Tactico derivatives and their preparation methods

Abstract

The invention discloses a triazole derivative and a preparation method thereof. According to the preparation method, aryl diazonium fluoroborate, a diazoester derivative and organic nitrile are takenas reaction substrates, transition metal is taken as a catalyst, inorganic alkali is taken as an additive, and the triazole derivative is prepared by virtue of cyclization reaction. The preparation method has the characteristics that the reaction is relatively economical, the substrates are relatively wide in universality, the later-period functionalization is relatively easily realized, reactionconditions are mild, the reaction can be carried out in air, the dose of a catalyst is low, the post-treatment is simple and convenient, and the purification and industrial utilization of a product are promoted; and meanwhile, the raw materials including reactants and catalysts adopted in the preparation method are cheap and easily available, the reaction constitution is reasonable, a ligand is not required, reaction steps are few, the relatively high yield can be realized only through one-step reaction, and the preparation method is accordant with the requirements and directions of current environment-friendly chemistry and pharmaceutical chemistry and is suitable for screening high-activity triazole derivative drugs.

Description

technical field [0001] The invention relates to a triazole derivative and a preparation method thereof, belonging to the technical field of organic synthesis. Background technique [0002] Triazole derivatives, as a very valuable five-membered nitrogen-containing heterocyclic skeleton, widely exist in many functional molecules and are used in organic catalysis, material science and other fields. In addition, the triazole derivative skeleton also appears in many biologically active molecules, and has important uses in the pharmaceutical industry and pesticides. At present, the method for preparing triazole derivatives has the disadvantages of many reaction steps, complicated preparation of raw materials, complicated reaction conditions, and narrow substrate scope. For example: [0003] (1) Michael J. Stocks and others reported the preparation of triazole derivatives from primary amines, amide diacetal derivatives, and hydrazide derivatives, but multi-step reactions are requ...

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Problems solved by technology

[0003] (1) Michael J. Stocks and others reported the preparation of triazole derivatives from primary amines, amide diacetal derivatives, and hydrazide derivatives, but multi-step reactions are required and the scope of reaction substrates is narrow (see: Michael J. Stocks ; Org. Lett. 2004, 6 , 2969);

[0004] (2) Hideko Nagasawa et al. reported the preparation of triazole derivatives from amidine hydrochloride derivatives and organic nitriles, but the reaction temperature was high and the substrate range was narrow (see: Hideko Nagasawa; J. Am. Chem. Soc. 2009, 131 ,15080);

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