Joseph C. Walsh1, Hartmuth C. Kolb1
1Siemens Molecular Imaging Biomarker Research, 6100 Bristol Parkway, Culver City, CA 90230, USA
Tóm tắt
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.
