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

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Syntheses of [11C]2- and [11C]3-trifluoromethyl-4-aminopyridine: potential PET radioligands for demyelinating diseases
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2020-07-24 , DOI: 10.1039/d0md00190b
Karla M Ramos-Torres ₁ , Yu-Peng Zhou ₁ , Bo Yeun Yang ₂ , Nicolas J Guehl ₁ , Moon Sung-Hyun ₁ , Sanjay Telu ₂ , Marc D Normandin ₁ , Victor W Pike ₂ , Pedro Brugarolas ₁

Affiliation

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.

中文翻译：

[11C]2- 和 [11C]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

三氟甲基在 PET 放射性药物中受到极大关注。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。在这里，我们描述了生产¹¹ C-三氟甲基化 4AP 衍生物的方法，并展示了恒河猴中 [ ¹¹ C]3-三氟甲基-4AP 的早期成像结果。本研究展示了 [ ¹¹ C]CuCF ₃用于标记吡啶的效用，并为 [ ¹¹ C]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。

更新日期：2020-08-06

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