High-Relaxivity Gd(III)-Hemicryptophane Complex

Org Lett. 2019 Apr 5;21(7):1999-2003. doi: 10.1021/acs.orglett.9b00081. Epub 2019 Mar 11.

Abstract

The polytopic hemicryptophane cage HC1 combining a cyclotriveratrylene (CTV) unit and a tris(2-aminoethyl)amine (tren) moiety connected by three 2-hydroxyisophthalamide linkers was synthesized in 12 steps. The resulting highly functionalized covalent host is soluble in aqueous medium and has been used to complex Gd(III) ion. The Gd(III)@HC1 complex presents promising relaxivity properties when compared to the clinically used Dotarem MRI agent.