A concept for intermolecular C–N
cross-coupling amination
has been discovered using tetrazoles and aromatic and aliphatic azides
with boronic acids under iron-catalyzed conditions. The amination
follows an unprecedented metalloradical activation mechanism that
is different from traditional metal-catalyzed C–N cross-coupling
reactions. The scope of the reaction has been demonstrated by the
employment of a large number of tetrazoles, azides, and boronic acids.
Moreover, several late-stage aminations and a short synthesis of a
drug candidate have been showcased for further synthetic utility.
Collectively, this iron-catalyzed C–N cross-coupling should
have wide applications in the context of medicinal chemistry, drug
discovery, and pharmaceutical industries.