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化学进展  2010 

“点击化学”在放射性药物合成中的应用*

, PP. 1591-1602

Keywords: 点击化学,放射性药物,标记化合物,PET成像,SPET成像

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Abstract:

“点击化学”是近几年发展起来的一种新的合成方法,由于其众多的优点而受到广大化学工作者的关注;并在先导化合物库的合成、蛋白质组学、生物偶联技术和生物医药等众多领域得到了飞速的发展。近来,点击化学,特别是Cu+催化的端位炔和叠氮的1,3-偶极[3+2]环加成反应已经应用于放射性药物的领域。本文简要介绍了“点击化学”的概念、特点和反应机理;重点介绍了点击化学合成用于显影的多种放射性示踪剂的进展,“点击化学”在放射性药物的制备、标记化合物的合成、PET成像以及用于PET成像的18F、11C用于SPECT成像的99mTc、188Re、125I、111In等放射性核素等方面的应用;并简要分析了该应用的发展前景。

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