Abstract

Indole benzylic stereocenters are molecular frameworks largely present in natural occurring compounds, with their absolute configuration being of key importance in determining the biological activity of the entire molecule. In this context, the development of new catalytic asymmetric strategies for their preparation is a research area of astonishingly rapid growth by means of organic as well as organometallic catalysts. Here, an update of this thriving scenario is presented by focusing in highly stereocontrolled Michael addition approaches, addition to carbonyl units, direct aromatic C-H activation/alkylation, and allylic alkylation.

Keywords: Alkylation, asymmetric catalysis, Friedel-Crafts, indoles