Thianthrenium salts to arynes: base promoted C‐N bond construction

Amine compounds are widely found in natural products, pharmaceuticals, and pesticides. We propose a base‐facilitated synthesis method of polysubstituted aromatic amines. A simple, rapid, plateau‐utilization, and highly regioselective non‐in‐situ amination reaction was achieved by using aryl thianthrenium salt as the aryne precursor, and the arylynyl distortion induced by the substituents. This method provides new possibilities for organic synthesis.