Highly regio- and enantioselective synthesis of polysubstituted 2H-pyrroles via Pd-catalyzed intermolecular asymmetric allylic dearomatization of pyrroles.

Abstract

A highly efficient synthesis of chiral polysubstituted 2H-pyrrole derivatives via a Pd-catalyzed intermolecular asymmetric allylic dearomatization reaction of pyrroles is presented. With the commercially available palladium precursor and chiral ligand, the polysubstituted 2H-pyrrole products containing a chiral quaternary carbon center were obtained with up to 97% ee and >95/5 regioselectivity.