^3H标记噻喏啡的合成  

Synthesis of 3H-thienorphine

作　　者：王竞艳[1] 陈兰福[1] 吴波[1] 仲伯华[1] 吴久伟 廖沙 沈德存 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850 [2]中国原子能科学院同位素研究所,北京102413

出　　处：《中国新药杂志》2004年第11期1012-1015,共4页Chinese Journal of New Drugs

摘　　要：目的:合成镇痛戒毒新药噻喏啡的3H标记化合物,以进行药动学研究。方法:以蒂巴因为原料,经过7步反应制得3H标记噻喏啡的前体--澳代噻喏啡,然后与3H2进行氚-卤交换反应,产物经制备薄板层析分离后得到定位标记的3H标记噻喏啡纯品。结果:产品总放射性活度为35mCi,放射比活度为18Ci·mmol-1,放化纯度为95％。结论:该合成路线方便筒捷,能够获得高比度和高纯度的3H标记噻喏啡。Objective: To synthesize 3H-thienorphine. Methods: The bromo-thienorphine was firstly synthesized and 3H-thienorphine was then prepared via the tritium-bromine substitution reaction in the presence of Pd-C and a preparative TLC purification. Results:3H-thienorphine showed a radioactivity at 35mCi and a specific activity at 18Ci·mmol-1 with radiochemical purity at 95% .Conclusion: This synthetic route produces 3H-thienorphine with high specific activity and purity.

关 键 词：噻喏啡 药物合成 氚标记 

分 类 号：R914.5[医药卫生—药物化学] R971.2[医药卫生—药学]