Iodine-Catalyzed Oxidative Benzylic C-H Bond Amination of Azaarenes: Practical Synthesis of Quinazolin-4(3H)-ones

Abstract

An efficient iodine-catalyzed oxidative benzylic C-H bond amination of azaarenes to afford 2-heteroaryl quinazolinones has been developed. This reaction utilizes unfunctionalized alkyl azaarenes as starting materials and proceeds under metal-free conditions with dioxygen as the terminal oxidant, thus is much "greener" than the previous synthetic methods.