Flubatine


Flubatine is a fluorine-18 labeled radiotracer and radioligand for positron emission tomography imaging, developed as a high-affinity ligand for brain nicotinic acetylcholine receptors of the α4β2 subtype. It is used to image cholinergic deficits in disorders such as Alzheimer’s disease and Parkinson’s disease. Both - and - enantiomer bind specifically to α4β2 nAChRs.

Synthesis

Flubatine is prepared by radiolabeling a precursor molecule with fluorine-18 under no-carrier-added conditions. The synthetic route involves two main steps:Precursor synthesis: Optically pure precursor compounds are synthesized by organic chemical methods starting from epibatidine-like intermediates.Radiolabeling: The fluoride ion is introduced by nucleophilic aromatic substitution of the precursor under controlled conditions. Using a trimethylammonium leaving group on the pyridine ring allows for efficient fluorination.