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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.

SUBMITTER: Ramos-Torres KM

PROVIDER: S-EPMC7651860 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature

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

Ramos-Torres Karla M KM Zhou Yu-Peng YP Yang Bo Yeun BY Guehl Nicolas J NJ Sung-Hyun Moon M Telu Sanjay S Normandin Marc D MD Pike Victor W VW Brugarolas Pedro P

RSC medicinal chemistry 20200724 10

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 pote ...[more]

PMID: 33479620

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