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 SNAr reaction. The advantages of the present approach are transition metal free, easy to operate, and all the starting materials are commercially available.

Automated summary

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