CuBr-Catalyzed Aerobic Decarboxylative Cycloaddition for the Synthesis of Indolizines under Solvent-Free Conditions

J Org Chem. 2017 Mar 17;82(6):2835-2842. doi: 10.1021/acs.joc.6b02455. Epub 2017 Feb 28.

Abstract

An efficient synthesis of diversified indolizine derivatives was developed via CuBr-catalyzed reaction of pyridines, methyl ketones and alkenoic acids under solvent-free conditions in oxygen atmosphere. This synthesis involves cascade processes of copper-catalyzed bromination of the methyl ketone, 1,3-dipolar cycloaddition of the pyridinium ylide with the alkenoic acid, followed by oxidative decarboxylation and dehydrogenative aromatization of the primary cycloadduct. By this protocol, a wide range of indoliznes with different substitution patterns were selectively prepared in one pot from simple substrates in good to excellent yields.

Publication types

  • Research Support, Non-U.S. Gov't