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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 a ~ (123) Ⅰ labeled benzothiazole Aβ plaque imaging agent for Alzheimer’s disease, 3’125 125 Ⅰ BTA-0 was synthesized by direct labeling ~ (125) Ⅰ was used to directly label the experimental conditions of BTA-0. The optimal reaction conditions were as follows: reaction time 25 min, pH value 2.5, reaction temperature 60 ℃, 0 solution (containing 50% ethanol), the mass concentration of oxidant H_2O_2 was 0.4 kg / L. Under optimal labeling conditions, the labeling rate of 3’- (125) I-BTA-0 was 72% and the radiochemical purity was more than 95%. The crystal structure of 3’-I-BTA-0 was prepared by electrophilic reaction. The crystal structure of 3’-I-BTA-0 showed that the I atom and the S atom in the labeled molecule were the same.