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 Hutchins, Qi-Huang Zheng

Research output: Contribution to journalArticle

34 Citations (Scopus)

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

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Raclopride
Dopamine D2 Receptors
methyl bromide
Methylation
Purification

Keywords

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

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Fei, X., Mock, B. H., DeGrado, T. R., Wang, J. Q., Glick-Wilson, B. E., Sullivan, M. L., ... Zheng, Q-H. (2004). An improved synthesis of PET dopamine D2 receptors radioligand [11c]raclopride. Synthetic Communications, 34(10), 1897-1907. https://doi.org/10.1081/SCC-120034174

An improved synthesis of PET dopamine D2 receptors radioligand [11c]raclopride. / Fei, Xiangshu; Mock, Bruce H.; DeGrado, Timothy R.; Wang, Ji Quari; Glick-Wilson, Barbara E.; Sullivan, Michael L.; Hutchins, Gary; Zheng, Qi-Huang.

In: Synthetic Communications, Vol. 34, No. 10, 2004, p. 1897-1907.

Research output: Contribution to journalArticle

Fei, X, Mock, BH, DeGrado, TR, Wang, JQ, Glick-Wilson, BE, Sullivan, ML, Hutchins, G & Zheng, Q-H 2004, 'An improved synthesis of PET dopamine D2 receptors radioligand [11c]raclopride', Synthetic Communications, vol. 34, no. 10, pp. 1897-1907. https://doi.org/10.1081/SCC-120034174
Fei X, Mock BH, DeGrado TR, Wang JQ, Glick-Wilson BE, Sullivan ML et al. An improved synthesis of PET dopamine D2 receptors radioligand [11c]raclopride. Synthetic Communications. 2004;34(10):1897-1907. https://doi.org/10.1081/SCC-120034174
Fei, Xiangshu ; Mock, Bruce H. ; DeGrado, Timothy R. ; Wang, Ji Quari ; Glick-Wilson, Barbara E. ; Sullivan, Michael L. ; Hutchins, Gary ; Zheng, Qi-Huang. / An improved synthesis of PET dopamine D2 receptors radioligand [11c]raclopride. In: Synthetic Communications. 2004 ; Vol. 34, No. 10. pp. 1897-1907.
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AU - Hutchins, Gary

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