Carbon‐11 labeling of a potent, nonpeptide, at1‐selective angiotensin‐II receptor antagonist: MK‐996

William B. Mathews, H. Donald Burns, Robert F. Dannals, Hayden T. Ravert, Elizabeth M. Naylor

Research output: Contribution to journalArticle

Abstract

[α‐11C]Benzoyl chloride was synthesized and purified by normal phase HPLC. [11C]MK‐996 ([11C]N‐[[4′[(2‐ethyl‐5,7‐dimethyl‐3H‐imidazo [4,5‐b]pyridin‐3‐yl)methyl][1,1′‐biphenyl]‐2‐yl]sulfonyl]‐benzamide), a potent and selective ligand for the AT1 receptor, was prepared by N‐benzoylation of L‐159,221 with [α‐11C]benzoyl chloride in tetrahydrofuran using lithium bis(trimethylsilyl)amide as a base. The radiotracer was purified by semi‐preparative reverse‐phase HPLC. The average specific activity was 1162 mCi/μmol calculated at end‐of‐synthesis (EOS). The average time of synthesis including formulation was 30 minutes.

Original languageEnglish (US)
Pages (from-to)729-737
Number of pages9
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume36
Issue number8
DOIs
StatePublished - Aug 1995

Keywords

  • Angiotensin
  • Benzoyl chloride
  • Carbon‐11
  • PET
  • Radiotracer

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

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