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Merck

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

Organic letters (2002-02-14)
Edward J Hennessy, Stephen L Buchwald
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.

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Sigma-Aldrich
Diethyl malonate, ReagentPlus®, 99%
Sigma-Aldrich
Diethylmalonic acid, 98%