Assembly of Isoquinolines via CuI-Catalyzed Coupling of β-Keto Esters and 2-Halobenzylamines

Abstract

CuI-catalyzed coupling of 2-halobenzylamines with beta-keto esters or 1,3-diketones in i-PrOH under the action of K(2)CO(3) produced 1,2-dihydroisoquinolines as the coupling/condensative cyclization products, which underwent smooth dehydrogenation under air atmosphere to afford substituted isoquinolines.