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Syntheses of [11C]2- and [11C]3-trifluoromethyl-4-aminopyridine: potential PET radioligands for demyelinating diseases

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Abstract

Trifluoromethyl groups are of great interest in PET radiopharmaceuticals. Radiolabelled 4-aminopyridine (4AP) derivatives have been proposed for imaging demyelinating diseases. Here, we describe methods for producing 11C-trifluoromethylated derivatives of 4AP and present early imaging results with [11C]3-trifluoromethyl-4AP in a rhesus macaque. This study shows the utility of [11C]CuCF3 for labelling pyridines and provides initial evidence for the potential use of [11C]3-trifluoromethyl-4AP as a PET radioligand.

Graphical abstract: Syntheses of [11C]2- and [11C]3-trifluoromethyl-4-aminopyridine: potential PET radioligands for demyelinating diseases

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Article information


Submitted
05 Jun 2020
Accepted
17 Jul 2020
First published
24 Jul 2020

RSC Med. Chem., 2020, Advance Article
Article type
Research Article

Syntheses of [11C]2- and [11C]3-trifluoromethyl-4-aminopyridine: potential PET radioligands for demyelinating diseases

K. M. Ramos-Torres, Y. Zhou, B. Y. Yang, N. J. Guehl, M. Sung-Hyun, S. Telu, M. D. Normandin, V. W. Pike and P. Brugarolas, RSC Med. Chem., 2020, Advance Article , DOI: 10.1039/D0MD00190B

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