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

lick chemistry was used to study on radiolabeling of 1,2,3-triazole analogs with fac-[188Re(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-[188Re(CO)3(H2O)3]+ was coordinated to the six triazoles. The results showed that the radiochemical yields (RCY) of the conjugation of fac-[188Re(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 188Re-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.