Bis(4-benzyloxyphenyl)iodonium salts as effective precursors for the no-carrier-added radiosynthesis of 4-[¹⁸F]fluorophenol

Appl Radiat Isot. 2013 Dec:82:264-7. doi: 10.1016/j.apradiso.2013.08.011. Epub 2013 Sep 5.

Abstract

4-[¹⁸F]Fluorophenol is a very useful intermediate compound for building-up more complex molecules bearing a 4-[¹⁸F]fluorophenoxy moiety. Bis(4-benzyloxyphenyl)iodonium salts proved very effective as labeling precursors for the radiosynthesis of this compound in no-carrier-added form. Starting from the bromide salt and performing the radiofluorination by conventional heating, 4-[¹⁸F]fluorophenol was obtained in an overall RCY of 43 ± 12% while a yield of 52 ± 3% was achieved more reliably starting from the tosylate salt and employing microwave heating.

Keywords: 4-[(18)F]fluorophenol; Diaryliodonium salt; Fluorine-18; Microwave heating; Radiofluorination.