Pd-catalyzed ortho-arylation of 3,4-dihydroisoquinolones via C–H bond activation: synthesis of 8-aryl-1,2,3,4-tetrahydroisoquinolines

Abstract An efficient route to synthesize biologically interesting 8-aryl-1,2,3,4-tetrahydroisoquinoline has been developed. It involves the Pd-catalyzed direct arylation of 3,4-dihydroisoquinolones via C–H bond activation with aryl iodides to afford a variety of 8-arylated cross-coupling products, which are subsequently reduced to 8-aryl-1,2,3,4-tetrahydroisoquinolines in good to excellent yields.