同位素2011，Vol.24Issue(4)：205-211,7.
新型骨显像剂99Tcm-BIPrDP的制备及其反应动力学研究
Preparation and Reaction Kinetics of a New Bone Imaging Agent 99Tcm-BIPrDP
摘要
Abstract
A new diphosphonic acid ligand, 1-hydroxy 3-(2-butyl-lH-imidazol-l-yl)propane-1,1-diyldiphosphonic acid (BIPrDP)? Was prepared from the starting material 2-butyl-lH-imidazole by three steps of reactions: N-alkylation, ester hydrolysis and phosphoric acid ac-ylation. The structures of the intermediate and target compounds were identified by elemental analysis, MS and 'H-NMR. BIPrDP was directly labeled by Na9'Tcm04 in the presence of the reducing agent SnCl2 to afford a new bone imaging agent "Tcm-BIPrDP. The kinetics of the labeling reaction between BIBrDP and "TcmO4~ was also studied. The reaction rate constants, k, were determined to be 0. 018 3, 0.020 7, 0.024 1, 0.027 0, 0.028 8, 0.031 9 at 40..50,60,70,80 and 90 °C , respectively. The correlation between the reaction rate constant k and temperature Twasln￡= - 1 267. IX (1/D+0. 055<V=0. 990 2). The reaction activation energy, E,, was found to be 10. 53 kj ? Mol"1, much lower than the activation energy of general chemical reactions (typically 20~ 150 kj ? Mol"1) , which was consistent with the observation that the preparation of "Tc^-BIPrDP took place rapidly. In addition, based on the data of the radiolabeling yield (RLY) at different temperatures, a correlation between the RLY and temperature was developed as ln[RLY/(l -RLY)] = -6 218. 4/T+ 19. 84. This correlation suggests that, in order to achieve radiolabeling yields of higher than 90%, the reaction temperature should be higher than 79. 31 °C.关键词
99Tcm-BIPrDP/骨显像剂/反应动力学Key words
"Tcm-BIPrDP/ bone imaging agent/ reaction kinetics分类
医药卫生引用本文复制引用
张姝,罗世能,邱玲,林建国,夏咏梅..新型骨显像剂99Tcm-BIPrDP的制备及其反应动力学研究[J].同位素,2011,24(4):205-211,7.基金项目
国家自然科学基金资助项目(20801024) （20801024）
江苏省自然科学基金资助项目(BK2009077) （BK2009077）
江苏省卫生厅科研项目(H200963) （H200963）
