一种二氨基二硫醇双功能偶联剂的合成及其锝[^(99m)Tc]标记  

Synthesis of a bisaminoethanethiol bifunctional coupling agent and its labeling of technetium

作　　者：刘春仪[1] 李晓敏[1] 王颂佩[1] 唐婕[1] 陈正平[1] 

机构地区：[1]江苏省原子医学研究所卫生部核医学重点实验室,江苏无锡214063

出　　处：《化学研究与应用》2009年第6期824-827,共4页Chemical Research and Application

基　　金：江苏省高技术研究计划(BG2007603)资助;国家自然科学基金(30570518)资助;江苏省卫生厅科研基金(H200401)资助

摘　　要：本文在比较温和的条件下,以半胱胺盐酸盐为原料,合成了一种二氨基二硫醇双功能偶联剂N-(2-巯乙基)-2-[(2-羧乙基)(2-巯乙基)氨基]乙酰胺。部分合成步骤在参考文献的基础上进行了改进,优化了合成条件,总收率为5.4%,各步产物结构均经IR、MS等进行了表征。采用葡庚糖酸钠(GH)交换法对目标产物进行了锝[99mTc]标记,采用上行薄层色谱(TLC)十段法测定的标记率为[(96.85±0.23)%,n=4]。A new compound N- （ 2 - mercaptoethyl ） -2 - [ （ 2 -earboxylethyl） （ 2 -mercaptoethyl ） amino ] aeetamide was synthesized by using cysteamine hydrochloride as raw material in moderate conditions. Part of the process was made further improvement according to the literature methods. The overall yield was 5.4%. The products of every step was characterized by IR, MS The objective product was labeled with technetium by sodium glucoheptonate （GH） transchelation. Radiolabeling yield was determined by thin layer chromatography （TLC）. Average labeling yield was about 97%.

关 键 词：双功能偶联剂 二氨基二硫醇 标记 99mTc 

分 类 号：R817.9[医药卫生—影像医学与核医学]