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首页> 外文期刊>Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine >Synthesis procedure for routine production of 2-F-18fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-F-18F-A-85380)
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Synthesis procedure for routine production of 2-F-18fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-F-18F-A-85380)

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摘要

2-F-18Fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-F-18F-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-18F-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-18F-A-85380 were produced from a starting activity of 100GBq F-18fluoride 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.

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