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

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 11 C-trifluoromethylated derivatives of 4AP and present early imaging results with...

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Published inMedChemComm Vol. 11; no. 1; pp. 1161 - 1167
Main Authors Ramos-Torres, Karla M, Zhou, Yu-Peng, Yang, Bo Yeun, Guehl, Nicolas J, Sung-Hyun, Moon, Telu, Sanjay, Normandin, Marc D, Pike, Victor W, Brugarolas, Pedro
Format Journal Article
LanguageEnglish
Published England Royal Society of Chemistry 01.10.2020
Subjects
Chemistry
Demyelinating diseases
Demyelination
Derivatives
High-performance liquid chromatography
Labeling
Positron emission
Production methods
Pyridines
Radioisotopes
Tomography
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Summary: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 11 C-trifluoromethylated derivatives of 4AP and present early imaging results with [ 11 C]3-trifluoromethyl-4AP in a rhesus macaque. This study shows the utility of [ 11 C]CuCF 3 for labelling pyridines and provides initial evidence for the potential use of [ 11 C]3-trifluoromethyl-4AP as a PET radioligand. [ 11 C]fluoroform was used to produce 11 C-trifluoromethylated derivatives of 4-aminopyridine with high molar activity for PET imaging of the brain.
Bibliography:Electronic supplementary information (ESI) available: Full experimental methods and HPLC chromatograms for all reactions. See DOI
10.1039/d0md00190b
ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 14
ISSN:2632-8682
2040-2503
2632-8682
2040-2511
DOI:10.1039/d0md00190b