Synthesis procedure for routine production of 2-[18F]fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-[18F]F-A-85380)

2-[F-18]Fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-[F-18]F-A-85380) was among the first subtype selective radioligands to visualise the in vivo distribution of alpha 4 beta 2-containing neuronal nicotinic acetylcholine receptors (nAChRs) in human brain. We developed a one-pot synthesis for the preparation of 2-[F-18]F-A-85380 in a commercially available TRACERlab FXF-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 20GBq 2-[F-18]F-A-85380 were produced from a starting activity of 100GBq [F-18]fluoride in 60min with a specific activity of about 4 center dot 105 GBq/mmol and a mean radiochemical purity of more than 99%. (c) 2007 Elsevier Ltd. All rights reserved.