Dearomatizing Amination Reactions

Abstract

Dearomatization reactions allow the direct synthesis of structurally complex sp3-rich molecules from readily available “flat” precursors. Established dearomatization processes commonly involve the formation of new C−C bonds, whereas methods that enable the introduction of C−N bonds have received less attention. Because of the privileged position of nitrogen in drug discovery, significant recent methodological efforts have been directed towards addressing this deficiency. Consequently, a variety of new processes are now available that allow the direct preparation of sp3-rich amino-containing building blocks and scaffolds. This review gives an overview of C−N bond forming dearomatization reactions, particularly with respect to scaffold assembly processes. The discussion gives historical context, but the main focus is on selected methods that have been reported recently.