Transition-metal-free synthesis of multisubstituted N-arylindoles via reaction of arynes and α-amino ketones

A simple transition-metal-free protocol for the synthesis of indoles has been developed using aryne cycloaddition. The in situ-generated arynes couple with α-amino ketones through a one-step N-arylation-nucleophilic addition process under mild conditions and efficiently produce multisubstituted N-arylindoles.

Graphical abstractDownload high-res image (184KB)Download full-size imageSynthesis of multisubstituted N-arylindoles via cycloaddition of arynes.