A kind of preparation method of fully substituted pyrazole containing sulfone group

A technology of fully substituted pyrazoles, which is applied in the field of preparation of fully substituted pyrazoles, can solve problems such as limited applications and complex starting material synthesis operations, and achieve the effects of reduced production costs, wide application range, and safe reactions
CN103980201BInactive Publication Date: 2016-02-10南京凯莫森医药科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
南京凯莫森医药科技有限公司
Publication Date
2016-02-10
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a preparation method of fully substituted pyrazoles containing sulfone groups, comprising the following steps: taking 1,3-diketone and aromatic sulfonyl hydrazide as reaction substrates, using iodide as catalyst, and tert-butanol peroxide as an oxidizing agent, cobalt acetate tetrahydrate or anhydrous cobalt chloride as an additive, ethyl acetate or benzene as a solvent, and a fully substituted pyrazole containing a sulfone group is prepared through condensation reaction. The preparation method disclosed in the invention can achieve good or even excellent yields for various arylsulfonylhydrazides and 1,3-diketones, etc., and the yield can reach up to 97%; the functional group compatibility of the substrate is high, compared with the traditional The method has a wide range of substrates; and the preparation process is controllable, which is suitable for industrial production of fully substituted pyrazoles containing sulfone groups.
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Description

technical field

[0001] The invention relates to a method for preparing pyrazole compounds, in particular to a method for preparing fully substituted pyrazoles containing sulfone groups. Background technique

[0002] Pyrazole is a five-membered heterocyclic aromatic compound containing two adjacent nitrogen atoms. The first synthetic pyrazole compound was in 1883. L. Knott synthesized 1-phenyl-3- from ethyl acetoacetate and phenylhydrazine Methyl pyrazolone, named after "pyrazole". Because of high efficiency, low toxicity and multi-directional transformation of substituents on the pyrazole ring, fully substituted pyrazoles have become a very important class of organic compounds, which are widely used in biology, medicine, pesticides, materials, etc.

[0003] The traditional methods for synthesizing fully substituted pyrazoles mainly include the following three methods: 1. Condensation cyclization of monosubstituted hydrazine and substituted 1,3-bis-electrophiles, and this me...

Claims

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