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

摘要: Click 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.