Mundwiler, S; Candreia, L; Häfliger, P; Ortner, K; Alberto, R (2004). Preparation of no-carrier-added technetium-99m complexes via metal-assisted cleavage from a solid phase. Bioconjugate Chemistry, 15(1):195-202.
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A novel method for the preparation of no-carrier-added (nca) complexes [99mTc(CO)3L] (L = diethylenetriamine or picolylamine-N-acetic acid) is described. The ligands were covalently bound to a solid support of organic polymers via formation of a tertiary amine from the chelating unit. This C-N bond to the solid phase is selectively cleaved during the formation of the technetium complexes by intramolecular nucleophilic attack of a remaining hydroxy ligand to the alpha-carbon. The complex [99mTc(CO)3L] is released into solution while uncomplexed ligand and uncleaved complex remain solid-phase bound. High specific activity technetium complexes can then be isolated by simple filtration. Cleavage yield depends on temperature, pH, and ligand. Up to 50% release from the solid phase could be achieved under optimized conditions. Corresponding to the 99mTc concentration, free ligand is present in concentrations lower than 10(-7) M. If a targeting vector is conjugated to these ligands, no-carrier-added radiopharmaceuticals can be prepared in that way.
|Item Type:||Journal Article, refereed|
|Communities & Collections:||07 Faculty of Science > Department of Chemistry|
|Deposited On:||11 Feb 2008 12:25|
|Last Modified:||27 Nov 2013 18:28|
|Publisher:||American Chemical Society|
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