I2-Catalyzed Oxidative Synthesis of N,4-Disubstituted Quinazolines and Quinazoline Oxides

An easy and efficient approach to the synthesis of N,4-disubstituted quinazoline-2-amine and oxides is described. This transformation proceeds smoothly in the presence of molecular iodine. The metal-free protocol presented here is insensitive to air moisture and operationally simple. This versatile and synthetic methodology is broadly applicable to a variety of N,4-disubstituted quinazoline-2-amines and oxides, which are synthesized in good to excellent yields starting from readily available inexpensive precursors.