Sulfur-Substituted Polycyclic Derivatives for Resistant Pest Control
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Solution Overview
Problem
Current pesticidally active compounds lack effectiveness against resistant animal pests, including insects and Acarina, and have limitations in their application spectrum and tolerance by warm-blooded species, fish, and plants.
Innovation Solution
Development of novel polycyclic derivatives containing sulfur substituents, specifically compounds of formula I, which are synthesized through Suzuki and Stille reactions, offering a broad spectrum of activity against various pest developmental stages.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current pesticidally active compounds are used, then they provide some level of pest control, but they lack effectiveness against resistant animal pests and have limitations in application spectrum
Solution Approach 1:
The patent applies parameter changes by systematically varying substituents at multiple positions (R1-R6, X1-X3, A1-A3, Q) in the polycyclic derivative structure. This includes changing atomic types (C, N, O, S), chain lengths (C1-C6), and substituent patterns to create a series of analogs with different biological activities, thereby achieving both improved effectiveness against resistant pests and expanded application spectrum
Solution Approach 2:
The invention employs composite molecular structures combining polycyclic core frameworks with diverse heterocyclic substituents containing sulfur atoms. This composite approach integrates multiple functional moieties (e.g., thiophene, thiazole, selenophene rings) with the core structure to create molecules that simultaneously achieve high efficacy against resistant pests and broad-spectrum activity
2Reliability
If higher application rates are used to overcome resistance, then pest control effectiveness may improve, but tolerance by warm-blooded species, fish, and plants decreases
Solution Approach 1:
The patent applies local quality by introducing sulfur-containing heterocyclic substituents at specific positions on the polycyclic core structure. These localized modifications at particular molecular sites enhance binding affinity to pest targets while maintaining selective toxicity, allowing effective pest control at low application rates without harming warm-blooded species, fish, or plants
Solution Approach 2:
The invention uses parameter changes to optimize the balance between efficacy and safety by systematically varying substituent types (sulfur vs. oxygen vs. nitrogen), chain lengths, and positional isomers. This enables fine-tuning of molecular properties to achieve high pest control effectiveness while maintaining low toxicity to non-target organisms
Data Source
AI summary
Polycyclic derivatives of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.