点击化学在^(18)F标记PET药物中的应用  

Application of “Click Chemistry” in PET Radiopharmaceuticals Labelled With ^(18)F

作　　者：贾丽娜[1,2] 江大卫[1,2] 孟虎[1,2] 程登峰[3] 周伟[1] 张岚[1] 

机构地区：[1]中国科学院上海应用物理研究所放射化学与工程技术部,上海201800 [2]中国科学院研究生院,北京100049 [3]复旦大学附属中山医院,上海200032

出　　处：《核化学与放射化学》2013年第4期193-210,共18页Journal of Nuclear and Radiochemistry

基　　金：国家自然科学基金资助项目(No.10875163)

摘　　要："点击化学"是一种模块化的合成方法,在生物偶联、药物筛选、材料科学等领域得到了广泛的应用,而其中的Cu(I)催化的叠氮与炔的1,3-偶极环加成(CuAAC)反应,由于其在温和条件下高效快速的反应特点,几乎成了"点击化学"的代名词。它一经引入到PET氟[18F]药物标记中就获得了极大的成功,受到了越来越多的放射性药物工作者的关注。本文重点根据Click合成子的分类综述了点击化学在18 F标记分子探针中的应用,也对近两年应用到18F标记中的环张力促进的点击标记进行了介绍,并简要展望了这些应用的发展前景。＂Click chemistry＂ is a powerful modular synthesis approach that widely applied in bioconjugation chemistry, drug screening and material science. The copper （I） catalyzed cycloaddition between azides and alkynes （CuAAC） to form 1,2, 3-triazoles is the most well-known ＂Click reaction＂ and nearly became synonymous with the concept of ＂Click chemistry＂ because of its high chemoselectivity and perfect regioselectivity under mild reaction and purification conditions. This reaction was introduced into the field of ^18F- radiopharmaceutical preparation and achieved great success which attracted more and more researchers＇ attention. In this review, the application of ＂Click chemistry＂ in the synthesis of ^18F labeled molecular probes was classified based on the click synthons, and the copper- free strain-promoted click （CFC） radiolabeling was also summarized. The prospect of this application was briefly discussed.

关 键 词：点击化学 放射性药物 正电子显像 合成子 18F标记 

分 类 号：O615.4[理学—无机化学]