公开(公告)号：US11072589B2

公开(公告)日：2021-07-27

申请号：US17067721

申请日：2020-10-11

Applicant: SOOCHOW UNIVERSITY

Inventor： Haiyan Li ,  Huihuang Li ,  Yaxiong Wang ,  Xiaobing Wan

IPC: C07D249/10 ,  B01J23/72

Abstract: 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.