“点击化学”在放射性药物合成中的应用

Application of "Click Chemistry" in Synthesis of Radiopharmaceuticals

"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多种用于显影的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99m Tc、188Re、125I、111 In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。

＂Click chemistry＂is a new synthetic method which has being developed in recent years.Due to its numerous advantages,its applications have been paid close attentions and developed rapidly including the synthesis of lead compound database,proteome,bioconjugate technology and biomedicine.Recently,click chemistry,and in particular the Cu ＋-mediated 1,3-dipolar [3 ＋ 2]cycloaddition between azides and alkynes,has also entered the field of radiopharmaceutical science.In this paper,the conception,characteristics and reaction mechanisms of ＂click chemistry＂are reviewed.Particularly,the recent developments of click chemistry applied in synthesizing various radiotracers,radiopharmaceuticals,labelled compounds and PET imaging are addressed.The radionuclides include 18F and 11C used for PET imaging and 99mTc,188Re,125I,111In for SPECT imaging.The prospects of this application in radiopharmaceutical science are analyzed.