Metal-Free [3+2] Annulation of Ynamides with Anthranils to Construct 2-Aminoindoles

Org Lett. 2021 Mar 19;23(6):2029-2035. doi: 10.1021/acs.orglett.1c00158. Epub 2021 Mar 1.

Abstract

A novel metal-free [3+2] annulation of ynamides with anthranils provides a facile, flexible, environmentally friendly, and atom-economical route to 2-aminoindoles. This synthetic process proceeds with efficiency, excellent regioselectivity, and wide functional group tolerance under mild conditions. Moreover, the obtained 2-aminoindole products represent a multifunctional platform for the construction of various 2-aminoindolyl frameworks.