Iodine-catalyzed 1,3-dipolar cycloaddition/oxidation/aromatization cascade with hydrogen peroxide as the terminal oxidant: general route to pyrrolo[2,1-a]isoquinolines

J Org Chem. 2014 Feb 7;79(3):1084-92. doi: 10.1021/jo402540j. Epub 2014 Jan 10.

Abstract

We report a novel molecular iodine-catalyzed 1,3-dipolar cycloaddition/oxidation/aromatization cascade process with hydrogen peroxide as the terminal oxidant for the construction of 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 without the need for a metal catalyst.