Radical migration of substituents of aryl groups on quinazolinones derived from N-acyl cyanamides

J Am Chem Soc. 2010 Mar 31;132(12):4381-7. doi: 10.1021/ja910653k.

Abstract

A newly designed radical cascade involving N-acyl cyanamides is reported. It builds on aromatic homolytic substitutions as intermediate events and leads to complex heteroaromatic structures via an unprecedented radical migration of a substituent on aryl groups of quinazolinones (hydrogen or alkyl). Mechanistic considerations are detailed, which allowed us to devise fine control over the domino processes. The latter could be predictably stopped at several stages, depending on the reaction conditions. Finally, a surgical introduction of a trifluoromethyl substituent on a quinazolinone was achieved via the reported migration.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biological Products / chemical synthesis
  • Cyanamide / chemistry*
  • Free Radicals / chemistry*
  • Hydrocarbons, Aromatic / chemistry
  • Molecular Structure
  • Quinazolinones / chemistry*

Substances

  • Biological Products
  • Free Radicals
  • Hydrocarbons, Aromatic
  • Quinazolinones
  • Cyanamide