Iron-Catalyzed Intermolecular C-N Cross-Coupling Reactions via Radical Activation Mechanism

摘要

A concept for intermolecular C-Ncross-coupling aminationhas been discovered using tetrazoles and aromatic and aliphatic azideswith boronic acids under iron-catalyzed conditions. The aminationfollows an unprecedented metalloradical activation mechanism thatis different from traditional metal-catalyzed C-N cross-couplingreactions. The scope of the reaction has been demonstrated by theemployment of a large number of tetrazoles, azides, and boronic acids.Moreover, several late-stage aminations and a short synthesis of adrug candidate have been showcased for further synthetic utility.Collectively, this iron-catalyzed C-N cross-coupling shouldhave wide applications in the context of medicinal chemistry, drugdiscovery, and pharmaceutical industries.