Enantioselective Annulation Reactions Enabled by Chiral Lithium Amides as Traceless Auxiliaries

Functionalized multimembered carbocyclic compounds are synthetically challenging scaffolds found in numerous pharmaceuticals and natural products. Herein, we describe a stereoselective and operationally straightforward method to form such carbocyclic compounds via a Michael addition-cyclization cascade. This method is effective in forming three or more contiguous stereocenters with high enantio- and diastereocontrol directly from α-substituted arylacetic acids with chiral lithium amides (CLAs) as traceless stereodirecting auxiliaries.