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Room-temperature copper-catalyzed alpha-arylation of malonates
Authors:Yip Sau Fan  Cheung Hong Yee  Zhou Zhongyuan  Kwong Fuk Yee
Institution:Open Laboratory of Chirotechnology of Institute of Molecular Technology for Drug Discovery and Synthesis, and Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Kowloon, Hong Kong.
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.
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