Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology; College of Pharmaceutical Sciences, Zhejiang University of Technology, Chao Wang Road 18th, 310014 Hangzhou, China.
Org Biomol Chem. 2021 Dec 1;19(46):10223-10227. doi: 10.1039/d1ob01754c.
A mild and simple method is reported for the construction of 3-difluoroarylmethylated coumarins using α,α-difluoroarylacetic acids as an easily handled difluoromethyl source in reaction with ester 3-arylpropiolates under the promotion of copper. The reaction involves a proposed radical-triggered domino decarboxylative aryldifluoromethylation/5- cyclization/ester migration process that directly forms Csp-CFAr and C-C bonds with good functional group tolerance.
报道了一种温和、简便的方法,使用α,α-二氟代苯乙酸作为易于处理的二氟甲基源,在铜的促进下与酯 3-芳基丙炔酸酯反应,构建 3-二氟甲基化香豆素。该反应涉及一个自由基引发的串联脱羧芳基二氟甲基化/5-环化/酯迁移过程,直接形成 Csp-CFAr 和 C-C 键,具有良好的官能团容忍度。