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用于正电子发射断层成像的2'-[18F]标记和3'-[18F]标记核苷的放射化学合成。

Radiochemical synthesis of 2'-[18F]-labelled and 3'-[18F]-labelled nucleosides for positron emission tomography imaging.

作者信息

Meyer Jan-Philip, Probst Katrin C, Westwell Andrew D

机构信息

School of Pharmacy and Pharmaceutical Sciences, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3NB, Wales, UK; Wales Research & Diagnostic PET Imaging Centre (PETIC), Institute for Translation, Innovation, Methodology & Engagement (TIME), School of Medicine, Heath Park, Cardiff University, Cardiff, CF14 4XN, Wales, UK.

出版信息

J Labelled Comp Radiopharm. 2014 May 15;57(5):333-7. doi: 10.1002/jlcr.3197. Epub 2014 Apr 1.

Abstract

This review article considers 2'-labelled and 3'-labelled nucleosides, which are of great importance as positron emission tomography (PET) probes in clinical diagnostics and PET research. Although the radiochemical preparation of several [(18)F]-labelled nucleosides such as [(18)F]fluorothymidine or (18)Fcytosine has been accomplished within the last two decades, a number of potentially interesting nucleoside-based biomarkers are not yet available for automated good manufacturing practice production due to the lack of fast and efficient synthetic methods for late-stage [(18)F]-introduction. In order to meet recent demands for new PET-based biomarkers in various clinical applications, appropriate precursors that can easily be fluorinated and deprotected need to be developed.

摘要

这篇综述文章探讨了2'-标记和3'-标记的核苷,它们作为正电子发射断层扫描(PET)探针在临床诊断和PET研究中具有重要意义。尽管在过去二十年中已经完成了几种[(18)F]标记核苷的放射化学制备,如[(18)F]氟代胸苷或[(18)F](氟代阿拉伯呋喃糖基)胞嘧啶,但由于缺乏用于后期[(18)F]引入的快速高效合成方法,许多潜在有趣的基于核苷的生物标志物尚未可用于自动化的良好生产规范生产。为了满足近期各种临床应用中对新型PET基生物标志物的需求,需要开发易于氟化和脱保护的合适前体。

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