Study on radiolabeling of 1,2,3-triazole analogs with fac-[^(188)Re(CO)_3 (H_2O)_3 ]^+ via click chemistry  

作　　者：WANG Cheng YIN Jilin ZHOU Wei ZHANG Lan ZHOU Zheng 

机构地区：[1]PET/CT center,General Hospital of Guangzhou Military Command [2]Shanghai Institute of Applied Physics,Chinese Academy of Sciences,Jiading Campus

出　　处：《Nuclear Science and Techniques》2013年第3期27-30,共4页核技术（英文）

基　　金：Supported by National Natural Science Foundation of China(No.10875163);Natural Science Foundation of Guangdong Province(Nos.2009B030108036 and S2012010010685)

摘　　要：Click chemistry was used to study on radiolabeling of 1,2,3-triazole analogs with fac-[188 Re(CO) 3 (H 2 O) 3]+ . CuSO 4 /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-[188 Re(CO) 3 (H 2 O) 3]+ was coordinated to the six triazoles. The results showed that the radiochemical yields (RCY) of the conjugation of fac-[188 Re(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 188 Re-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.Abstract Click chemistry was used to study on radiolabeling of 1,2,3-triazole analogs withfac-[188Re（CO）3（H20）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 preparedfac-[^188 Re（CO）3（H2O）3]^＋ was coordinated to the six triazoles. The results showed that the radiochemical yields （RCY） of the conjugation offac-[^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.

关 键 词：化学研究 三唑类 类似物 CO 生物活性评价 生物活性分子 化学产率 催化剂体系 

分 类 号：O626[理学—有机化学] R312[理学—化学]