Applications of click chemistry in radiopharmaceutical development.
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.
Siemens Molecular Imaging Biomarker Research, 6100 Bristol Parkway, Culver City, CA 90230, USA.
Joseph C
JC
Walsh
Hartmuth C
HC
Kolb
D000818:Animals; D035843:Biomedical Research / Q000379:methods*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D055808:Drug Discovery / Q000379:methods*; D051379:Mice; D015394:Molecular Structure; D009374:Neoplasms, Experimental / Q000000981:diagnostic imaging / Q000378:metabolism; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D014018:Tissue Distribution
D019275:Radiopharmaceuticals