Synthesis of Indolo[1,2-b]isoquinoline Derivatives by Lewis Acid-Catalyzed Intramolecular Friedel-Crafts Alkylation Reaction

A methodology for the synthesis of indolo[1,2-b]isoquinoline derivatives by Lewis acid-catalyzed intramolecular Friedel-Crafts alkylation reaction has been developed. The reaction proceeds well with both secondary and primary 2-indolylmethanols. The method efficiently affords pharmaceutically important polycyclic fused indole derivatives in moderate to high yields with good functional group tolerance. In addition, the reaction proceeded in large scale indicating that this method could be scaled up for the synthesis of indolo[1,2-b] isoquinoline derivatives.