Synthesis of 14-azacamptothecin, a water-soluble topoisomerase I poison

Nicolas J. Rahier, Kejun Cheng, Rong Gao, Brian M. Eisenhauer, Sidney M. Hecht

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35 Scopus citations

Abstract

(Chemical Equation Presented) 14-Azacamptothecin, a potent, water-soluble analogue of the antitumor agent camptothecin, has been prepared by a convergent synthesis. The key condensation of the AB and DE rings with concomitant formation of ring C of 14-aza CPT was carried out in two stages, the latter of which involved a radical cyclization strategy.

Original languageEnglish (US)
Pages (from-to)835-837
Number of pages3
JournalOrganic Letters
Volume7
Issue number5
DOIs
StatePublished - Mar 3 2005

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ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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