Syntheses of [11C]2- and [11C]3-trifluoromethyl-4-aminopyridine: potential PET radioligands for demyelinating diseases. Issue 10 (6th August 2020)

• Record Type: Journal Article
• 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
• Is Part Of: RSC medicinal chemistry. Volume 11:Issue 10(2020)
• Page Start: 1161
• Page End: 1167
• Publication Date: 2020-08-06
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1039/d0md00190b
• Languages: English
• ISSNs: 2632-8682

Abstract

Abstract : [ 11 C]fluoroform was used to produce 11 C-trifluoromethylated derivatives of 4-aminopyridine with high molar activity for PET imaging of the brain. 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 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]CuCF3 for labelling pyridines and provides initial evidence for the potential use of [ 11 C]3-trifluoromethyl-4AP as a PET radioligand.