Improved synthesis of β-CIT and [11C]β-CIT labeled at nitrogen or oxygen positions

Qi Huang Zheng, G. Keith Mulholland

Research output: Contribution to journalArticle

55 Scopus citations


The important radiotracer precursor 2β-carbomethoxy-3β-(4-iodophenyl)-tropane (β-CIT, RTI-55) was made in 52% overall yield from cocaine. Key steps were improved conjugate Grignard addition to anhydroecgonine methyl ester with >3.5:1 2β: 2α-isomer selectivity, and a mild new direct aromatic iodination with I2 and silver triflate in CH2Cl2. The [11C]β-CIT was labeled at either the N or O positions with [11C]methyl triflate; and efficient reversed-phase HPLC was used to preparatively separate [N-11C]β-CIT from N-nor-β-CIT for the first time, and a fast solid-phase extraction (SPE) method was applied to preparatively separate [O-11C]β-CIT from β-CIT-acid precursor.

Original languageEnglish (US)
Pages (from-to)981-986
Number of pages6
JournalNuclear Medicine and Biology
Issue number8
StatePublished - Nov 1 1996


  • carbon-11
  • iodination
  • monoamine transporter
  • phenyltropane
  • RTI-55

ASJC Scopus subject areas

  • Cancer Research
  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging

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