Synthesis of multidentate ligands with amido or amino donor groups for the preparation of rhenium and technetium radiopharmaceuticals

J Radioanal Nucl Chem. 2013;295(3):1599-1604. doi: 10.1007/s10967-012-2356-z. Epub 2012 Dec 11.

Abstract

A new method to prepare novel semi-rigid multidentate ligands containing nitrogen atom, to coordinate with rhenium and technetium, was established. The method was based on formylation of substituted anilines, followed by Mannich reaction with glycine and paraformaldehyde. The method was very promising to design ligands of various molecular structures (L1-L5) to coordinate with rhenium metal ions. The complexes were prepared through ligand exchange with the complex ReOCl3(PPh3)2, giving new complex of the structure ReOCl3L(1-5). The prepared ligands and complexes were identified by the use of UV-vis, and infrared absorption spectrometric techniques, elemental analysis, molecular weight determination by depression of freezing point. These ligands were labeled with 99mTc pertechnetate, and the labeling efficiency of the complexes was measured using a well type scintillation gamma counter equipment and obtained a good yield.

Keywords: Labeled with 99mTc pertechnetate; Multidentate ligands; Radioactive purity; Radiopharmaceuticals; ReOCl3L; Rhenium and technetium complex ReOCl3(PPh3)2.