Pyrazole Amide Compounds with Diphenyl Ether for Crop Disease Control
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Solution Overview
Problem
Current pyrazole amide compounds containing a diphenyl ether group are ineffective in preventing and treating rice sheath blight and cucumber powdery mildew, leading to significant yield losses due to drug resistance in pathogenic bacteria.
Innovation Solution
Development of two specific pyrazole amide compounds (represented by formula I and formula II) with a diphenyl ether group, which are synthesized using specific synthetic routes and formulated into pesticide compositions for effective application against rice sheath blight and cucumber powdery mildew.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing pyrazole amide compounds containing a diphenyl ether group are used, then the pesticide can be applied to crops, but the prevention and control effect on rice sheath blight and cucumber powdery mildew is poor
Solution Approach 1:
The patent modifies the chemical structure parameters of pyrazole amide compounds by introducing specific substituents (halogen atoms at positions 3 and 5 of the pyrazole ring, diphenyl ether group at position 1, and specific R1-R6 groups) to enhance biological activity. This structural parameter optimization resolves the contradiction by achieving both effective disease control and preventing yield loss.
Solution Approach 2:
The patent creates composite pesticide formulations by combining the novel pyrazole amide compound with adjuvants such as organic solvents, surfactants, and stabilizers. This composite approach enhances the efficacy of the active ingredient while maintaining crop safety and economic viability.
2Reliability
If existing bactericides are used extensively, then disease prevention can be achieved, but pathogenic bacteria develop serious drug resistance
Solution Approach 1:
The patent introduces a novel chemical structure with halogen substituents (Cl, F, or CF3) at positions 3 and 5 of the pyrazole ring, combined with a diphenyl ether group and specific amide substituents. This structural parameter change creates a new mode of action that overcomes existing drug resistance in pathogenic bacteria while maintaining effective disease control.
3Reliability
If new pyrazole amide compounds are developed, then better prevention and control effects can be achieved, but the synthesis complexity increases
Solution Approach 1:
The patent divides the synthesis into modular stages: (1) preparation of substituted phenyl halides, (2) coupling with pyrazole carboxylic acid derivatives, (3) introduction of diphenyl ether group, and (4) final amide bond formation. This segmentation allows each step to be optimized independently, achieving high biological activity while managing synthesis complexity.
Solution Approach 2:
The patent employs universal synthetic intermediates and reagents that can be applied across multiple compound variants. The core pyrazole-diphenyl ether scaffold serves as a universal platform that can accommodate various halogen and amide substituents, reducing overall synthesis complexity while maintaining high biological activity.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The compounds demonstrate superior biological activity compared to existing pyrazole amide compounds, achieving 100% control effect on rice sheath blight and cucumber powdery mildew, even at low concentrations, outperforming commercial bactericides like Thifluzamide.
Implementation Method 1
The prevention and treatment effect of such bactericide is achieved by inhibiting the activity of pathogenic bacteria succinate dehydrogenase and causing death of the pathogenic bacteria
Data Source
AI summary
Disclosed are a pyrazole amide compound containing diphenyl ether as represented by formula I and/or formula II, application thereof in the prevention and treatment of rice sheath blight and cucumber powdery mildew, and pesticide composition containing the compound. The pyrazole amide compound of the present invention containing diphenyl ether as represented by formula I and/or formula II, and a bactericide containing the pyrazole amide compound as an active ingredient have good prevention and treatment effects on rice sheath blight and cucumber powdery mildew.