Walsh Joseph C, Kolb Hartmuth C
Siemens Molecular Imaging Biomarker Research, 6100 Bristol Parkway, Culver City, CA 90230, USA.
Chimia (Aarau). 2010;64(1-2):29-33. doi: 10.2533/chimia.2010.29.
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.
点击化学是一种仅采用实用且可靠的转化方法进行化合物合成的概念，它在化学的多个领域，包括材料科学和药物发现中都产生了重大影响。本文描述了点击化学在放射性药物开发中的应用。目标导向的原位点击化学被用于先导化合物的生成。人们发现1,2,3 - 三唑部分可改善某些放射性药物的药代动力学性质。可靠的铜（I）催化点击反应被用于肽类化合物的放射性标记，而无需保护基团。总之，点击化学方法用于新放射性示踪剂的发现、优化和标记，是放射性药物开发的一种非常强大的工具。
