Assembly of isoquinolines via CuI-catalyzed coupling of β-keto esters and 2-halobenzylamines

CuI-catalyzed coupling of 2-halobenzylamines with beta-keto esters or 1,3-diketones in i-PrOH under the action of K2CO3 produced 1,2-dihydroisoquinolines as the coupling/condensative cyclization products, which underwent smooth dehydrogenation under air atmosphere to afford substituted isoquinolines.