Isoxazoline Derivatives With Broad-Spectrum Invertebrate Pest Control
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Solution Overview
Problem
There is a need for highly effective and versatile agents to combat a wide range of invertebrate pests, particularly difficult-to-control pests such as insects, with a broad activity spectrum.
Innovation Solution
The development of isoxazoline compounds of formula I, including their stereoisomers, salts, and N-oxides, which are prepared through various synthetic routes such as amidation, Buchwald-Hartwig reaction, Horner-Wadsworth-Emmons reaction, and 1,3-dipolar cycloaddition, utilizing specific reactants and conditions to enhance pesticidal activity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If conventional pesticidal agents are used, then some pest control effect is achieved, but the activity spectrum is narrow and difficult-to-control pests remain unaffected
Solution Approach 1:
The patent applies parameter changes by systematically varying the substituent groups (R1-R8, R11-R14) on the core isoxazoline structure to optimize pesticidal activity. Different combinations of substituents at positions 3, 5, and 6 of the isoxazoline ring, along with variations in the aryl/heteroaryl groups and linker moieties, enable the compounds to target diverse pest species while maintaining broad-spectrum efficacy against difficult-to-control insects
2Reliability
If existing isoxazoline compounds are used, then some pesticidal activity is observed, but the activity is insufficient against a broad range of invertebrate pests
Solution Approach 1:
The patent employs composite material principles by combining the isoxazoline core structure with diverse aryl and heteroaryl substituents (including phenyl, pyridyl, thienyl groups) and various linker moieties (amides, carbamates, sulfonamides). This composite molecular architecture creates compounds with enhanced and broadened pesticidal activity across multiple invertebrate pest categories, achieving both high reliability and versatility
Data Source
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.