Victor Pike and colleagues from the National Institute of Mental Health in Bethesda (Maryland, USA) have devised novel and efficient methods to readily access 18F-labelled mGluR5 PET radioligands that are useful for molecular imaging with positron emission tomography (PET).
While iodonium based compounds are considered promising for the preparation of PET radiotracers, very few examples of applications have been realised so far. Now, Pike and colleagues have designed appropriate diaryliodonium tosylates as precursors for introducing fluorine-18 into simple arenes to radiosynthesise standard PET radiotracers. These would otherwise be poorly accessible via traditional aromatic nucleophilic substitution reactions with the [18F]fluoride ion, due to the weak activation of the aryl ring.
The referees and the OBC Editorial office very much enjoyed this excellent paper, and we hope you will too! Read it for FREE for the next 4 weeks.
Syntheses of mGluR5 PET radioligands through the radiofluorination of diaryliodonium tosylates
Sanjay Telu, Joong-Hyun Chun, Fabrice G. Siméon, Shuiyu Lu and Victor W. Pike
Org. Biomol. Chem., 2011, Advance Article
DOI: 10.1039/C1OB05555K, Paper
