Chemoselective Radiosyntheses of Electron-Rich [18F]Fluoroarenes from Aryl(2,4,6-trimethoxyphenyl)iodonium Tosylates
Chemoselective Radiosyntheses of Electron-Rich [18F]Fluoroarenes from Aryl(2,4,6-trimethoxyphenyl)iodonium Tosylates
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DOI：
10.1021/acs.joc.9b00019
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发表时间：
2019-03-15
影响因子：
3.6
通讯作者：
Chun, Joong-Hyun
中科院分区：
文献类型：
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作者：
Kwon, Young-Do;Son, Jeongmin;Chun, Joong-Hyun
高价二芳基碘鎓盐已用于生产各种[F-18]氟代芳烃。碘鎓盐作为标记前体的方法已经建立，以同样提供复杂的F-18-氟化分子。由于固有的两个芳基环系统连接到一个中心的碘原子，在使用二芳基碘鎓盐的放射性显影过程中，保护化学选择性是重要的。在此，我们介绍了一个上级化学选择性放射合成[F-18]氟芳烃使用芳基（2，4，6-三甲氧基苯基）碘鎓甲苯磺酸盐作为前体的F-18-掺入，即使在富电子的芳基环。
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.