Copper-free Sonogashira reaction using 7-chloro camptothecins

Yu Luo, Heyong Gao, Yunfei Li, Weigang Huang, Wei Lu, Zhaoguo Zhang

Research output: Contribution to journalArticlepeer-review

29 Scopus citations

Abstract

We studied copper-free Sonogashira reaction using 7-chloro camptothecins, and determined that rac-BINAP/Pd(OAc)2 was an efficient catalyst for the coupling reaction. With this process, a number of 7-substituted camptothecins with a wide range of functional groups are potentially accessible. Besides, two drugs, SN-38 and BNP-1350, could be prepared by this method.

Original languageEnglish
Pages (from-to)2465-2470
Number of pages6
JournalTetrahedron
Volume62
Issue number11
DOIs
StatePublished - 13 Mar 2006

Keywords

  • Camptothecin
  • Catalysis
  • Palladium
  • Sonogashira coupling
  • Topoisomerase I

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