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 

作者机构：PET/CT centerGeneral Hospital of Guangzhou Military Command Shanghai Institute of Applied PhysicsChinese Academy of SciencesJiading Campus 

出 版 物：《Nuclear Science and Techniques》 (核技术（英文）)

年 卷 期：2013年第24卷第3期

页      面：27-30页

核心收录：

学科分类：081704[工学-应用化学] 1001[医学-基础医学(可授医学、理学学位)] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学] 10[医学] 

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

主　　题：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 

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.