^3H—去甲乌药碱的合成  

Synthesis of 3 H-higenamine

作　　者：张正[1] 陈宝玲[1] 郑英丽[1] 武德柱[2] 顾德良[1] 方丽[1] 

机构地区：[1]中国医学科学院,中国协和医科大学阜外心血管病医院药剂科,北京100037 [2]中国原子能科学研究院同位素研究所

出　　处：《中华核医学杂志》2003年第3期177-178,共2页Chinese Journal of Nuclear Medicine

基　　金：卫生部科学研究基金资助项目 (98 2 0 1 7)

摘　　要：目的　合成3H 去甲乌药碱。方法　以 1 (4 甲氧基苄基 ) 6 ,7 二甲氧基 3,4 二氢 异喹啉为前体 ,采用催化氚气加成反应及氢溴酸脱甲氧基反应合成3H 去甲乌药碱。标记物经薄层层析纯化 ,经紫外分光光度法 (UV)和高效液相色谱法 (HPLC)进行质量鉴定。结果　合成的3H 去甲乌药碱UV和HPLC图谱鉴定与去甲乌药碱标准品一致 ,放化纯 >98% ,比活度 >370GBq mmol。结论　该微量合成3H 去甲乌药碱的方法为去甲乌药碱的药代动力学研究提供了物质基础。Objective To synthesize 3 H higenamine. Methods The synthesis consisted of catalytic tritium gas addition and demethoxylation. 3 H higenamine was purified by thin layer chromatography and identified by UV and HPLC. Results The UV and HPLC spectrum of the synthesized 3 H higenamine were identical with that of the higenamine standard, the radiochemical purity was more than 98% and the specific activity was 370 GBq/mmol. Conclusion An effective method for synthesis of 3 H higenamine in small scale is developed, and it makes the further pharmacodynamical research of higenamine feasible.

关 键 词：^3H-去甲乌药碱 化学合成 紫外分光光度法 高效液相色谱法 

分 类 号：R914[医药卫生—药物化学]