Shanghai Key Laboratory of Chemical Biology School of Pharmacy, East China University of Science and Technology (ECUST), Shanghai, 200237, P. R. China.
Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry Chinese Academy of Sciences, Shanghai, 200032, P. R. China.
Chem Asian J. 2023 May 16;18(10):e202300144. doi: 10.1002/asia.202300144. Epub 2023 Apr 21.
A novel and facile method for the synthesis of N-β-CF -substituted 2-pyridones via hydroamination of α-(trifluoromethyl)styrenes with 2-pyridones was described. The reaction proceeded smoothly at room temperature, affording a variety of N-(β-trifluoromethyl-β-arylethyl)pyridin-2(1H)-ones in moderate to good yields with excellent N-regioselectivity.
描述了一种通过α-(三氟甲基)苯乙烯与 2-吡啶酮的氨化反应合成 N-β-CF3-取代 2-吡啶酮的新颖、简便方法。该反应在室温下顺利进行,以中等至良好的收率得到了各种 N-(β-三氟甲基-β-芳基乙基)吡啶-2(1H)-酮,具有优异的 N-区域选择性。