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Oxidative Fluorination with [18F]Fluoride - New Radiochemistry for PET Imaging (OXIFLU)
Start date: Mar 1, 2012, End date: Feb 28, 2014 PROJECT  FINISHED 

"The objective of this proposal is to provide a solution to a well-recognised problem in 18F-radiochemistry: the direct fluorination of electron rich aromatics with a nucleophilic source of 18F-Fluoride. The value of this new radiochemistry will be challenged with the synthesis of 6-[18F]Fluoro-L-3,4-dihydroxyphenylalanine ([18F]FDOPA) and 6-[18F]Fluoro-L-meta-tyrosine ([18F]FMT), two high value tracers to image the presynaptic sites of the dopaminergic system; yet these two radiotracers are notoriously difficult to produce using currently available radiochemistry. Conceptually, we advance that the nucleophilic fluorination of electron rich aromatics with fluoride may be possible using a so-called “substrate umpolung” approach. Under oxidative condition, we will revert the reactivity profile of the substrate from a nucleophilic to an electrophilic entity (umpolung), thereby allowing for nucleophilic 18F-labelling. This approach, which will rely heavily on microfluidic technology, has never been exploited for 18F-radiolabelling."

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