Issue 10, 2020

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

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

Supplementary files

Article information

Article type
Research Article
Submitted
05 Jun 2020
Accepted
17 Jul 2020
First published
24 Jul 2020

RSC Med. Chem., 2020,11, 1161-1167

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, 11, 1161 DOI: 10.1039/D0MD00190B

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