A new high-yield synthetic route to PET CB1 radioligands [ 11C]OMAR and its analogs

Mingzhang Gao, Min Wang, Qi Huang Zheng

Research output: Contribution to journalArticle

14 Scopus citations

Abstract

OMAR analogs reference standards and their corresponding desmethylated precursors were synthesized from substituted anilines either in 4 and 5 steps with 27-32% and 24-31% yield, or in 3 and 4 steps with 21-30% and 19-28% yield, respectively. [11C]OMAR and its analog radioligands were prepared from their desmethylated precursors with [11C]CH3OTf through O-[11C]methylation and isolated by HPLC combined with solid-phase extraction (SPE) in 50-65% radiochemical yields based on [ 11C]CO2 and decay corrected to end of bombardment (EOB), with 370-740 GBq/μmol specific activity at EOB.

Original languageEnglish (US)
Pages (from-to)3704-3709
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number11
DOIs
StatePublished - Jun 1 2012

Keywords

  • [C]OMAR ([C]JHU75528)
  • Automation
  • Brain imaging
  • Cannabinoid receptor 1 (CB1)
  • Positron emission tomography (PET)
  • Radiosynthesis

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

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