1587709-89-4Relevant academic research and scientific papers
Enantioselective radiosynthesis of positron emission tomography (PET) tracers containing [18F]fluorohydrins
Graham, Thomas J. A.,Lambert, R. Frederick,Ploessl, Karl,Kung, Hank F.,Doyle, Abigail G.
supporting information, p. 5291 - 5294 (2014/05/06)
Herein, we describe an operationally straightforward radiosynthesis of a chiral transition metal fluoride catalyst, [18F](salen)CoF, and its use for late-stage enantioselective aliphatic radiofluorination. We demonstrate the utility of the method by preparing single enantiomer experimental and clinically validated PET tracers that contain base-sensitive functional groups, epimerizable stereocenters, and nitrogen-rich motifs. Unlike the conventional radiosyntheses of these targets with [18F]KF, labeling with (salen)CoF is possible in the last step and under exceptionally mild conditions. These results constitute a rare example of a nucleophilic radiofluorination using a transition metal fluoride and highlight the potential of such reagents to enhance traditional methods for labeling aliphatic hydrocarbons.
