Study on radiolabeling of 1,2,3-triazole analogs with fac-[Re-188(CO)(3)(H2O)(3)](+) via click chemistry

Abstract

Click chemistry was used to study on radiolabeling of 1,2,3-triazole analogs with fac-[Re-188(CO)(3)(H2O)(3)](+). CuSO4/L-sodium ascorbate was chosen as the catalyst system, three terminal alkynes were conjugated with two different azides respectively, and then the new prepared fac-[Re-188(CO)(3)(H2O)(3)](+) was coordinated to the six triazoles. The results showed that the radiochemical yields (RCY) of the conjugation of fac-[Re-188(CO)(3)](+) with six triazoles were over 90%, and the triazoles showed high stability in phosphate-buffered saline and new-born calf serum. The preliminary biological evaluation results showed that the new Re-188-labeling method via click chemistry could have general application in labeling bioactive molecules in high radiochemical yield and high specific activity for further SPECT research.