A Novel Ternary Ligand System Useful for Preparation of Cationic 99mTc-Diazenido Complexes and 99mTc-Labeling of Small Biomolecules

摘要: This report describes a novel ternary ligand system composed of phenylhydrazine, crown ether-containing dithiocarbamate (DTC), and PNP-type bisphosphine (PNP). The combination three different ligands with (99m)Tc results in cationic (99m)Tc-diazenido complexes, [(99m)Tc(NNAr)(DTC)(PNP)]+, potential radiopharmaceuticals for heart imaging. Synthesis complexes can be accomplished two steps. For example, the reaction phenylhydrazine (99m)TcO4- at 100 degrees C presence excess stannous chloride 1,2-diaminopropane-N,N,N',N'-tetraacetic acid (PDTA) [(99m)Tc(NNPh)(PDTA)n] intermediate, which then reacts sodium N-(dithiocarbamato)-2-aminomethyl-15-Crown-5 (L4) N,N-bis[2-(bis(3-ethoxypropyl)phosphino)ethyl]ethoxyethylamine (PNP6) 15 min to give complex, [(99m)Tc(NNPh)(L4)(PNP6)]+ high yield (>90%). Cationic [(99m)Tc(NNPh)(DTC)(PNP)]+ are stable > or = 6 h. Their composition was determined 1:1:1:1 Tc:NNPh:DTC:PNP using mixed-ligand experiments on tracer ((99m)Tc) level further confirmed by ESI-MS spectral data model compound [Re(NNPh)(L4)(L6)]+. It found that both DTCs bisphosphines have significant impact lipophilicity their complexes. Results from (99m)Tc-labeling efficiency experiment showed 4-hydrazinobenzoic (HYBA) might useful as bifunctional coupling agent small biomolecules. However, HYBA is much lower than 6-hydrazinonicotinic (HYNIC) tricine trisodium triphenylphosphine-3,3',3''-trisulfonate (TPPTS) coligands.