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Nucleophilic Synthesis of 6-l-[18F]FDOPA. Is Copper-Mediated Radiofluorination the Answer?
Molecules ( IF 4.6 ) Pub Date : 2020-09-23 , DOI: 10.3390/molecules25194365
Raisa N. Krasikova

Positron emission tomography employing 6-l-[18F]fluoro-3,4-dihydroxyphenylalanine (6-l-[18F]FDOPA) is currently a highly relevant clinical tool for detection of gliomas, neuroendocrine tumors and evaluation of Parkinson’s disease progression. Yet, the deficiencies of electrophilic synthesis of 6-l-[18F]FDOPA hold back its wider use. To fulfill growing clinical demands for this radiotracer, novel synthetic strategies via direct nucleophilic 18F-radiloabeling starting from multi-Curie amounts of [18F]fluoride, have been recently introduced. In particular, Cu-mediated radiofluorination of arylpinacol boronates and arylstannanes show significant promise for introduction into clinical practice. In this short review these current developments will be discussed with a focus on their applicability to automation.

中文翻译:

6-l-[18F]FDOPA 的亲核合成。铜介导的放射性氟化是答案吗?

采用 6-l-[18F] 氟-3,4-二羟基苯丙氨酸 (6-l-[18F]FDOPA) 的正电子发射断层扫描目前是一种高度相关的临床工具,用于检测神经胶质瘤、神经内分泌肿瘤和评估帕金森病的进展。然而,6-l-[18F]FDOPA 亲电合成的缺陷阻碍了其更广泛的应用。为了满足对这种放射性示踪剂日益增长的临床需求,最近引入了通过直接亲核 18F 放射性标记从多居里量的 [18F] 氟化物开始的新型合成策略。特别是,Cu 介导的芳基频哪醇硼酸酯和芳基锡烷的放射性氟化显示出引入临床实践的重要前景。在这篇简短的评论中,将讨论这些当前的发展,重点是它们对自动化的适用性。
更新日期:2020-09-23
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