Department of Chemistry, Tianjin Key Laboratory of Molecular Optoelectronic Sciences, Tianjin University, Collaborative, Innovation Center of Chemical Science and Engineering (Tianjin), Tianjin, 300072, P. R. of China.
Angew Chem Int Ed Engl. 2017 Apr 10;56(16):4569-4574. doi: 10.1002/anie.201700955. Epub 2017 Mar 22.
We disclose an efficient one-pot transformation of trifluorodiazoethane and higher perfluorinated homologues with various nitroolefins. This method takes advantage of the nitro group as a traceless activating and directing group (TADG) that is released in the aromatization step to produce 4-substituted 3-perfluoroalkyl pyrazoles with complete regioselectivity. The potential of this method is further demonstrated by the synthesis of penthiopyrad.
我们公开了一种高效的一锅转化方法，可将三氟重氮乙烷和各种硝基烯烃转化为高氟化同系物。该方法利用硝基作为无痕迹活化和导向基团（TADG），在芳构化步骤中释放出来，以完全区域选择性生成 4-取代的 3-全氟烷基吡唑。该方法的潜力通过戊噻菌隆的合进一步得到证明。
