Department of Radiology & Nuclear Medicine, VU University Medical Center, Amsterdam, De Boelelaan 1085c, 1081 HV Amsterdam, The Netherlands.
Chem Soc Rev. 2017 Jul 31;46(15):4709-4773. doi: 10.1039/c6cs00492j.
Positron emission tomography (PET) is an important driver for present day healthcare. Fluorine-18 is the most widely used radioisotope for PET imaging and a thorough overview of the available radiochemistry methodology is a prerequisite for selection of a synthetic approach for new fluorine-18 labelled PET tracers. These PET tracers can be synthesised either by late-stage radiofluorination, introducing fluorine-18 in the last step of the synthesis, or by a building block approach (also called modular build-up approach), introducing fluorine-18 in a fast and efficient manner in a building block, which is reacted further in one or multiple reaction steps to form the PET tracer. This review presents a comprehensive overview of the synthesis and application of fluorine-18 labelled building blocks since 2010.
正电子发射断层扫描(PET)是当今医疗保健的重要推动因素。氟-18 是用于 PET 成像的最广泛使用的放射性同位素,对可用的放射化学方法进行全面概述是选择新的氟-18 标记的 PET 示踪剂合成方法的前提。这些 PET 示踪剂可以通过晚期放射性氟化来合成,即在合成的最后一步引入氟-18,也可以通过砌块方法(也称为模块构建方法)来合成,在砌块中快速有效地引入氟-18,然后在一个或多个反应步骤中进一步反应以形成 PET 示踪剂。本文综述了自 2010 年以来氟-18 标记砌块的合成和应用。