Abstract
2-[ 18F]Fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-[ 18F]F-A-85380) was among the first subtype selective radioligands to visualise the in vivo distribution of α4 β2-containing neuronal nicotinic acetylcholine receptors (nAChRs) in human brain. We developed a one-pot synthesis for the preparation of 2-[ 18F]F-A-85380 in a commercially available TRACERlab FX F−N synthesis module. The synthesis comprises a nucleophilic substitution followed by hydrolysis of a t-butyloxycarbonyl (BOC)-protected intermediate. After formulation for intravenous application up to 20 GBq 2-[ 18F]F-A-85380 were produced from a starting activity of 100 GBq [ 18F]fluoride in 60 min with a specific activity of about 4·10 5 GBq/mmol and a mean radiochemical purity of more than 99%.
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