Construction of Atropisomeric 3-Arylindoles via Enantioselective Cacchi Reaction

Org Lett. 2021 Aug 6;23(15):5901-5905. doi: 10.1021/acs.orglett.1c02012. Epub 2021 Jul 8.

Abstract

The de novo construction of axially chiral 3-arylindoles bearing a C(3)-C(aryl) chiral axis has been realized by Pd-catalyzed enantioselective Cacchi reaction between aryl bromides and o-alkynylanilines. The reaction proceeded under mild conditions in high yields and excellent enantioselectivities.