Preparation and Characterization of Technetium 99m- 4- Methyl- 1, 2- Phenylenediiminophenol Complexes as Nuclear Imaging Agents

Abstract

Four lipophilic 99mTc-imine phenols were prepared and characterized to evaluate their potential uses in nuclear medicine. A series of N2O2 4-methyl-1, 2-phenylenediiminophenol compounds were synthesized and characterized by instruments of melting point, proton nuclear magnetic resonance (1H-NMR) and elemental analysis (EA). The compounds were labeled with 99mTc-pertechnetate eluted from a 99Mo/99mTc generator. The labeling yield, lipophilicity and neutrality of the 99mTc-complexes were carried out by solvent extraction, paper electrophoresis and instant-thin-layer chromatography (ITLC). The 99mTc-complexes exhibit high labeling yield under pH 5~7.5. The lipophilicity of the 99mTc-complexes with log P values span from 2.30 to 2.45. Paper electrophoreses indicate that the 99mTc-complexes are neutral with their positions remaining at the origin. Planar gamma imaging tests demonstrate that the radioactivity and metabolic pathway of 99mTc-complexes on SD rats is via hepatobiliary duct.