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Comparison of tridentate ligands in competition experiments for their ability to form a [Tc(CO)3] complex
Authors:Dirk Rattat  Bernard Cleynhens  Humphrey Fonge
Institution:a Laboratory for Radiopharmaceutical Chemistry and Nuclear Medicine, Catholic University of Leuven, Herestraat 49, B-3000 Leuven, Belgium
b Mallinckrodt Inc., Nuclear Medicine R&D, 1755 Petten, The Netherlands
Abstract:In this study we have compared different ligands containing three or more hetero-atoms (N, O and/or S) with respect to their ability to form tridentate complexes with a Tc-tricarbonyl moiety. Comparison of each ligand in a competition reaction with histidine first and then with each other compound allowed to rank the ligands according to their ability of complex formation with the 99mTc(CO)3]+ precursor from diethylenetriamine (most efficient of the studied ligands) to nitrilotriacetic acid (weakest complexing properties). The results provide insight in the structural requirements for the formation of stable Tc-tricarbonyl complexes and suggest preferred combinations and arrangements of the hetero-atoms involved in the complex formation. They also give a good indication which type of ligand is most appropriate to modify biomolecules for an efficient and stable labelling with a Tc-tricarbonyl moiety.
Keywords:Technetium  Tc-tricarbonyl  Ligand  Competition reaction
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