Synthesis of Enantioenriched gem-Disubstituted 4-Imidazolidinones by Palladium-Catalyzed Decarboxylative Asymmetric Allylic Alkylation

Org Lett. 2021 Aug 20;23(16):6348-6351. doi: 10.1021/acs.orglett.1c02134. Epub 2021 Aug 4.

Abstract

A variety of enantioenriched gem-disubstituted 4-imidazolidinones were prepared in up to >99% yield and 95% ee by the Pd-catalyzed decarboxylative asymmetric allylic alkylation of imidazolidinone-derived β-amidoesters. In the process of preparing these substrates, a rapid synthetic route to 4-imidazolidinone derivatives was developed, beginning from 2-thiohydantoin. The orthogonality of the benzoyl imide and tert-butyl carbamate groups used to protect these nitrogen-rich products was demonstrated, enabling potential applications in drug design.

Publication types

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

MeSH terms

  • Alkylation
  • Catalysis
  • Imidazolidines / chemical synthesis*
  • Imidazolidines / chemistry
  • Molecular Structure
  • Palladium / chemistry*
  • Stereoisomerism

Substances

  • Imidazolidines
  • ethylene urea
  • Palladium