MAMA双功能螯合剂前体的合成及结构表征

Synthesis and structural characterization of the precursor of MAMA BFC

双功能螯合剂在放射性药物的研究、合成、应用,特别是在生物分子的放射性标记方面发挥着极为重要的作用。本文采用简易方法合成了MAMA双功能螯合剂前体,N-(2″-对甲氧苄巯乙基)-2-[(2′-对甲氧苄巯乙基)氨基]乙酰胺,并通过Uv-visI、R1、HNMR、MS以及元素分析等对其结构组成进行了确证;同时,利用Gaussian 03W程序对其进行了结构优化描述,并计算了相应的分子能量。此外,对制备得到的前体进行了稳定化处理,将其转化为盐酸盐形式,并用IR1、HNMR等进行了检验,确定了此处理是合理可行的。

The present paper aims to introduce the authors＇ newly developed method on synthesizing a hi-functional chelator, or a bifunctional chelating agent. As is known, the bi-functional chelating agent is of great importance in the radio-pharmaceutical domain, especially, when it was labeled as bio-molecule with radio-nuclides. The authors of this paper has done a series of experiments with N-[2＂- （ 4-methoxybenzylmercapto ） ethyl 1-2-[（ 2＇-（ 4-methoxybenzylmercapto）ethyl）aminol acetamide trying to synthesize the hi-functional chelator as a precursor of MAMA in a simple method, and then verify it by Uv-vis, IR, ^1HNMR, MS and element analysis. Next, they have given a detailed description of its optimum structure by using Gaussian 03W program, with the homologous minimal energy of its molecules calculated in the meantime, And, finally, the precursor has been translated into its hydrochloride as a stable form for convenient reservation. The likelihood and reasonableness of this method has also been testified by measuring some relevant spectroscopic properties such as IR and ^1HNMR.