Catalyst-Free Aromatic Radiofluorination via Oxidized lodoarene Precursors

Oxidized iodoarenes (OlAs), prepared via mCPBA-mediated oxidation, have been demonstrated as versatile precursors for the synthesis of [F-18]fluoroarenes in the absence of catalysts. OIAs have been identified as intermediates in single-pot syntheses of iodonium salts and ylides but have never been recognized as radiofluorination precursors. Here, the isolated OlAs were used without any catalysts to produce functionalized [F-18]fluoroarenes, regardless of the electronic nature of the arenes. This method was also applied to the production of radiolabeling synthons for use as aromatic F-18-labeled building blocks.