The significance of amination of aryl halides has been
manifested by its wide applications in the synthesis of the
organically and medicinally interesting building blocks
containing the N-aryl moiety throughout pharmaceuticals,
agrochemicals, natural products, and materials.1 The stateof-
the-art in the area includes the copper-mediated Ullmann
coupling2 and the Buchwald-Hartwig reaction3 by utilizing
the palladium-catalyzed arylation of amines. Although these
methods are highly effective, there is still much room for
improvement, for example, these methods usually require
long reaction times and high reaction temperatures, and
moreover some of them suffer from a relatively narrow scope
of substrates. Microwave (MW)-assisted organic reactions
have been demonstrated as a powerful means in significantly
accelerating organic processes including aromatic nucleophilic
substitution reactions.4 Notably, Tu and Meciarova,
respectively, reported the construction of arylamines using
this technique.5 Our group also have achieved success by
using arylboronic acids and amines as the substrates.6
However, the described methods are only limited to electronrich
aliphatic amines or imidazole. The electron-deficient
nitrogen-containing aromatic heterocycles were found to be
less reactive or unreactive.7
Herein, we wish to report a novel MW-assisted protocol
for the efficient amination of aryl halides with various amines
in the presence of Cu(OAc)2. Several distinguished features
of the process are deserved to be mentioned: (i) proceeding
faster and generally giving good to excellent yields, (ii) using
Cu(OAc)2 without requiring any other additives, and more
significantly, (iii) a much broader substrate scope: both
aromatic and aliphatic amines and various substituted aryl
halides can be applied.