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

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

Research output: Contribution to journalArticlepeer-review

39 Scopus citations


(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
Issue number5
StatePublished - Mar 3 2005
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry


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