A Facile method to transform trans-4-carboxy-3,4-dihydro-3-phenyl- 1(2H)-isoquinolones to indeno[1,2-c]isoquinolines

J Org Chem. 2005 Aug 5;70(16):6496-8. doi: 10.1021/jo050831t.

Abstract

The indeno[1,2-c]isoquinolines are an important class of topoisomerase I inhibitors with anticancer activity. The condensation of Schiff bases with homophthalic anhydrides provides a mixture of cis- and trans-4-carboxy-3,4-dihydro-3-phenyl-1(2H)isoquinolones. Although the cis products can be readily converted to indeno[1,2-c]isoquinolines with thionyl chloride, the trans products do not afford indeno[1,2-c]isoquinolines using this method. The present report describes a route for conversion of the trans diastereomers to indeno[1,2-c]isoquinolines using selenoxide elimination and Friedel-Crafts cyclization chemistry.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Cyclization
  • Hydrogen / chemistry
  • Indenes / chemistry*
  • Isoquinolines / chemistry*
  • Stereoisomerism
  • Sulfur Oxides / chemistry

Substances

  • Indenes
  • Isoquinolines
  • Sulfur Oxides
  • thionyl chloride
  • Hydrogen