Synthesis of N-Substituted Indole-3-carboxylic Acid Derivatives via Cu(I)-Catalyzed Intramolecular Amination of Aryl Bromides

A variety of N-alkylated and N-arylated derivatives of methyl 1 H-indole-3-carboxylate were synthesized efficiently via Ullmann-type intramolecular arylamination, using the CuI-K 3PO 4-DMF system. This catalytic amination procedure can be performed with good to high yields under mild conditions under an air atmosphere.