Radical-Mediated Cascade Spirocyclization of N-Benzylacrylamides with Polyhaloalkanes: Access to Polyhalo-Substituted Azaspirocyclohexadienones

J Org Chem. 2022 Mar 4;87(5):2740-2747. doi: 10.1021/acs.joc.1c02664. Epub 2022 Jan 28.

Abstract

A novel and mild metal-free catalyzed radical-mediated cascade spirocyclization of N-benzylacrylamides with polyhaloalkanes is proposed for the preparation of polyhalo-substituted azaspirocyclohexadienones. Notably, polyhaloalkanes are employed as efficient alkyl radical sources via the cleavage of C(sp3)-H bonds. This protocol undergoes a cascade radical addition and intramolecular cyclization/dearomatization process, and enables the easy construction of multiple chemical bonds and a spiro ring in a single reaction.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cyclization
  • Free Radicals
  • Spiro Compounds* / chemistry

Substances

  • Free Radicals
  • Spiro Compounds