[¹⁸F]β‐CFT is a positron emission tomography (PET) ligand for imaging of dopamine transporter. It was proved to be a sensitive PET marker to detect presynaptic dopaminergic hypofunction in Parkinson's disease. In recent years, copper‐mediated ¹⁸F‐fluorination of aryl boronic esters has been successful in some molecules containing aromatic groups. In this study, we describe the novel synthetic strategy of [¹⁸F]β‐CFT by copper‐mediated nucleophilic radiofluorination with pinacol‐derived aryl boronic esters upon reaction with [¹⁸F]KF/K₂₂₂ and Cu (OTf)₂(py)₄. The radiolabeling protocol was optimized with [¹⁸F]fluoride elution method and amount of copper catalyst used. [¹⁸F]β‐CFT is obtained from boronic ester precursors in 2.2% to 10.6% non‐isolated radiochemical yield (RCY). Purified [¹⁸F]β‐CFT with >99% radiochemical purity (RCP) and high molar activity was obtained in validation runs. The radiolabeling procedure is straightforward and can easily be adapted for clinical use.

中文翻译：

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铜介导的 [18F]β-CFT 亲核放射性氟化用于多巴胺转运蛋白的正电子发射断层扫描成像

[ ¹⁸ F]β-CFT 是一种正电子发射断层扫描 (PET) 配体，用于多巴胺转运蛋白的成像。它被证明是检测帕金森病突触前多巴胺能功能减退的敏感 PET 标志物。近年来，铜介导的芳基硼酸酯的¹⁸ F-氟化在一些含有芳香基团的分子中取得了成功。在这项研究中，我们描述了通过铜介导的亲核放射性氟化与频哪醇衍生的芳基硼酸酯与 [ ¹⁸ F]KF/K ₂₂₂和 Cu (OTf) ₂ ⁽ py ）₄。^{使用 [ 18} ] 优化了放射性标记协议F]氟化物洗脱方法和铜催化剂用量。[ ¹⁸ F]β-CFT 由硼酸酯前体获得，非分离放射化学产率 (RCY) 为 2.2% 至 10.6%。在验证运行中获得了具有 >99% 放射化学纯度 (RCP) 和高摩尔活性的纯化 [ ^{18 F]β-CFT。}放射性标记程序很简单，可以很容易地适应临床使用。