A general, simple and green process to access pyrrolo[2,1-a]isoquinolines using a KI/TBHP catalytic system

A novel KI/TBHP-catalyzed 1,3-dipolar cycloaddition/oxidation/aromatization cascade reaction provided general, efficient and green access to biologically important pyrrolo[2,1-a]isoquinolines. The product pyrrolo[2,1-a]isoquinolines were obtained from reactions between simple, readily available dipolarophiles and tetrahydroisoquinolines in moderate to excellent yields The reaction was environmentally benign in the adoption of nontoxic KI as a catalyst and IOH was generated in situ from the oxidation reaction of KI and TBHP.