Synthesis of radiolabeled sugar metal complexes

C - Chemistry – Metallurgy – 07 – F

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C07F 13/00 (2006.01) C07F 15/00 (2006.01) C07F 17/00 (2006.01)

Patent

CA 2579355

The invention provides a method for manufacturing or preparing neutral, low molecular weight 99mTc-labeled and 186Re-labeled carbohydrate complexes with an improved radiochemical yield from a simple functionalized sugar, such as glucosamine. In particular the synthesis relies on single ligand transfer (SLT) or double ligand transfer (DLT) reactions for converting a ferrocene compound into a rhenium or technetium tricarbonyl complex. The ferrocene compound may be linked to a sugar through various functional groups including, for example, thio, amino and alcohol functionalities to provide a wide range of radiolabeled sugar complexes that include both water soluble and relatively water insoluble compounds.

L'invention concerne un procédé permettant de fabriquer ou de préparer des complexes glucidiques marqués 99mTc et 186Re neutres et à faible poids moléculaire avec un rendement radiochimique amélioré à partir d'un simple sucre fonctionnalisé, tel que la glucosamine. D'une manière plus spécifique, la synthèse est basée sur des réactions de transfert de ligands simples (SLT) ou de transfert de ligands doubles (DLT) afin de convertir un composé ferrocène en un complexe de tricarbonyle de rhénium ou de technétium. Le composé ferrocène peut être lié à un sucre par divers groupes fonctionnels comprenant, notamment, des fonctionnalités thio, amino et alcool afin d'obtenir une large gamme de complexes de sucre radiomarqués qui comprennent à la fois des composés solubles dans l'eau et relativement insolubles dans l'eau.

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