An improved synthesis of PET dopamine D2 receptors radioligand [11c]raclopride

Xiangshu Fei, Bruce H. Mock, Timothy R. DeGrado, Ji Quari Wang, Barbara E. Glick-Wilson, Michael L. Sullivan, Gary D. Hutchins, Qi Huang Zheng

Research output: Contribution to journalArticlepeer-review

34 Scopus citations

Abstract

An improved synthesis of [11C]raclopride is reported. The precursor desmethyl-raclopride was synthesized from 3,5-dichloro-2,6-dimethoxybenzoic acid and (S)-(-)-2-aminoethyl-1-ethylpyrrolidine via a straight-forward, four-step synthetic approach with 29% overall chemical yield. [11C]Raclopride was prepared by O-[11C]methylation of the precursor with [ 11C]methyl triflate and purification with a semi-preparative HPLC method in 20-34% radiochemical yield, based on [11C]methyl bromide, decay corrected to end of bombardment (EOB).

Original languageEnglish (US)
Pages (from-to)1897-1907
Number of pages11
JournalSynthetic Communications
Volume34
Issue number10
DOIs
StatePublished - 2004

Keywords

  • Dopamine D receptors
  • Positron emission tomography
  • Radioligand
  • Synthesis
  • [C]Raclopride

ASJC Scopus subject areas

  • Organic Chemistry

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