An efficient synthetic strategy for obtaining 4-methoxy carbon isotope labeled combretastatin a-4 phosphate and other Z-combretastatins

George Pettit, Mathew D. Minardi, Fiona Hogan, Pat M. Price

Research output: Contribution to journalArticle

10 Scopus citations

Abstract

Human cancer and other clinical trials under development employing combretastatin A-4 phosphate (1b, CA4P) should benefit from the availability of a [11C]-labeled derivative for positron emission tomography (PET). In order to obtain a suitable precursor for addition of a [11C]methyl group at the penultimate step, several new synthetic pathways to CA4P were evaluated. Geometrical isomerization (Z to E) proved to be a challenge, but it was overcome by development of a new CA4P synthesis suitable for 4-methoxy isotope labeling.

Original languageEnglish (US)
Pages (from-to)399-403
Number of pages5
JournalJournal of Natural Products
Volume73
Issue number3
DOIs
StatePublished - Mar 26 2010

ASJC Scopus subject areas

  • Analytical Chemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine
  • Organic Chemistry

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