Iron-Catalyzed Direct α-C(sp3)–H Arylamination of Glycine Derivatives with (Hetero)arylamines

Abstract An iron-catalyzed direct α-C(sp3)–H arylamination of glycine derivatives with (hetero)arylamines has been developed, providing a straightforward approach to the unnatural basic amino acids. This protocol is characterized by mild conditions and good functional group compatibility as well as atom-economy. Preliminary mechanistic studies suggested that the reaction involves radical processes and the imine was the key intermediate. Furthermore, the formation of a Fe-complex between iron salts and (hetero)arylamines is crucial for the progression of the reaction.