室温下铜催化丙二酸酯的α-芳基化反应
Room-temperature copper-catalyzed alpha-arylation of malonates.
作者信息
Yip Sau Fan, Cheung Hong Yee, Zhou Zhongyuan, Kwong Fuk Yee
机构信息
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.
出版信息
Org Lett. 2007 Aug 16;9(17):3469-72. doi: 10.1021/ol701473p. Epub 2007 Jul 18.
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.
报道了一种靶向α-芳基丙二酸酯的有效方法。在催化量的2-吡啶甲酸和碘化亚铜存在下，芳基碘化物与丙二酸二乙酯的偶联反应即使在室温下也能顺利进行。高度的官能团兼容性和异常温和的反应条件使其成为制备各种芳基化丙二酸酯的有吸引力的方法。
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