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Synthesis of a new tricyclic tetraazatriacetic acid as ligand for gadolinium(III)
Authors:Fabienne Dioury  Aurore Di Scala-Roulleau  Alain Guy
Institution:a Laboratoire de Chimie Organique UMR CNRS 7084, Case 303, Conservatoire national des arts et métiers, 2 rue Conté, 75003 Paris, France
b Guerbet, Centre de Recherche, BP 50400, 95943 Roissy CdG Cedex, France
Abstract:Polyazapolycarboxylic acids are known to be efficient ligands for the development of gadolinium-based contrast agents used in magnetic resonance imaging (MRI). Given that rigidification of the ligand structure seems to be an important structural parameter to increase the relaxivity of the corresponding gadolinium complex, we have synthesized a new tricyclic tetraazatriacetate ligand from commercially available trans-2-aminocyclohexanol. In the synthetic routes described here, the 2-nitrobenzenesulfonamide chemistry was used to selectively functionalize the polyamine precursors.
Keywords:Polyazapolycarboxylic acid  Macrocyclic ligand  Gadolinium  Contrast agent  MRI  2-Nitrobenzene sulfonamide  Functionalized polyamine
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