铜/钯催化炔烃的硼氟烯基化反应合成硼取代的单氟烯烃。
Cu/Pd-Catalyzed Borylfluoroallylation of Alkynes for the Synthesis of Boryl-Substituted Monofluoroalkenes.
机构信息
Hefei National Laboratory for Physical Sciences at the Microscale, CAS Key Laboratory of Urban Pollutant Conversion, Anhui Province Key Laboratory of Biomass Clean Energy, Center for Excellence in Molecular Synthesis of CAS, University of Science and Technology of China, Hefei 230026, China.
Institute of Energy, Hefei Comprehensive National Science Center, Hefei 230031, China.
出版信息
Org Lett. 2021 May 7;23(9):3259-3263. doi: 10.1021/acs.orglett.1c00668. Epub 2021 Apr 19.
Monofluoroalkenes normally act as metabolically stable bioisosteres for amide groups (-NH-CO-) and have widespread applications in drug discovery. Additionally, they are widely used as building blocks in organic synthesis. In this study, the Cu/Pd-catalyzed borylfluoroallylation of alkynes was achieved, providing a modular and general tactic for the preparation of monofluorinated alkene scaffolds with high regioselectivity and stereoselectivity. Moreover, an array of synthetic building blocks can be generated by downstream transformations.
单氟烯烃通常作为酰胺基团 (-NH-CO-) 的代谢稳定的生物等排体，在药物发现中具有广泛的应用。此外，它们还广泛用作有机合成中的构建块。在这项研究中，实现了炔烃的 Cu/Pd 催化硼氟烯丙基化反应，为高区域选择性和立体选择性地制备单氟烯烃骨架提供了一种模块化和通用的策略。此外，通过下游转化可以生成一系列合成构建块。
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