Pyrazole Derivatives for Low-Rate Pest Control

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Solution Overview

Problem

Current pyrazole derivatives for pest control lack efficacy at low application rates and have limited spectrum against resistant pest strains.

Innovation Solution

Development of specific pyrazole derivatives with structures defined by formulas (I) and (II), incorporating various substituents, which exhibit enhanced insecticidal, acaricidal, and molluscicidal properties through specific synthetic methods, allowing for effective pest control at lower application rates.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current pyrazole derivatives are used for pest control, then pest control function is provided, but efficacy at low application rates is insufficient and spectrum against resistant pest strains is limited

Engineering Contradiction:
Improveefficacy against pestsVSAvoidapplication rate
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent applies parameter changes by systematically varying substituents at specific positions (R1 at position 5, R2 at position 4, Y1/Y3 at positions 2/6) of the pyrazole core structure. This includes changing molecular weight, hydrophobicity, and steric properties through different alkyl, haloalkyl, and functional group combinations, resulting in compounds with enhanced efficacy at lower application rates

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates composite molecular structures by combining the pyrazole core with diverse substituent patterns including fluorinated alkyl groups, cyano substituents, and various carbonyl-containing groups. These composite structures synergistically improve both efficacy and spectrum of activity against resistant pest strains

Inventive Principle:
Principle #40Composite materials

2Adaptability or versatility

If current pyrazole derivatives are used for pest control, then basic pest control function is provided, but spectrum against resistant pest strains is limited

Engineering Contradiction:
Improvespectrum against resistant pest strainsVSAvoidefficacy against pests
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent achieves universality by designing a pyrazole core structure that can simultaneously target multiple pest types (insects, mites, nematodes) and overcome various resistance mechanisms. The substituent patterns are optimized to provide broad-spectrum activity while maintaining high efficacy against specific resistant strains through multiple modes of action

Inventive Principle:
Principle #6Universality (Multi-functionality)

Data Source

PatentUS11490620B2Pesticidally active thiophene derivatives
Publication Date: 2022.11.08 SYNGENTA CROP PROTECITON AG
  • US11490620B2 patent drawing
  • US11490620B2 patent drawing
  • US11490620B2 patent drawing

AI summary

Compounds of formula (I), as defined herein, to processes for preparing them, to pesticidal, in particular insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control pests such as insect, acarine, molluse and nematode pests.