ortho -Lithiation driven one-pot synthesis of quinazolines via [2 + 2 + 2] cascade annulation of halofluorobenzenes with nitriles.

A one-pot synthesis of 2,4-disubstituted quinazoline derivatives from halofluorobenzenes with nitriles was reported, via sequential nucleophilic addition and S N Ar reaction. The advantages of the present approach are transition metal free, easy to operate, and all the starting materials are commercially available.