Diastereoselective α‑Alkylation of Metallo Enamines Generated from N–C Axially Chiral Mebroqualone Derivatives

The reactions of various alkyl halides with the metallo enamines generated from racemic and optically pure N–C axially chiral mebroqualone derivatives were found to proceed with a synthetically attractive stereochemical outcome (up to 99% yield and up to dr = 26:1) allowing preparation of a structurally new type of pharmaceutically interesting compounds possessing elements of axial and central chirality