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

[(11)C]2-和[(11)C]3-三氟甲基-4-氨基吡啶的合成:用于脱髓鞘疾病的潜在PET放射性配体

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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 (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.

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