A General and Mild Copper-Catalyzed Arylation of Diethyl Malonate

Edward J. Hennessy and Stephen L. Buchwald*

*Department of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, Email: sbuchwalmit.edu

E. J. Hennessy, S. L. Buchwald, Org. Lett., 2002, 4, 269-272.

DOI: 10.1021/ol017038g (free Supporting Information)

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Abstract

The coupling of aryl iodides and diethyl malonate in the presence of Cs₂CO₃ and catalytic amounts of CuI and 2-phenylphenol gave α-aryl malonates in good to excellent yields. This mild method tolerates various functional groups.

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required bidentate binding

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Key Words

Copper-Catalysis, Malonic Acid Ester, Active Methylenes, Arenes

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ID: J54-Y2002-710