Isoxazoline Compound Structures for High-Efficacy Pest Control

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Solution Overview

Problem

Existing insecticides and acaricides do not meet the increasing demand for higher activity in agriculture and other fields, necessitating the development of compounds with superior insecticidal and acaricidal efficacy.

Innovation Solution

Development of isoxazoline compounds with specific structural variations, including different substituents and stereoisomers, and their salts, which exhibit enhanced insecticidal and acaricidal activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing insecticide compounds (KC1, KC2, KC3) are used, then basic insecticidal activity is achieved, but the insecticidal and acaricidal efficacy is insufficient to meet increasing application requirements

Engineering Contradiction:
Improveinsecticidal and acaricidal efficacyVSAvoidpest control effectiveness
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent applies parameter changes by systematically varying substituent groups (R1, R2, R3) at different positions of the isoxazoline core structure. Specific substitutions including fluorine, chlorine, methyl, ethyl, and various alkoxy groups were tested to optimize biological activity. This structural parameter optimization resulted in compounds with significantly enhanced insecticidal and acaricidal efficacy compared to prior art compounds KC1-KC3

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite material principles by combining the isoxazoline core structure with diverse substituent groups to create compound series with improved properties. The combination of electron-withdrawing groups (CF3, F, Cl) with various alkyl and alkoxy substituents on the benzene ring creates composite molecular structures that exhibit synergistic effects, resulting in superior pest control activity compared to simpler structures

Inventive Principle:
Principle #40Composite materials

2Reliability

If new isoxazoline compounds with enhanced activity are developed, then superior insecticidal and acaricidal efficacy is achieved, but structural complexity increases

Engineering Contradiction:
Improveinsecticidal and acaricidal efficacyVSAvoidmolecular structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the molecular structure into distinct functional segments: the isoxazoline core (providing basic activity), the benzene ring substituent (R1 position for polarity control), the alkyl/alkoxy chain (R2 position for lipophilicity), and the terminal functional group (R3 position for metabolic stability). This modular approach allows systematic optimization of each segment to enhance activity while maintaining reasonable structural complexity

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent implements local quality by introducing specific substituent groups at strategic positions to enhance particular properties. For example, fluorine and chlorine atoms at R1 position improve electron withdrawal and metabolic stability, while branched alkyl groups at R2 position enhance lipophilicity and binding affinity. This localized optimization allows enhancement of specific activity aspects without requiring complete structural redesign

Inventive Principle:
Principle #3Local quality

Data Source

PatentUS12371410B2Isoxazoline compounds and use thereof
Publication Date: 2025.07.29 METISA BIOTECHNOLOGY CO LTD
  • US12371410B2 patent drawing
  • US12371410B2 patent drawing
  • US12371410B2 patent drawing

AI summary

Disclosed are an isoxazoline compound and an application thereof. The structure of the compound is as shown in general formula (I). The definitions of substituents in the formula are described in the description. The description also discloses use of the compound of general formula (I) as an insecticide, acaricide and animal parasite control agent.