Fluorine-18 (18F) is the most popular radionuclide for clinically relevant Positron Emission Tomography (PET) applications due to its ease of preparation and nuclear decay properties.  The use of this radionuclide in medical diagnosis can be implemented through the use of [18F]-fluoride binding agent that is conjugated to a biomolecule just prior to injection.  This approach is powerful because time-consuming synthetic steps can be done before introduction of the relatively short-lived 18F radionuclide. As part of our ongoing efforts in this area, we have synthesized the ortho-phenylene phosphine-boranes 1  and 2  which their trifluoroborate moieties are stabilized by neighboring phosphonium ions to impede fluoride ion dissociation in water. We also show that the [18/19F]1  and [18/19F]2  are easily prepared via direct 18F-19F isotopic exchange reaction in aqueous solution and are stable in vivo.  In this presentation, we will disclose a new type of zwitterionic boron-based fluoride captors with superior hydrolytic stability.  We will also show how these new [18F]-fluoride captors can be radiolabeled and conjugated to biomolecules.

Novel organoboranes for <sup>18</sup>F fluoride anion capture

248th National Meeting (2014)

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Novel organoboranes for 18F fluoride anion capture

Novel organoboranes for ¹⁸F fluoride anion capture