773136-70-2Relevant academic research and scientific papers
Preparation method of 3, 4-dimethylpyrazole-5-formate compound
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Paragraph 0046-0052; 0069-0072, (2021/05/22)
The invention provides a preparation method of a 3, 4-dimethylpyrazole-5-formate compound. According to the method, 2-butanone and oxalic acid diester serve as raw materials, a 3-methyl acetylacetonate compound is prepared in a high-yield and high-regioselectivity mode under the catalysis of an organic annular secondary amine catalyst, the 3-methyl acetylacetonate compound reacts with hydrazine, and the 3, 4-dimethylpyrazole-5-formate compound is prepared in a high-yield mode. According to the preparation method, organic nitrogen-containing cyclic secondary amine compounds such as pyrroline, piperidine and morpholine are used as catalysts, and alcohols such as methanol and ethanol are used as solvents for reaction. The method has the characteristics of relatively mild reaction conditions, simplicity and convenience in operation, high regioselectivity, high yield and the like, and the synthesized 3, 4-dimethylpyrazole-5-formate compound can be used for preparing cyenopyrafen acaricides.
Synthesis, Acaricidal Activity, and Structure-Activity Relationships of Pyrazolyl Acrylonitrile Derivatives
Yu, Haibo,Cheng, Yan,Xu, Man,Song, Yuquan,Luo, Yanmei,Li, Bin
, p. 9586 - 9591 (2017/01/12)
A series of novel pyrazolyl acrylonitrile derivatives was designed, targeting Tetranychus cinnabarinus, and synthesized. Their structures were identified by combination of1H NMR,13C NMR, and MS spectra. The structures of compounds 18 and 19 were further confirmed by X-ray diffraction. Extensive greenhouse bioassays indicated that compound 19 exhibits excellent acaricidal activity against all developmental stages of T. cinnabarinus, which is better than the commercialized compounds cyenopyrafen and spirodiclofen. It was shown that the acute toxicity of compounds 19 to mammals is quite low. The structure-activity relationships are also discussed.
