Radical aminomethylation of imines

J Org Chem. 2014 Sep 5;79(17):8128-33. doi: 10.1021/jo501332j. Epub 2014 Aug 21.

Abstract

Taking advantage of the high level of performance of N-alkoxycarbonyl-imines, we achieved the first example of addition of the aminomethyl radical to imine. The reaction efficiency depended on the structure of the radical precursor, whether it is an iodide or a xanthate, and an electron-withdrawing group on the nitrogen atom of the radical. This reaction allows direct introduction of an N-substituted aminomethyl group onto imine to provide 1,2-diamine as well as the short-step synthesis of ICI-199,441.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Diamines / chemical synthesis*
  • Diamines / chemistry
  • Ethylamines / chemistry*
  • Imines / chemistry*
  • Methylation
  • Molecular Structure
  • Stereoisomerism

Substances

  • Diamines
  • Ethylamines
  • Imines