Synthesis of combretastatin A-4 and its water-soluble analogues

Zhong Yi Gu*, Lei Fu

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract

Objective: To synthesize the anticancer agent combretastatin A-4 and its water-soluble analogues. Methods: 3,4,5-Trimethoxyphenylacetic acid and isovanilline were used as starting materials to prepare combretastatin A-4 and its water-soluble analogues via condensation, modification with mPEG side chain, and de-carboxylation reactions. Results: The structures of target compounds were confirmed by 1H NMR, 13C NMR, MS and melting point; the overall yields were about 40%. Conclusion: The synthetic routes developed herein require simple reaction conditions and few steps, and yield high stereoselectivity of cis conformation, which are suitable for large-scale manufacturing.

Original languageEnglish
Pages (from-to)1322-1325
Number of pages4
JournalChinese Journal of New Drugs
Volume17
Issue number15
Publication statusPublished - 2008
Externally publishedYes

Keywords

  • Anticancer
  • Combretastatin A-4
  • Synthesis
  • Water-soluble analogues

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