Facile synthesis of bis(hydroxamamide)-based tetradentate ligands for 99mTc-radiopharmaceutical

被引：7
作者：
Xu, H [1 ]
Chu, TW [1 ]
Wang, XG [1 ]
Liu, XQ [1 ]
机构：
[1] Peking Univ, Dept Appl Chem, Coll Chem & Mol Engn, Beijing 100871, Peoples R China
来源：
APPLIED RADIATION AND ISOTOPES | 2005年 / 62卷 / 06期
基金：
中国国家自然科学基金;
关键词：
tetradentate ligands; Tc-99m complex; labeling; N; N'-ethylene bis(1-(4-nitroimidazole-1-yl)propanhydroxy-iminoamide); N'-propylene-bis(1-(4-nitroimidazole-1-yl)-propanhydroxyiminoamide);
D O I：
10.1016/j.apradiso.2004.12.008
中图分类号：
O61 [无机化学];
学科分类号：
070301 ; 081704 ;
摘要：
A facile, two-step synthesis of the bis(hydroxamamide)-based tetradentate ligands for (99)mTc-radiopharmaceuticals is described. Firstly, the hydroxamamide was converted to hydroximic acid chloride by reaction with sodium nitrite in hydrochloric acid at 0 degrees C. Secondly, treating the halide with the ethylenediamine or 1,3-propylenediamine in absolute ethanol formed the desired products, NAP-ethylene bis(l-(4-nitroimidazole-1-yl)-propan-hydroxyiminoamide) (1) and N,N'-propylene bis(l-(4-nitroimidazole-1-yl)-propanhydroxyiminoamide) (II). The corresponding Tc-99m complexes showed high yields and were found by paper clectrophoresis to be electrically neutral under physiological conditions. The partition coefficients indicated a distinct difference between the two complexes. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：919 / 922
页数：4
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