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“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 synthesis method developed in recent years. Due to its many merits, it has attracted the attention of the majority of chemists and has been widely used in the synthesis, proteomics and bioconjugation of lead compound libraries And biomedicine and other fields have been rapid development. Recently click chemistry, especially Cu + catalyzed 1,3-dipolar [3 + 2] cycloaddition of terminal alkyne and azide, has been used in the field of radiopharmaceuticals. This article briefly introduced the concept, characteristics and reaction mechanism of click chemistry, highlighting the advances in click chemistry for the synthesis of various radiotracers for development, the preparation of the “click chemistry” for radiopharmaceuticals, the labeling Compound synthesis, PET imaging and 18F, 11C SPECT imaging 99m Tc, 188Re, 125I, 111 In and other radionuclides applications for PET imaging; and briefly analyzed the prospects for the development of the application.