Synthesis of a radiotracer for studying nicotinic acetylcholine receptors: 2-[18F]fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-[18F]A- 85380)

Andrew G. Horti, Andrei O. Koren, Hayden T. Ravert, John L. Musachio, William B. Mathews, Edythe D. London, Robert F. Dannals

Research output: Contribution to journalArticlepeer-review


The radiochemical synthesis of 2-[18F]fluoro-3-(2(S)- azetidinylmethoxy)pyridine (2-[18F]A-85380, [18F]1) was accomplished by Kryptofix® 222 assisted nucleophilic no-carrier-added [18F]fluorination of 2-iodo-3-((1-tert-butoxycarbonyl-2(S)-azetidinyl)methoxy)pyridine, 2 followed by acidic deprotection. The average radiochemical yield was 10% and the average specific radioactivity was 1050 mCi/μmol, calculated at end-of- synthesis (EOS).

Original languageEnglish (US)
Pages (from-to)309-318
Number of pages10
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Issue number4
StatePublished - Apr 1998


  • A-85380
  • Acetylcholine
  • F
  • Fluorination
  • Halogen-exchange
  • Nicotinic receptors
  • Positron emission tomography
  • Radiotracer

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

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