Synthesis of Edatrexate (2-13C-glutamate)

Joseph I. DeGraw, William T. Colwell, Thomas Jue

Research output: Contribution to journalArticlepeer-review


The experimental antitumor drug Edatrexate, labeled with 99% 13C at the 2-position of the glutamate acid group was required for 13C-magnetic resonance spectroscopy studies in biological media. Coupling of 2,4-diamino-4-deoxy-10-ethyl-10-deazapteroic acid with diethyl L-2-13C-glutamate as promoted by BOP reagent afforded Edatrexate (2-13C-glu) diethyl ester in 60% yield following purification by column chromatography. Saponification by aqueous NaOH in 2-methoxyethanol gave the target molecule in 44% yield or 26% overall.

Original languageEnglish (US)
Pages (from-to)99-103
Number of pages5
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Issue number2
StatePublished - Feb 1997


  • C-magnetic resonance spectroscopy
  • Antitumor
  • Edatrexate

ASJC Scopus subject areas

  • Clinical Biochemistry
  • Molecular Medicine
  • Analytical Chemistry
  • Organic Chemistry
  • Drug Discovery
  • Pharmacology


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