Metal free, one‐pot oxidative triple functionalization of azaarenes with methyl arenes mediated by molecular iodine/TBHP: Synthesis of N‐benzylated iodo(iso)quinolinones.

An efficient metal-free one-pot triple functionalization of azaarenes has been developed via a successive regioselective iodination, N-benzylation and amidation by using readily available methylarenes in presence of molecular iodine and TBHP. This method avoids the use of expensive noble metal catalysts and multi-step conversions. Moreover, we have shown the synthetic utility of the iodo functionality with traditional cross-coupling reactions (like Suzuki, Heck and Sonogashira) and the corresponding products were obtained in good yields.