Lossen rearrangement by Rh(iii)-catalyzed C–H activation/annulation of aryl hydroxamates with alkynes: access to quinolone-containing amino acid derivatives

Abstract

A convenient and robust method for the preparation of new CF₃-containing 2-quinolones has been developed via a Rh(III)-catalyzed C–H activation/Lossen rearrangement/annulation cascade of N-pivaloyloxy-arylamides with internal alkynes bearing an α-CF₃-α-amino acid moiety on the triple bond. This work expands the scope of valuable products that are available through C–H activation/annulation reactions of arylamides in organic synthesis.