Title:18F-Labeled Aryl-Tracers through Direct Introduction of [18F]fluoride into Electron-Rich Arenes
Volume: 17
Issue: 23
Author(s): Mitja Kovac, Sylvie Mavel and Marko Anderluh
Affiliation:
Keywords:
Aromatic fluorination, Arylfluoride, Balz-Schiemann reaction, Diaryliodonium salts, 18F-labeled molecules, PET, Triazene.
Abstract: Rapid and efficient methods using no-carried-added [18F]fluoride as the source of fluorine-18 for nucleophilic aromatic fluorination
play an important role in the development of new radiopharmaceuticals for positron emission tomography (PET). Molecules that
bear electron-rich aromatic moieties are especially difficult to label by direct single-step nucleophilic no-carrier-added radiofluorination.
Classical Balz-Schiemann reaction with its modifications, Wallach reaction and diaryliodonium salts methodology are a few methods to
enable this. The present review provides a critical overview of these chemical methods with the emphasis on diaryliodonium salt as precursors
for the direct introduction of [18F]fluoride into electron-rich arenes in synthesis of 18F-labeled molecules for PET scanning.