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Issue 20, 2017
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18F-Labelling of electron rich iodonium ylides: application to the radiosynthesis of potential 5-HT2A receptor PET ligands

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Abstract

18F-Labelling of aromatic moieties was limited to electron deficient aromatic systems for many years but recent developments have provided access to the direct labelling of electron rich aromatic systems. Herein we report the synthesis and 18F-labelling of iodonium ylide precursors in the pursuit of 18F-labelled 5-HT2A receptor agonist PET-ligands. Subsequent evaluation in pigs showed high brain uptake of the PET ligands but a blocking dose of ketanserin did not significantly reduce the signal in relevant brain regions – indicating that the ligands do not interact specifically with the 5-HT2A receptor in vivo.

Graphical abstract: 18F-Labelling of electron rich iodonium ylides: application to the radiosynthesis of potential 5-HT2A receptor PET ligands

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Publication details

The article was received on 14 Mar 2017, accepted on 25 Apr 2017 and first published on 25 Apr 2017


Article type: Paper
DOI: 10.1039/C7OB00628D
Citation: Org. Biomol. Chem., 2017,15, 4351-4358
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    18F-Labelling of electron rich iodonium ylides: application to the radiosynthesis of potential 5-HT2A receptor PET ligands

    I. N. Petersen, J. Villadsen, H. D. Hansen, J. Madsen, A. A. Jensen, N. Gillings, S. Lehel, M. M. Herth, G. M. Knudsen and J. L. Kristensen, Org. Biomol. Chem., 2017, 15, 4351
    DOI: 10.1039/C7OB00628D

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