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

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.