation, even on electron-rich aryl rings.