Abstract
AbstractHerein, we report a polar‐radical relay strategy for α‐C−H amination of cyclic amines with N‐chloro‐N‐sodio‐carbamates. The relay is initiated by in situ generation of cyclic iminium intermediate using N‐iodosuccinimide (NIS) oxidant as an initiator, which then operates through a series of polar (addition and elimination) and radical (homolysis, hydrogen‐ and halogen atom transfer) reactions to enable the challenging C−N bond formation in a controlled manner. A broad range of α‐amino cyclic amines were readily accessed with excellent regioselectivity, and the superb applicability was further demonstrated by functionalization of biologically relevant compounds.
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