Bis(hetero)aryl Thioether Amides for Fungicidal Efficacy
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Solution Overview
Problem
Current crop protection agents are inadequate in effectively controlling a broad spectrum of phytopathogenic microorganisms, such as fungi, with low toxicity, high selectivity, and at low application rates, while also preventing the emergence of resistances.
Innovation Solution
Development of new Bis(hetero)aryl thioether (thio)amide derivatives that act as fungicides, offering improved efficacy against phytopathogenic fungi with reduced toxicity and the potential to prevent resistance development.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If new fungicidal compounds are developed to control a broad spectrum of phytopathogenic microorganisms, then efficacy against fungi is improved, but toxicity may increase
Solution Approach 1:
The patent employs parameter changes by systematically varying molecular structures within the pyridine amide framework (different substituents R1-R6, ring systems Y1-Y6) to optimize the balance between fungicidal efficacy and toxicity. This allows tuning of compound properties to achieve broad-spectrum effectiveness while maintaining low toxicity profiles.
Solution Approach 2:
The invention creates composite molecular structures combining pyridine amide cores with various heterocyclic and aromatic substituents. These composite structures integrate multiple functional moieties that work synergistically to enhance antifungal activity while controlling toxicity through careful selection of biocompatible groups.
2Object-affected harmful factors
If application rate is reduced to lower toxicity impact, then environmental safety is improved, but control effectiveness may decrease
Solution Approach 1:
The patent achieves enhanced potency at low application rates through parameter changes in molecular structure, specifically optimizing lipophilicity, molecular weight, and functional group composition. These changes increase the compounds' biological activity per unit dose, enabling effective control at reduced application rates that minimize toxic impact.
3Productivity
If existing crop protection agents are used, then immediate pest control is achieved, but resistance development occurs
Solution Approach 1:
The patent applies segmentation by developing multiple distinct pyridine amide compounds with varied molecular structures and modes of action. This diversification within the product family allows rotation and mixing strategies that prevent resistance development, while each individual compound maintains immediate effectiveness against target pathogens.
Data Source
AI summary
The present invention relates to Bis(hetero)aryl thioether (thio)amides derivatives and the uses thereof for controlling phytopathogenic microorganisms such as phytopathogenic fungi. It also relates to processes and intermediates for preparing these compounds.