Isoxazoline-Substituted Benzamide Compounds for Pest Control
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Solution Overview
Problem
Pests have developed resistance to conventional pesticides, making them less effective, and some pesticides are toxic and persist in the environment, disrupting native ecosystems.
Innovation Solution
Development of novel isoxazoline-substituted benzamide compounds with excellent insecticidal and acaricidal activity that have low toxicity and short persistence, targeting harmful arthropods in agricultural and livestock settings.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional pesticides are used repeatedly, then pest control effectiveness is maintained initially, but pests develop resistance and control effectiveness decreases over time
Solution Approach 1:
The patent introduces a completely new chemical structure class (isoxazoline-substituted benzamide) with distinct molecular parameters compared to conventional pesticides. This structural parameter change creates novel modes of action that pests have not encountered before, thereby preventing resistance development while maintaining control effectiveness
Solution Approach 2:
The patent combines multiple functional moieties (isoxazoline ring, benzamide group, and various substituent patterns) into a composite molecular structure. This composite approach creates complex three-dimensional structures with multiple interaction points, enhancing efficacy while reducing the likelihood of resistance through multi-target engagement
2Reliability
If conventional pesticides are used to ensure pest control, then harmful effects on native ecosystems and persistence in environment occur
Solution Approach 1:
The patent employs specific substituent patterns at defined positions on the benzamide core structure, creating localized functional regions with optimized properties. The isoxazoline substitution at specific positions provides selective activity against target arthropods while the overall molecular architecture limits non-specific interactions with non-target species, reducing ecological harm
Solution Approach 2:
The patent designs compounds with intentional environmental transientness - the molecular structure is optimized for rapid degradation after fulfilling its pest control function. This short-living characteristic ensures the pesticide acts effectively during the treatment period then breaks down, preventing long-term persistence and cumulative ecological damage
3Reliability
If novel isoxazoline-substituted benzamide compounds are developed, then pest control activity with low toxicity is achieved, but synthesis complexity increases
Solution Approach 1:
The patent divides the complex molecular structure into distinct synthetic modules: the isoxazoline ring system, the benzamide core, and various substituent groups. Each module can be prepared separately through standardized reactions, then assembled through coupling reactions. This segmentation transforms a potentially complex one-step synthesis into multiple manageable steps, improving selectivity while controlling overall synthesis complexity
Solution Approach 2:
The patent employs universal building blocks and protecting group strategies that can be applied across multiple compound variants in the series. The benzamide core and isoxazoline substitution pattern serve as universal frameworks that accommodate various R groups through consistent synthetic protocols, reducing the incremental complexity of generating diverse analogs with optimized selectivity profiles
Data Source
AI summary
An isoxazoline-substituted benzamide compound of formula (1) or a salt thereof:wherein A1, A2 and A3 independently of one another are carbon atom or nitrogen atom, G is benzene ring, etc., X is halogen atom, C1-C6haloalkyl, etc., Y is halogen atom, C1-C6alkyl, etc., R1 is C1-C12alkyl arbitrarily substituted with R16, C3-C2alkenyl, arbitrarily substituted with R16 is oxygen atom or sulfur atom, —N(R20)R19, etc., R2 is hydrogen atom, C1-C4alkoxy C1-C6alkyl, etc., R3 is C1-C6haloalkyl, etc., R16 is halogen atom, cyano, phenyl substituted with (Z)p1, D-1 to D-60, E-1 to E-49, etc., R19 is phenyl, phenyl substituted with (Z)p1, etc., R20 is hydrogen atom, C1-C6alkyl, etc., Z is halogen atom, nitro, C1-C4alkoxy, etc., D-1 to D-60 are 5- or 6-membered aromatic heterocyclic rings, E-1 to E-49 are 5- or 6-membered saturated heterocyclic rings, m is an integer of 0 to 5, n is an integer of 0 to 4, p1 is an integer of 1 to 5. The pesticide containing these compounds.