Zhang Min, Lin Jin-Hong, Xiao Ji-Chang
Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, 345 Lingling Road, Shanghai 200032, China.
Org Lett. 2021 Aug 6;23(15):6079-6083. doi: 10.1021/acs.orglett.1c02146. Epub 2021 Jul 23.
Trifluoromethyl substitution is notably popular in pharmaceuticals and agrochemicals; however, trifluoromethylated compounds normally rely on the use of cost-prohibitive or gaseous trifluoromethylating reagents, which diminishes the general applicability of these methods. Herein an efficient trifluoromethylation reagent trifluoromethylsulfonyl-pyridinium salt () was reported, which can be readily prepared from cheap and easily available bulk industrial feedstocks. can generate a trifluoromethyl radical under photocatalysis and realize the effective azido- or cyano-trifluoromethylation reactions of alkenes.
三氟甲基取代在药物和农用化学品中尤为常见;然而,三氟甲基化化合物通常依赖于使用成本高昂或气态的三氟甲基化试剂,这降低了这些方法的普遍适用性。在此报道了一种高效的三氟甲基化试剂三氟甲基磺酰基吡啶盐(),它可以很容易地从廉价且易于获得的大宗工业原料制备而成。该试剂在光催化下能产生三氟甲基自由基,并实现烯烃的有效叠氮基或氰基三氟甲基化反应。