Positron Emission Tomography (PET) imaging with Zr-89 has been gaining a lot of interest because it allows for extended imaging of slow processes such as slowly-accumulating pharmaceuticals or changes in tumor size. In particular, it is suited for imaging with large biomolecules such as antibodies and nano-particles. Desferrioxamine-B (DFO) has been often used as the ligand of choice for imaging with Zr-89, but it has been found to lack stability <i>in vivo </i>causing the radio-active Zr-89 to accumulate in the bone, which has harmful effects. The hexadentate DFO leaves two coordination sites on Zr-89 open, which has been related to the <i>in vivo</i> instability of the complex. Otherwise, few bifunctional ligands meeting the general requirement of eight-coordination and high stability with Zr(IV) are known, and some of those require an extended synthetic route. In this work, we report the design, efficient one-step synthesis and aqueous speciation of a bifunctional octadentate Zr(IV) ligand.

Design and efficient synthesis of a bifunctional octadentate ligand for immunoPET imaging with Zr-89

254th National Meeting (2017)

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