4.8 Article

Room-temperature copper-catalyzed α-arylation of malonates

Journal

ORGANIC LETTERS
Volume 9, Issue 17, Pages 3469-3472

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol701473p

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An effective method in targeting alpha-aryl malonates is reported. In the presence of a catalytic amount of 2-picolinic acid and CuI, the coupling of aryl iodides with diethyl malonate proceeds smoothly even at room temperature. The high levels of functional group compatibility and exceptionally mild reaction conditions offer this an attractive protocol in accessing a variety of arylated malonates.

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