Recent developments in the organocatalytic asymmetric cycloaddition/annulation reactions involving indolylmethanols

Abstract

Enantioenriched indole frameworks constitute the structural core of a wide array of biologically active natural products and therapeutic agents; as such, their synthesis has emerged as a central and enduring objective in organic synthesis. In this regard, suitably substituted indolylmethanols have emerged as versatile precursors to a series of catalytic asymmetric transformations to construct complex indole-based architectures. This article provides a concise overview of the fundamental chemistry of n-indolylmethanols, with a specific emphasis on their role as key substrates in enantioselective cycloadditions catalyzed by chiral phosphoric acids.