3′-^(125)Ⅰ-BTA-0的直接标记法及其晶体结构  

Direct Label Method and Crystal Structure of 3′-^(125)I-BTA-0

作　　者：王武尚[1,2] 刘伯里[2] 高敏[3] 

机构地区：[1]西北核技术研究所,陕西西安710024 [2]北京师范大学化学学院,北京100875 [3]西安交通大学理学院应用化学系,陕西西安710049

出　　处：《核化学与放射化学》2007年第4期238-243,共6页Journal of Nuclear and Radiochemistry

基　　金：国家自然科学基金资助项目(30640042)

摘　　要：为了研制^(123)Ⅰ标记的、诊断阿尔茨海默病的苯并噻唑类Aβ斑块显像剂,采用直接标记法合成了3′-^(125)Ⅰ-BTA-0,并探索了^(125)Ⅰ直接标记BTA-0的实验条件,最佳条件为:反应时间25 min,pH值约为2.5,反应温度约为60℃,配体最佳用量为0.1 mL 0.6 g/LBTA-0溶液(含50%乙醇),氧化剂H_2O_2的质量浓度为0.4 kg/L。在最佳标记条件下,3′-^(125)I-BTA-0的标记率为72%,放射化学纯度大于95%。通过亲电反应制备了3′-I-BTA-0的单晶,晶体结构测定结果表明,标记物分子中I原子与S原子同侧。In order to develop ^123I-labeled benzothiazole derivatives as imaging agents for Aβ plaques in the brain with Alzheimer＇s disease, 3＇-^125I-BTA-0 was synthesized with direct labeling method. The experimental condition of directly labeling BTA-0 with ^125I was studied. The optimum condition is obtained： labeling reaction lasts for 25 min at 60 ℃ and pH≈2.5, the volume of 0.6 g/L BTA-0 is 0.1 mL, and the mass concentration of H2O2 is about 0.4 kg/L. Under the optimum condition, the labeling yield of 3’-^125I-BTA-0 is 72%, and its radiochemical purity is more than 95%. The single crystal of 3＇-I-BTA-0 was prepared via electrophilic reaction. The crystal structure of 3＇-I-BTA-0 was determined. The result indicates that I atom and S atom are on the same side in the molecule.

关 键 词：阿尔茨海默病 ^125I Aβ斑块 晶体结构 

分 类 号：O614.712[理学—无机化学]