Harnessing the reactivity of ortho-formyl-arylketones: base-promoted regiospecific synthesis of functionalized isoquinolines

Abstract

An efficient and base-mediated one-pot regiospecific synthesis of structurally diversified isoquinolines and benzo[h] isoquinolines from easily accessible ortho-formyl-arylketones and aryl/(het)arylmethanamines has been described. Challenging 3-alkynyl/alkenyl isoquinolines and bis-isoquinolines were easily attained through this developed chemistry, which can be further used for various organic transformations. Operational simplicity, high atom-economy, broad substrate scope, functional group tolerance and applicability towards large scale synthesis are the advantageous features of this developed methodology.