Synthesis of Biologically Active Indenoisoquinoline Derivatives via a One-Pot Copper(II)-Catalyzed Tandem Reaction

Chia Yu Huang, Veerababurao Kavala, Chun Wei Kuo, Ashok Konala, Tang Hao Yang, Ching Fa Yao

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A concise route for the synthesis of indenoisoquinoline derivatives from 2-iodobenzamide and 1,3-indanedione derivatives in the presence of copper(II) chloride and cesium carbonate in acetonitrile solvent is reported. A wide variety of 2-iodobenzamide derivatives and indandiones could be used to synthesize indenoisoquinoline derivatives and other fused indenoisoquinoline in moderate to good yields. This methodology was adapted for the one-step synthesis of a series of clinically active topoisomerase I inhibitors such as NSC 314622, LMP-400, LMP-776.

Original languageEnglish
Pages (from-to)1961-1968
Number of pages8
JournalJournal of Organic Chemistry
Issue number4
Publication statusPublished - 2017 Feb 17


ASJC Scopus subject areas

  • Organic Chemistry

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