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
Gordon Center for Medical Imaging , Department of Radiology , Massachusetts General Hospital and Harvard Medical School , Boston , MA , USA . Email:
Molecular Imaging Branch , National Institute of Mental Health , National Institutes of Health , Bethesda , MD , USA . Email:
RSC Med Chem. 2020 Jul 24;11(10):1161-1167. doi: 10.1039/d0md00190b. eCollection 2020 Oct 1.
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 C-trifluoromethylated derivatives of 4AP and present early imaging results with [C]3-trifluoromethyl-4AP in a rhesus macaque. This study shows the utility of [C]CuCF for labelling pyridines and provides initial evidence for the potential use of [C]3-trifluoromethyl-4AP as a PET radioligand.
三氟甲基基团在正电子发射断层扫描（PET）放射性药物中备受关注。放射性标记的4-氨基吡啶（4AP）衍生物已被提议用于脱髓鞘疾病的成像。在此，我们描述了制备4AP的碳-三氟甲基化衍生物的方法，并展示了在恒河猴中使用[碳]3-三氟甲基-4AP的早期成像结果。这项研究表明了[碳]CuCF用于标记吡啶的效用，并为[碳]3-三氟甲基-4AP作为PET放射性配体的潜在用途提供了初步证据。
