Synthesis of (±) 3-(6-nitro-2-quinolinyl)-[9-methyl-11C]-3,9-diazabicyclo-[4.2.1]- nonane ([11C-methyl]NS 4194)

Svend B. Jensen, Dirk Bender, Donald F. Smith, Jørgen Scheel-Krüger, Elsebet Nielsen, Gunnar M. Olsen, Dan Peters, Albert Gjedde

Research output: Contribution to journalArticle

Abstract

(±) 3-(6-Nitro-2-quinolinyl)-[9-methyl-11C]-3,9-diazabicyclo-[4.2.1]- nonane ([11C-methyl]NS 4194), a selective serotonin reuptake inhibitor (SSRI), was synthesised within 35 min after end of bombardment with a radiochemical purity > 98%. It had a decay-corrected radiochemical yield of 7% after preparative HPLC, and a specific radioactivity around 37 GBq/μmol (EOS). A typical production starting with 40 GBq [11C]CO2 yielded 800 MBq of radiolabelled [11C-methyl]NS 4194 in a formulated solution. The synthesis of the precursor to [11C-methyl]NS 4194, (±) 9-H-3-[6-nitro-(2-quinolinyl)]-3,9-diazabicyclo-[4.2.1]-nonane, as well as the unlabelled analogue (±) 9-methyl 3-[6-nitro-(2-quinolinyl)]-3,9-diazabicyclo-[4.2.1]-nonane (NS 4194), are also described.

Original languageEnglish (US)
Pages (from-to)181-189
Number of pages9
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume45
Issue number3
DOIs
StatePublished - Mar 15 2002

Keywords

  • C
  • PET
  • Radiolabelling
  • Selective serotonin reuptake inhibitor

ASJC Scopus subject areas

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

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    Jensen, S. B., Bender, D., Smith, D. F., Scheel-Krüger, J., Nielsen, E., Olsen, G. M., Peters, D., & Gjedde, A. (2002). Synthesis of (±) 3-(6-nitro-2-quinolinyl)-[9-methyl-11C]-3,9-diazabicyclo-[4.2.1]- nonane ([11C-methyl]NS 4194). Journal of Labelled Compounds and Radiopharmaceuticals, 45(3), 181-189. https://doi.org/10.1002/jlcr.542