Abstract
A new method is presented for the synthesis of 2-aminoquinazolines, which is based
on a Chan–Evans–Lam coupling of (2-formylphenyl)boronic acids with guanidines. Relatively
mild conditions involving the use of inexpensive CuI as a catalyst and methanol as
a solvent permit the application of the method to a wide range of substrates. Nonsubstituted,
N-monosubstituted, and N,N-disubstituted guanidines can be used as reactants to give
the corresponding 2-aminoquinazolines in moderate yields from readily available (2-formylphenyl)boronic
acids.
Key words
guanidines - Chan–Evans–Lam coupling - quinazolines - copper catalysis - formylphenylboronic
acids