Keerthika K, S Bazil Muhammed, Geetharani K
Department of Inorganic and Physical Chemistry, Indian Institute of Science, Bangalore 560012, India.
J Org Chem. 2024 Aug 16;89(16):11480-11486. doi: 10.1021/acs.joc.4c01159. Epub 2024 Jul 26.
Herein, we report a protocol for the synthesis of α-trifluoromethylated ketones through trifluoromethylation of the corresponding catecholboron enolates of α,β-unsaturated ketones. The reaction of the 1,4-hydroborated product of enones with the Togni II reagent affords the α-trifluoromethylated ketones without any catalyst or additive. Moreover, the protocol has been employed on a series of α,β-unsaturated ketones, including chalcones, substrate-bearing heterocycles, and bioactive molecules. Mechanistic studies suggest the involvement of a trifluoromethyl radical during the reaction.
在此,我们报道了一种通过α,β-不饱和酮的相应邻苯二酚硼烯醇盐的三氟甲基化反应合成α-三氟甲基化酮的方法。烯酮的1,4-硼氢化产物与Togni II试剂反应,无需任何催化剂或添加剂即可得到α-三氟甲基化酮。此外,该方法已应用于一系列α,β-不饱和酮,包括查耳酮、含杂环底物和生物活性分子。机理研究表明反应过程中涉及三氟甲基自由基。