¹⁸F-Labeled Aryl-Tracers through Direct Introduction of [¹⁸F]fluoride into Electron-Rich Arenes

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.

Cite this article as:

Kovac Mitja, Mavel Sylvie and Anderluh Marko, ¹⁸F-Labeled Aryl-Tracers through Direct Introduction of [¹⁸F]fluoride into Electron-Rich Arenes, Current Organic Chemistry 2013; 17 (23) . https://dx.doi.org/10.2174/13852728113179990022