4.7 Article

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

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JOURNAL OF ORGANIC CHEMISTRY
卷 84, 期 6, 页码 3678-3686

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AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.9b00019

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  1. National Research Foundation of Korea [NRF2015R1D1A1A02061420]
  2. Yonsei University College of Medicine [6-2018-0100]

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Hypervalent diaryliodonium salts have been used to produce various [F-18]fluoroarenes. The iodonium salt approach as a labeling precursor has been established to equally afford complex F-18-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 [F-18]fluoroarenes using an aryl(2,4,6-trimethoxyphenyl)iodonium tosylate as a precursor for F-18-incorporation, even on electron-rich aryl rings.

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