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

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%.