A class of polysubstituted pyrazole amide derivatives and preparation method and applications thereof
A technology of pyrazole amide and multi-substitution, which is applied in the fields of botany equipment and methods, chemicals for biological control, biocides, etc., and can solve the problems of safety and prohibition
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Embodiment 1
[0029] Embodiment 1: the preparation of compound II-1:
[0030]
[0031] In a 100 ml single-necked round bottom flask, add 3 mmol of polysubstituted pyrazole acid I-1, add 30 ml of dichloromethane solution, ice-water bath, the temperature drops to zero, two drops of N, N-dimethylformamide, Slowly add 6 mmol oxalyl chloride solution dropwise, after the dropwise addition, slowly rise to room temperature, and stir at room temperature for 2 hours; after spotting the plate to monitor the completion of the reaction, first concentrate under reduced pressure to remove excess oxalyl chloride solution and dichloromethane. The crude product II-1 was obtained for use. The amount of compound II-1 prepared and the volume of the reaction vessel are enlarged or reduced in proportion.
Embodiment 2
[0032] Embodiment 2: the preparation of compound IV-1:
[0033]
[0034] Add 3 millimoles of compound III-1 in a 100 milliliter single-necked round bottom flask, dissolve it with 30 milliliters of dry dichloromethane, add 6 millimoles of triethylamine to the reaction, after the addition, stir in an ice bath for 10 minutes, Then, 3 millimoles of compound II-1 dissolved in 5 milliliters of dry dichloromethane was added dropwise to the reaction system; after the addition, it was stirred in an ice bath for 30 minutes, and then stirred at room temperature for 4 hours. After the reaction, 15 milliliters of Extract with water and dichloromethane three times, separate the organic layer, wash the organic layer once with saturated sodium chloride, dry over anhydrous sodium sulfate, filter with suction, remove the solvent under reduced pressure, and purify the residue by 100-200 mesh silica gel column chromatography to obtain Compound IV, eluent is sherwood oil of 60~90 degrees centig...
Embodiment 3
[0035] Example 3: Determination of the bactericidal activity of the multi-substituted pyrazole amide derivative IV of the present invention:
[0036] The common phytopathogenic fungus code name and title of the present invention's test are as follows: AS: tomato early blight fungus, its Latin name is: Alternaria solani, BC: cucumber gray mold, its Latin name is: Botrytis cinerea, GZ: wheat scab, Its Latin name: Gibberella zeae, PI: Potato infestans, its Latin name: Phytophthorainfestans (Mont.) de Bary, PP: Apple ringworm, its Latin name: Physalospora piricola, PS: Rice sheath blight , its Latin name: Pellicularia sasakii, RC: Rhizoctonia graminearum, its Latin name: Rhizoctonia cerealis, SS: Sclerotinia sclerotiorum, its Latin name: Sclerotinia sclerotiorum. These species represent most of the pathogenic species that occur in fields in agricultural production.
[0037] The results of the cell growth rate method are shown in Table 2. Table 2 shows that most of the compounds o...
PUM
Login to View More Abstract
Description
Claims
Application Information
Login to View More