A concise and efficient synthesis of flumazenil and its precursor for radiolabeling with fluorine-18

Sean R. Donohue, Robert F. Dannals

Research output: Contribution to journalArticlepeer-review

Abstract

Presently there is a strong interest in developing radioligands for in vivo imaging the GABAA-Bz site with positron emission tomography (PET). Flumazenil (1), a high-affinity GABAA-Bz site inverse agonist, is amenable for 11C and 18F-labeling. The current methods for synthesis of 1 and its precursor for 18F-labeling are not ideal and restrict structure-activity relationship (SAR) development. Herein we present a novel and less troublesome synthesis of 1 and its cognates to aid in the development of improved radioligands for PET imaging of GABAA-Bz site.

Original languageEnglish (US)
Pages (from-to)7271-7273
Number of pages3
JournalTetrahedron Letters
Volume50
Issue number52
DOIs
StatePublished - Dec 30 2009

Keywords

  • Benzodiazepine
  • Flumazenil
  • Fluorine-18
  • GABA-Bz site
  • Nitromazenil
  • PET

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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