Rapid Synthesis of Fused N‐Heterocycles by Transition‐Metal‐Free Electrophilic Amination of Arene CH Bonds

Abstract

We disclose an efficient and operationally simple protocol for the preparation of fused N-heterocycles starting from readily available 2-nitrobiaryls and PhMgBr under mild conditions. More than two dozen N-heterocycles, including two bioactive natural products, have been synthesized using this method. A stepwise electrophilic aromatic cyclization mechanism was proposed by DFT calculations.