Carborane-carbohydrate derivatives � Versatile platforms for developing targeted radiopharmaceuticals

Green, Andrew E. C.; Harrington, Laura E.; Valliant, John F.
November 2008
Canadian Journal of Chemistry;Nov2008, Vol. 86 Issue 11, p1063
Academic Journal
A series of carborane-carbohydrate derivatives were prepared as model platforms for developing targeted radiopharmaceuticals in which a single ligand can be tagged with two different classes of radionuclides. A nido-carborane linked to glucose was synthesized and the cage labelled with a radiometal (99mTc) and a radiohalogen (125I) in good radiochemical yield. The 99mTc-metallocarborane derivative was prepared via microwave-assisted reactions, while the iodinated derivative was prepared using oxidative labelling methods in mere minutes. Fully characterized reference standards were prepared using nonradioactive rhenium and iodine and used to demonstrate that the isolated radioactive compounds were in fact the desired targets. The work reported, which is one of the rare examples of a single ligand system that can be labelled with both radiohalogens and radiometals, forms the basis of a new paradigm for developing targeted radiopharmaceuticals.


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