Organocatalytic Approach to Benzofused Nitrogen‐Containing Heterocycles: Enantioselective Total Synthesis of (+)‐Angustureine

Simply selective: The organocatalytic intramolecular aza-Michael reaction (IMAMR) was employed as an enantioselective tool to generate enantiomerically enriched isoindolines, indolines, tetrahydroquinolines, and tetrahydroisoquinolines from o-substituted alkylidenes, anilines and benzylamines (see scheme). The methodology was applied to the synthesis of the natural product (+)-Angustureine.