Synthesis of 1 H-Pyrrol-3(2 H)-ones via Three-Component Reactions of 2,3-Diketo Esters, Amines, and Ketones

J Org Chem. 2018 Sep 21;83(18):11288-11297. doi: 10.1021/acs.joc.8b01887. Epub 2018 Aug 31.

Abstract

An efficient one-pot, three-component reaction of 2,3-diketo esters with amines and ketones has been developed for the synthesis of 1 H-pyrrol-3(2 H)-ones. By using trifluoroacetic acid (TFA) as the additive and acetonitrile (MeCN) as the solvent, this convenient method provides a library of 1 H-pyrrol-3(2 H)-ones in moderate to good yields. The simple protocol features readily available starting materials, a straightforward process, good functional group tolerance, and broad substrate scope.

Publication types

  • Research Support, Non-U.S. Gov't