Facile synthesis of bis(hydroxamamide)-based tetradentate ligands for 99mTc-radiopharmaceutical.
A facile, two-step synthesis of the bis(hydroxamamide)-based tetradentate ligands for 99mTc-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, N,N'-ethylene bis(1-(4-nitroimidazole-1-yl)-propan-hydroxyiminoamide) (I) and N,N'-propylene bis(1-(4-nitroimidazole-1-yl)-propanhydroxyiminoamide) (II). The corresponding 99mTc complexes showed high yields and were found by paper electrophoresis to be electrically neutral under physiological conditions. The partition coefficients indicated a distinct difference between the two complexes.
Xu
Hong
H
Department of Applied Chemistry, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
Chu
Taiwei
T
Wang
Xiangyun
X
Liu
Xinqi
X
D004590:Electrophoresis, Paper; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000737:chemistry; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D019275:Radiopharmaceuticals / Q000737:chemistry*
D006877:Hydroxamic Acids; D008024:Ligands; D019275:Radiopharmaceuticals