Substituted Isoxazoline Compounds for Broad-Spectrum Pest Control

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Solution Overview

Problem

There is a need for highly effective and versatile agents that can combat a wide range of invertebrate pests, particularly difficult-to-control insects, with a broad activity spectrum.

Innovation Solution

The development of isoxazoline compounds of specific structural formulae, including their stereoisomers, salts, and N-oxides, which are synthesized through various chemical reactions such as amidation, Buchwald-Hartwig reaction, and Horner-Wadsworth-Emmons reaction, using starting materials and catalysts to achieve good pesticidal activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If existing pesticidal compounds are used, then some pest control activity is achieved, but the activity spectrum is insufficient and difficult-to-control insects remain unaffected

Engineering Contradiction:
Improveactivity spectrumVSAvoidefficacy against difficult-to-control pests
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent applies parameter changes by systematically modifying the chemical structure of isoxazoline compounds through varying substituents at different positions (R1-R6 groups). This structural parameter optimization enables the compounds to achieve both broad spectrum activity and high efficacy against difficult-to-control pests by tuning molecular properties to enhance pest control effectiveness.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If new pesticidal compounds with broad activity spectrum are developed, then efficacy against difficult-to-control pests improves, but the complexity of compound synthesis increases

Engineering Contradiction:
Improve pesticidal activityVSAvoidsynthesis complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent employs segmentation by dividing the complex molecule into distinct functional modules or building blocks that can be synthesized separately and then assembled. This modular approach to molecular construction simplifies the overall synthesis process while maintaining the complex structural features necessary for high pesticidal activity.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent applies universality by developing a core isoxazoline structure that serves multiple pesticidal functions and can target different pest types. This multi-functional core structure reduces synthesis complexity by using a single versatile platform that can be adapted to achieve broad-spectrum activity rather than requiring separate specialized compounds for each pest type.

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

Data Source

PatentEP4291551B1Substituted isoxazoline derivatives
Publication Date: 2025.08.13 BASF SE
  • EP4291551B1 patent drawing
  • EP4291551B1 patent drawing
  • EP4291551B1 patent drawing

AI summary

The invention relates to isoxazoline compounds of formula (I) wherein the variables have the meanings as defined in the specification, to compositions comprising them, to active compound combinations comprising them, and to their use for protecting growing plants and animals from attack or infestation by invertebrate pests, furthermore, to seed comprising such compounds.