Application of "Click Chemistry" in Synthesis of Radiopharmaceuticals

"Click chemistry" is a new synthetic method which has being developed in recent years. Due to its numerous advantages, its applications have been paid close attentions and developed rapidly including the synthesis of lead compound database, proteome, bioconjugate technology and biomedicine. Recently, click chemistry, and in particular the Cu+-mediated 1, 3-dipolar [3 + 2] cycloaddition between azides and alkynes, has also entered the field of radiopharmaceutical science. In this paper, the conception, characteristics and reaction mechanisms of "click chemistry" are reviewed. Particularly, the recent developments of click chemistry applied in synthesizing various radiotracers, radiopharmaceuticals, labelled compounds and PET imaging are addressed. The radionuclides include F-18 and C-11 used for PET imaging and Tc-99m, Re-188, I-125, In-111 for SPECT imaging. The prospects of this application in radiopharmaceutical science are analyzed.