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Burai, L ; Tóth, E ; Sour, A ; Merbach, AE

Separation and characterization of the two diastereomers for [Gd(DTPA-bz-NH2)(H2O)]2-, a common synthon in macromolecular MRI contrast agents. Their water exchange and isomerization kinetics

Inorganic Chemistry 44 (10) 3561-3568

par Administrateur - publié le

Abstract :

Chiral, bifunctional poly(amino carboxylate) ligands are commonly used for the synthesis of macromolecular, Gd-III-based MRI contrast agents, prepared in the objective of increasing relaxivity or delivering the paramagnetic Gd-III to a specific site (targeting). Complex formation with such ligands results in two diastereomeric forms for the complex which can be separated by HPLC. We demonstrated that the diastereomer ratio for Ln(III) DTPA derivatives (∼ 60:40) remains constant throughout the lanthanide series, in contrast to Ln(III) EPTPA derivatives, where it varies as a function of the cation size with a maximum for the middle lanthanides (DTPA(5-) = diethylenetriaminepentaacetate ; EPTPA(5-) = ethylenepropylenetriaminepentaacetate).