Efficient Copper-Catalyzed Synthesis of N-Alkylanthranilic Acids via an ortho-Substituent Effect of the Carboxyl Group of 2-Halobenzoic Acids at Room Temperature

摘要

We have developed an efficient Copper-catalyzed method for the Synthesis of N-alkylanthranilic acids. The protocol uses inexpensive copper(l) iodide/racemic 1,1'-binaphthyl-2,2'-diol (rac-BINOL) as the catalyst/ligand system, readily available 2-halobenzoic acids and aliphatic amines as the starting materials, the Coupling reactions were performed at room temperature, and Various functionalities in the Substrates were tolerated.