Rearrangement of Benzylic Trichloroacetimidates to Benzylic Trichloroacetamides

J Org Chem. 2017 Apr 7;82(7):3982-3989. doi: 10.1021/acs.joc.7b00245. Epub 2017 Mar 27.

Abstract

The rearrangement of allylic trichloroacetimidates is a well-known transformation, but the corresponding rearrangement of benzylic trichloroacetimidates has not been explored as a method for the synthesis of benzylic amines. Conditions that provide the trichloroacetamide product from a benzylic trichloroacetimidate in high yield have been developed. Methods were also investigated to transform the trichloroacetamide product directly into the corresponding amine, carbamate, and urea. A cationic mechanism for the rearrangement is implicated by the available data.

Publication types

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

MeSH terms

  • Acetamides / chemistry*
  • Chloroacetates / chemistry*
  • Magnetic Resonance Spectroscopy / methods

Substances

  • Acetamides
  • Chloroacetates
  • trichloroacetamide