- Synthesis method of pyrazole disulfide
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The invention discloses a synthesis method of pyrazole disulfide, which is realized through the following steps: 1) dissolving a pyrazole ring, and dissolving a pyrazole ring raw material in butyl acetate; adding a pre-weighed reducing agent into the solu
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Paragraph 0024-0034
(2021/08/14)
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- Preparation method of 5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl) pyrazole disulfide
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The invention discloses a preparation method of 5-amino-3-cyano-1-(2, 6-dichloro-4-trifluoromethylphenyl)pyrazole disulphide, and belongs to the technical field of medicines. The preparation method comprises the steps of dissolving 5-amino-3-cyano-1-(2,6-
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Paragraph 0066-0090
(2021/07/24)
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- Substrate-Controlled [5+1] Annulation of 5-Amino-1H-phenylpyrazoles with Alkenes: Divergent Synthesis of Multisubstituted 4,5-Dihydropyrazolo[1,5-a]quinazolines
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A new and efficient [5+1] annulation reaction for the first synthesis of 5,5-disubstituted 4,5-dihydropyrazolo[1,5-a]quinazolines is described. This transition-metal-free tandem cyclization was performed with 5-amino-1H-phenylpyrazole and readily availabl
- Jiang, Xunyuan,Wei, Xiaoyi,Lin, Fei,Zhang, Zhixiang,Yao, Guangkai,Yang, Shuai,Zhao, Weijing,Zhao, Chen,Xu, Hanhong
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supporting information
p. 3997 - 4003
(2020/06/17)
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- Thioether-bridged arylalkyl-linked N-phenylpyrazole derivatives: Design, synthesis, insecticidal activities, structure-activity relationship and molecular-modeling studies
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Owing to thioether diverse physicochemical properties by non-covalent interactions with bio-macromolecules, thioether derivatives containing heterocyclic moiety are known for their interesting insecticidal bioactivities and attracting considerable attenti
- Fei, Chengcheng,Chen, Yanfei,Jiang, Zhiyan,Jiang, Dingxin
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supporting information
p. 1792 - 1796
(2018/04/19)
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- Design, synthesis and insecticidal activity of novel phenylpyrazoles containing a 2,2,2-trichloro-1-alkoxyethyl moiety
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A series of novel phenylpyrazoles containing a 2,2,2-trichloro-1- alkoxyethyl moiety were designed and synthesized via the key intermediate 5-trichloroethylideneimino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl) -4-alkylsulfenylpyrazole (5). The addition reaction of the imine 5 was closely related with the nature of the alcohol. The target compounds were confirmed by 1H NMR and elemental analysis. The results of bioassays indicated that the target compounds possessed excellent activities against a broad spectrum of insects such as bean aphid (Aphis craccivora), mosquito (Culex pipiens pallens) and diamondback moth (Plutella xylostella). Especially, the foliar contact activity against bean aphid of compound 7h at 2.5 mg kg -1 was 89%, the larvacidal activity against mosquito of compound 6c at 2.5 μg kg-1 was 100%, the activity against diamondback moth of compound 7a at 5 mg kg-1 was 87%, and all of these activities were much higher than the contrast ethiprole. The results of insecticidal activities showed that the two pairs of enantiomers 7d-1 and 7d-2 gave activities without distinctive difference, and it was the similar situation for 7e-1 and 7e-2. Interestingly, the target compounds exhibited high selectivity between diamondback moth and oriental armyworm, both of which are of the order Lepidoptera. The 2,2,2-trichloro-1-alkoxyethyl moiety was essential for high insecticidal activities.
- Zhao, Qiqi,Li, Yongqiang,Xiong, Lixia,Wang, Qingmin
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experimental part
p. 4992 - 4998
(2011/09/15)
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- Process for preparing 4-trifluoromethylsulfinylpyrazole derivative
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A process for the preparation of a compound of formula (I) comprising oxidizing a compound of formula (II) with trifluoroperacetic acid in the presence of a corrosion inhibiting compound such as boric acid. Also, a process for preparing a compound of formula (II) by adding sulfur dioxide to a mixture of the corresponding disulfide, a formate salt, trifluoromethyl bromide and a polar solvent; and a process for preparing the disulfide comprising adding S2Cl2to a solution, in an organic solvent, of the corresponding 4-unsubstituted pyrazole.
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