α‐Amination of 1,3‐Dicarbonyl Compounds and Analogous Reactive Enolate‐Precursors Using Ammonia under Oxidative Conditions

Abstract

Abstract We, herein, introduce a method for the direct α‐amination of different carbonyl compounds by employing aqueous ammonia as the N ‐source. Upon using NH 3 in combination with hypochlorites as simple oxidants under phase‐transfer catalytic conditions it is possible to carry out the direct α‐amination of reactive enolate‐precursors such as cyclic β‐ketoesters, oxindoles, as well as malonitriles and malonates with good to excellent yields, while simple ketone precursors being out of the scope thus far. Furthermore, a first proof‐of‐concept for an asymmetric variant by employing a chiral quaternary ammonium salt is reported.