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Astatine.

作者信息

Meyer Geerd-J

机构信息

Klinik für Nuklearmedizin/Radiopharmazeutische Chemie, Medizinische Hochschule Hannover, Hannover, Germany.

出版信息

J Labelled Comp Radiopharm. 2018 Mar;61(3):154-164. doi: 10.1002/jlcr.3573. Epub 2018 Feb 22.

Abstract

This educational review describes and summarizes the historic discovery of element 85, the experiments leading to its physical and chemical characterization and comparison with its lighter homologue iodine. The half-lives of its longest living isotopes At and At with 8.3 and 7.22 hours respectively together with their alpha decay characteristics made these isotopes interesting for radiation biological research. However, the lack of stable isotopes of astatine presents a strong challenge for all characterizations. Nevertheless, the decay characteristics especially of At stimulated several research groups to develop labelling strategies for the preparation of astatinated radiopharmaceuticals for targeted alpha radiation therapy. Because of the distinct differences in the chemical behaviour of astatine, when compared with iodine, these approaches are quite challenging. Accordingly, quite different labelling strategies have been tested, namely nucleophilic and electrophilic substitution reactions as well as complex forming strategies. Classic and new developments for the preparation of these compounds are reviewed.

摘要

这篇教育综述描述并总结了85号元素的历史性发现、对其进行物理和化学表征的实验,以及与较轻的同系物碘的比较。其最长寿同位素砹-211和砹-210的半衰期分别为8.3小时和7.22小时,连同它们的α衰变特性,使得这些同位素在放射生物学研究中很有趣。然而,砹缺乏稳定同位素给所有表征带来了巨大挑战。尽管如此,特别是砹-211的衰变特性促使几个研究小组开发标记策略,以制备用于靶向α放射治疗的砹化放射性药物。由于与碘相比,砹的化学行为存在明显差异,这些方法颇具挑战性。因此,已经测试了相当不同的标记策略,即亲核和亲电取代反应以及络合形成策略。本文综述了制备这些化合物的经典方法和新进展。

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