5-oxy-substituted 3-phenylisoxazoline Amides for Selective Weed Control
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Solution Overview
Problem
Current herbicides and fungicides lack effective compounds for selective control of broad-leaved weeds and weed grasses in crops, with existing agrochemicals either lacking herbicidal action or being non-selective, leading to damage to crop plants.
Innovation Solution
Development of 5-oxy-substituted 3-phenylisoxazoline-5-carboxamides and 5-oxy-substituted 3-phenylisoxazoline-5-thioamides, which exhibit both herbicidal and fungicidal activity, specifically designed to target unwanted plant species while minimizing impact on economically important crops.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing agrochemical compounds are used, then some herbicidal or fungicidal action is achieved, but the compounds either lack herbicidal action or are non-selective causing damage to crop plants
Solution Approach 1:
The patent applies local quality by introducing specific substituent patterns at defined positions on the phenyl ring (positions 2, 3, 4, 5, or 6) and isoxazoline ring (positions 5 and 6). Different substituent combinations at these specific locations create compounds with selective herbicidal activity that spares crop plants, resolving the contradiction between herbicidal efficacy and crop safety.
Solution Approach 2:
The patent employs parameter changes by systematically varying substituent types (halogens, alkyl groups, alkoxy groups, cyano groups), their positions, and the nature of linkers (A and B groups) to optimize the balance between herbicidal activity and selectivity. This structured modification of molecular parameters enables achievement of both high herbicidal reliability and minimal crop damage.
2Adaptability or versatility
If non-selective herbicides are used, then broad weed control is achieved, but crop plants are damaged
Solution Approach 1:
The patent achieves selective broad-spectrum weed control through local quality modifications at specific molecular positions. The defined substituent patterns on the phenyl and isoxazoline rings create compounds that can target multiple weed types while maintaining selectivity for crop safety, resolving the contradiction between versatility and crop protection.
Solution Approach 2:
The patent creates multi-functional compounds that simultaneously provide herbicidal activity against broadleaf weeds and grasses, fungicidal activity, and crop safety. The core isoxazoline structure with specific substituent patterns enables these multiple functions to coexist, achieving universal weed control without crop damage.
3Object-affected harmful factors
If selective herbicides are used, then crop safety is improved, but efficacy against difficult-to-control perennial weeds is reduced
Solution Approach 1:
The patent uses parameter changes to enhance herbicidal efficacy while maintaining crop safety. By varying substituent types, positions, and linker characteristics, the invention optimizes the compounds' ability to control perennial weeds with tough root systems while preserving selectivity that protects crop plants, resolving the contradiction between efficacy and safety.
Solution Approach 2:
The patent creates composite molecular structures combining the isoxazoline core with specifically designed phenyl substituents and linker groups. This composite structure integrates multiple functional elements that work together to achieve both high efficacy against perennial weeds and selective crop safety, overcoming the limitation of conventional selective herbicides.
Data Source
AI summary
Herbicidally and fungicidally active 5-oxy-substituted 3-phenylisoxazoline-5-carboxamides and 5-oxy-substituted 3-phenylisoxazoline-5-thioamides of the formula (I) are described.In this formula (I), X, X2 to X6, R1 to R4 are radicals such as hydrogen, halogen and organic radicals such as substituted alkyl. A is a bond or a divalent unit. Y is a chalcogen.