Organic Letters 2007-08-16

Room-temperature copper-catalyzed alpha-arylation of malonates.

Sau Fan Yip, Hong Yee Cheung, Zhongyuan Zhou, Fuk Yee Kwong

Index: Org. Lett. 9(17) , 3469-72, (2007)

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Abstract

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.