Organic Letters 2002-01-24

A general and mild copper-catalyzed arylation of diethyl malonate.

Edward J Hennessy, Stephen L Buchwald

Index: Org. Lett. 4(2) , 269-72, (2002)

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Abstract

[reaction: see text] A general method for the synthesis of alpha-aryl malonates is described. The coupling of an aryl iodide and diethyl malonate in the presence of Cs(2)CO(3) and catalytic amounts of copper(I) iodide and 2-phenylphenol affords the alpha-aryl malonate in good to excellent yields. The mild reaction conditions and high levels of functional group compatibility make this an attractive synthetic alternative to previous methods.