Mechanistic Pathways in Amide Activation: Flexible Synthesis of Oxazoles and Imidazoles

Org Lett. 2017 Jul 21;19(14):3815-3818. doi: 10.1021/acs.orglett.7b01678. Epub 2017 Jul 13.

Abstract

The preparation of substituted aminooxazoles and aminoimidazoles from α-arylamides and α-aminoamides through triflic anhydride-mediated amide activation is reported. These reactions proceed via the intermediacy of nitrilium adducts and feature N-oxide-promoted umpolung of the α-position of amides as well as a mechanistically intriguing sequence that results in sulfonyl migration from nitrogen to carbon. Quantum-chemical mechanistic analysis sheds light on the intricacies of the process.

Publication types

  • Research Support, Non-U.S. Gov't