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

Author(s): Mitja Kovac, Sylvie Mavel, Marko Anderluh

Journal Name: Current Organic Chemistry

Volume 17 , Issue 23 , 2013

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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.

Keywords: Aromatic fluorination, Arylfluoride, Balz-Schiemann reaction, Diaryliodonium salts, 18F-labeled molecules, PET, Triazene.

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Article Details

Year: 2013
Page: [2921 - 2935]
Pages: 15
DOI: 10.2174/13852728113179990022
Price: $58

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