Liu Jianchang, Zhang Jida, Wu Chaolin, Liu Hefu, Liu Hui, Sun Fenggang, Li Yueyun, Liu Yuying, Dong Yunhui, Li Xinjin
College of Chemistry and Chemical Engineering, Shandong University of Technology 266 West Xincun Road Zibo 255000 China
Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences 345 Lingling Road Shanghai 200032 China.
RSC Adv. 2019 Sep 9;9(49):28409-28413. doi: 10.1039/c9ra06406k.
1,1-Difluoroethylated aromatics are of great importance in medicinal chemistry and related fields. 1,1-Difluoroethyl chloride (CHCFCl), a cheap and abundant industrial raw material, is viewed as an ideal 1,1-difluoroethylating reagent, but the direct introduction of the difluoroethyl (CFCH) group onto aromatic rings using CHCFCl has not been successfully accomplished. Herein, we disclose a nickel-catalyzed 1,1-difluoroethylation of arylboronic acids with CHCFCl for the synthesis of (1,1-difluoroethyl)arenes.
1,1-二氟乙基化芳烃在药物化学及相关领域具有重要意义。1,1-二氟氯乙烷（CHCFCl）是一种廉价且丰富的工业原料，被视为理想的1,1-二氟乙基化试剂，但使用CHCFCl将二氟乙基（CFCH）基团直接引入芳环尚未成功实现。在此，我们报道了一种镍催化的芳基硼酸与CHCFCl的1,1-二氟乙基化反应，用于合成（1,1-二氟乙基）芳烃。
