氘氚标记治疗老年性痴呆症药物zt-1

Preparation of Labelled zt-1 With Tritium and Deuterium

用钠硼氘、钠硼氚还原5-氯-邻香草醛制备氘标记、氘标记5-氯-邻香草醛,然后与石杉碱甲在避光条件 下缩合生成氘标记、氚标记zt-1。经硅胶板层析所得Rf与zt-1标准品的一致,经紫外检测其λmax=303nm也 与标准品的一致。氚标记zt-1的放化纯度>95％,放射性比活度为401.3GBq/g。

zt-1 is a petential drug for treatment of Alzheimer's disease. For the study of this drug, isotope labeled compounds should be prepared. After reduction of 5-chloro-o-vanillin with sodium boron deuteride and triterid, and condensation, zt-1 labeled with tritium and deuterium are prepared. UV absorption spectrum and Rf of tritium labeled zt-1 are the same as authentic sample. The radiochemical purity of 3H-zt-l is more than 95%, and the specific radioactivity is 401. 3 GBq/g.