Many interesting PET radioligands contain fluoro-pyridine moiety, such as [18F]AZD4694 for Aβ-amyloid in Alzheimer’s disease, [18F]T807 for neurofibrillary tangle in Alzheimer’s disease, [18F]NCFHEB for α4β2-nicotinic acetyl choline receptors (nACnRs), [18F]fluoroisonicotinamide for melanoma cancer, and many other radioligands. A variety of synthetic radiolabeling methods have been developed to synthesize these radioligands, with different leaving groups, such as halide, tosylate, -NO2, and –NR3+. Not every precursor is synthetically available, since these with the most reactive leaving groups are normally much challenge to synthesize. There is a need for auxiliary agents to activate somewhat inert precursor for radiolabeling by [18F]fluoride. We have developed a group of additives based on dabco/quinuclidine, and their other analogs, to facilitate the radiolabeling of fluoro-pyridine moiety by [18F]fluoride. The scope and limitation of this radiolabeling method are described here.

Dabco/quinuclidine increases the radiofluorinations of 2-halopyridines

254th National Meeting (2017)

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