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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.

MATERIALS
Product Number
Brand
Product Description

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