Issue 20, 2017

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

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

Supplementary files

Article information

Article type
Paper
Submitted
14 Mar 2017
Accepted
25 Apr 2017
First published
25 Apr 2017

Org. Biomol. Chem., 2017,15, 4351-4358

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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