L-Amino Acid Based Urea-Tertiary Amine-Catalyzed Chemoselective and Asymmetric Stereoablative Carboxylation of 3-Bromooxindoles with Malonic Acid Half Thioesters

J Org Chem. 2015 Dec 18;80(24):12686-96. doi: 10.1021/acs.joc.5b02286. Epub 2015 Nov 12.

Abstract

An L-amino acid based urea-tertiary amine-catalyzed enantioselective stereoablative carboxylation of 3-bromooxindoles with malonic acid half thioesters (MAHTs) and diverse commercially available carboxylic acids has been developed. A series of valuable 3-substituted 3-hydroxy-2-oxindoles were obtained in high enantioselectivities (up to 93% ee). This chemoselective reaction represents the first example of MAHTs as carboxylating agents.

Publication types

  • Research Support, Non-U.S. Gov't