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    1,2,4-triazole and preparation method therefor
    4.
    发明授权
    1,2,4-triazole and preparation method therefor 有权

    公开(公告)号：US11072589B2

    公开(公告)日：2021-07-27

    申请号：US17067721

    申请日：2020-10-11

    申请人： SOOCHOW UNIVERSITY

    发明人： Haiyan Li ,  Huihuang Li ,  Yaxiong Wang ,  Xiaobing Wan

    IPC分类号： C07D249/10 ,  B01J23/72

    摘要： A method for preparing 1,2,4-triazole includes using a fluoroborate aryl diazonium salt, a diazoester derivative and an organic nitrile as reaction substrates, a transition metal salt as a catalyst, and an inorganic base as an additive in a cyclization reaction. The method has the following characteristics: the reaction is economical; the substrate is universal; the post-functionalization is easy; the reaction conditions are mild; the reaction can be performed in air; the catalyst amount used is less; and the post-treatment is simple. Meanwhile, the raw materials, such as the reactants and the catalyst used, are inexpensive and easily available; the reaction composition is reasonable; no ligand is needed; there are less reaction steps; and only one step of reaction is required to obtain a high yield, meeting the requirements and directions of contemporary green chemistry and medicinal chemistry, being suitable for screening highly active 1,2,4-triazole drugs.

    Method for preparing 3-trifluoromethyl chalcones
    10.
    发明授权
    Method for preparing 3-trifluoromethyl chalcones 有权

    公开(公告)号：US10160731B2

    公开(公告)日：2018-12-25

    申请号：US15946601

    申请日：2018-04-05

    申请人： E.I. DU PONT DE NEMOURS AND COMPANY

    发明人： Gary David Annis

    IPC分类号： C07D261/04 ,  C07C17/35 ,  C07C45/45 ,  C07C45/70 ,  C07C49/80 ,  C07C49/813 ,  C07C67/343 ,  C07C205/45 ,  C07C209/74 ,  C07C231/12 ,  C07C235/84 ,  C07D213/40 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D249/08 ,  C07D249/10 ,  C07D277/28 ,  C07C25/13 ,  C07C231/14

    摘要： Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water. Also disclosed is a method for preparing a compound of Formula 2 comprising (1) forming a reaction mixture comprising a Grignard reagent derived from contacting a compound of Formula 5 wherein X is Cl, Br or I with magnesium metal or an alkylmagnesium halide in the presence of an ethereal solvent, and then (2) contacting the reaction mixture with a compound of Formula 6 wherein Y is OR11 or NR12R13, and R11, R12 and R13 are as defined in the disclosure. Further disclosed is a method for preparing a compound of Formula 7 wherein Q and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method disclosed above.