Applications of Click Chemistry in Radiopharmaceutical Development
Applications of Click Chemistry in Radiopharmaceutical Development
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DOI：
10.2533/chimia.2010.29
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发表时间：
2010-01-01
期刊：
影响因子：
1.2
通讯作者：
Kolb, Hartmuth C.
中科院分区：
文献类型：
--
作者：
Walsh, Joseph C.;Kolb, Hartmuth C.
点击化学是一种只采用实用和可靠的化合物合成转化的概念，在化学的几个领域产生了重大影响，包括材料科学和药物发现。本文介绍了使用点击化学放射性药物的发展。靶模板化原位点击化学用于铅生成。发现1，2，3-三唑部分改善某些放射性药物的药代动力学性质。可靠的Cu（I）催化的点击反应用于肽化合物的放射性标记而不需要保护基团。总之，用于发现、优化和标记新的放射性示踪剂的点击化学方法代表了用于放射性药物开发的非常强大的工具。
Click chemistry, a concept that employs only practical and reliable transformations for compound synthesis, has made a significant impact in several areas of chemistry, including material sciences and drug discovery. The present article describes the use of click chemistry for the development of radiopharmaceuticals. Target templated in situ click chemistry was used for lead generation. The 1,2,3-triazole moiety was found to improve the pharmacokinetic properties of certain radiopharmaceuticals. The reliable Cu(I)-catalyzed click reaction was employed for radiolabeling of peptidic compounds without the need for protecting groups. In summary, the click chemistry approach for the discovery, optimization and labeling of new radiotracers, represents a very powerful tool for radiopharmaceutical development.