Palladium-Catalyzed C2-Regioselective Perfluoroalkylation of the Free (NH)-Heteroarenes
作者:Hong Qin、Jie Zhang、Kai Qiao、Dong Zhang、Wei He、Chengkou Liu、Zheng Fang、Kai Guo
DOI:10.1021/acs.joc.0c02782
日期:2021.2.5
A highly regioselective and atom-efficient strategy for the construction of fused free (NH) heteroarenes through a palladium-catalyzed perfluoroalkyl insertion reaction has been accomplished. This protocol employed multiple iodofluoroalkanes as practical and available perfluoroalkyl sources to provide an operationally simple and versatile route for the synthesis of perfluoroalkylated indoles. Moreover
已经实现了通过钯催化的全氟烷基插入反应构建稠合的游离(NH)杂芳烃的高度区域选择性和原子效率高的策略。该方案采用多种碘氟烷烃作为实用和可用的全氟烷基来源,为合成全氟烷基化的吲哚提供了操作上简单而通用的途径。此外,没有指导小组协助的吲哚被用作底物,实现了吲哚的C(sp 2)–H位点选择性官能化,收率高达95%。此外,该协议还用于生物活性化合物(如植物生长素,色氨酸和褪黑激素类似物)的后期C2全氟烷基化。