biostudies-literatureUnknown9(1)Yuan CTransition-metal-catalyzed direct site-selective functionalization of arene C-H bonds has emerged as an innovative approach for building the core structure of pharmaceutical agents and other versatile complex compounds. However, para-selective C-H functionalization has seldom been explored, only a few examples, such as steric-hindered arenes, electron-rich arenes, and substrates with a directing group, have been reported to date. Here we describe the development of a ruthenium-enabled para-selective C-H difluoromethylation of anilides, indolines, and tetrahydroquinolines. This reaction tolerates various substituted arenes, affording para-difluoromethylation products in moderate to good yields. Results of a preliminary study of the mechanism indicate that chelation-assisted cycloruthenationNature communications1189https://www.ebi.ac.uk/biostudies/studies/S-EPMC5864885biostudies-literatureRuthenium(II)-enabled para-selective C-H difluoromethylation of anilides and their derivatives.PMC5864885Yuan CYang YZhu LChen XChen CLan YZhao YfalseRuthenium(II)-enabled para-selective C-H difluoromethylation of anilides and their derivatives.Transition-metal-catalyzed direct site-selective functionalization of arene C-H bonds has emerged as an innovative approach for building the core structure of pharmaceutical agents and other versatile complex compounds. However, para-selective C-H functionalization has seldom been explored, only a few examples, such as steric-hindered arenes, electron-rich arenes, and substrates with a directing group, have been reported to date. Here we describe the development of a ruthenium-enabled para-selective C-H difluoromethylation of anilides, indolines, and tetrahydroquinolines. This reaction tolerates various substituted arenes, affording para-difluoromethylation products in moderate to good yields. Results of a preliminary study of the mechanism indicate that chelation-assisted cycloruthenation2018-01-01T00:00:00Z2018 Mar2025-04-04T12:55:40.691Z2019-03-26T23:20:42ZS-EPMC58648852956795310.1038/s41467-018-03341-6