A ligand-free, copper-catalyzed cascade sequence to indole-2-carboxylic esters

SG Koenig, JW Dankwardt, Y Liu, H Zhao, SP Singh

Index: Koenig, Stefan G.; Dankwardt, John W.; Liu, Yanbing; Zhao, Hang; Singh, Surendra P. Tetrahedron Letters, 2010 , vol. 51, # 50 p. 6549 - 6551

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Citation Number: 17

Abstract

A variety of indole-2-carboxylic esters are accessible in yields up to 61% through a ligand- free, copper-catalyzed reaction of a series of commercially available 2-halo aryl aldehydes with benign glycine amidoesters, including the common reagent ethyl acetamidoacetate. This one-pot, three-reaction format allows ready entry to the desired heterocycles from starting substrates in the reactivity order of iodo> bromo⩾ chloro substituents. An ...