Simple synthesis of new carbon-11-labeled 1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives for PET imaging of A3 adenosine receptor

Mingzhang Gao, Andy Chufan Gao, Min Wang, Qi Huang Zheng

Research output: Contribution to journalArticle

6 Scopus citations

Abstract

The reference standards 4a-b, 6a-b, 7a-c, and desmethylated precursors 9a-b, 10a-b, 8a-c were synthesized from 4-methoxyaniline, ethyl 2-chloro-acetoacetate and substituted benzene-1,2-diamines with 3, 5, 6 steps in 61-67%, 34-41%, 23-31%, and with 4, 6, 7 steps in 49-57%, 28-35%, 20-27% overall chemical yield, respectively. The target tracers [11C]4a-b, [11C]6a-b, [11C]7a-c were synthesized from their corresponding precursors with [11C]CH3OTf through O-[11C]methylation and isolated by simplified SPE in 40-60% decay corrected radiochemical yields at EOB, with 185-370GBq/μmol specific activity at EOS.

Original languageEnglish (US)
Pages (from-to)71-78
Number of pages8
JournalApplied Radiation and Isotopes
Volume91
DOIs
StatePublished - Sep 2014

Keywords

  • Cancer
  • Carbon-11-labeled 1,2,4-triazolo[4,3,a]quinoxalin-1-one derivatives
  • Cardiac diseases
  • Neurological disorders
  • Positron emission tomography (PET)

ASJC Scopus subject areas

  • Radiation
  • Medicine(all)

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