Synthesis of 123I‐and labelled 5‐iodo‐6‐nitroquipazine

Chester A. Mathis, Joel D. Enas, Stephen M. Hanrahan, Eyup Akgün

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The syntheses of the potent and selective serotonin reuptake complex radioligands [123I]‐ and [125I]5‐iodo‐6‐nitroquipazine (5‐iodo‐6‐nitro‐2‐piperazinylquinoline) are reported. A seven step synthetic sequence provided the BOC‐protected 5‐tributyltin‐6‐nitroquipazine precursor for radioiodination. End of synthesis radioiodination yields of ∼40% for 123I and ∼60% for 125I were achieved resulting in labelled products with high specific activities (>4000 and >2000 Ci/mmol, respectively) and radiochemical purities (>98%).

Original languageEnglish (US)
Pages (from-to)905-913
Number of pages9
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Issue number10
StatePublished - Oct 1994


  • 5‐iodo‐6‐nitroquipazine
  • 5‐iodo‐6‐nitro‐2‐piperazinylquinoline
  • [I]5‐iodo‐6‐nitroquipazine
  • [I]5‐iodo‐6‐nitroquipazine
  • serotonin reuptake complex


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