Aryl Amidines Broad-Spectrum Fungicidal Activity

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Solution Overview

Problem

Current fungicides are not universally effective against various fungal pathogens affecting plants, and there is a need for compounds that are easier to use and cost-effective.

Innovation Solution

Development of aryl amidine compounds, specifically those of Formula I, which can be used as fungicides to protect plants against ascomycetes, basidiomycetes, deuteromycetes, and oomycetes, applied in formulations such as solutions, dusts, or granules, utilizing a phytologically acceptable carrier to ensure efficacy and safety.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If current fungicides are used, then some fungal pathogens are controlled, but they are not universally effective against various fungal pathogens

Engineering Contradiction:
Improvefungicidal spectrumVSAvoidcontrol effectiveness
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent develops aryl amidine compounds with a core chemical structure (Formula I) that provides broad-spectrum fungicidal activity against multiple fungal groups including ascomycetes, basidiomycetes, deuteromycetes, and oomycetes. The universal amidine scaffold serves multiple functions by targeting different fungal pathogens through a single compound design, resolving the contradiction between specialization and broad effectiveness.

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

Solution Approach 2:

The patent systematically varies substituent parameters (R1-R10 groups) on the amidine core structure to optimize activity against different fungal pathogens. By changing chemical parameters such as alkyl groups, haloalkyl groups, alkoxy groups, and heterocyclic substituents at different positions, the compound's fungicidal spectrum and effectiveness are enhanced across multiple fungal types simultaneously.

Inventive Principle:
Principle #35Parameter changes

2Adaptability or versatility

If new fungicidal compounds are developed, then broader protection is achieved, but development cost and complexity increase

Engineering Contradiction:
Improvefungicidal spectrumVSAvoidcompound structure complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The fungicidal compound is segmented into a core amidine structure (Formula I) with distinct substitutable positions (R1-R10). This segmentation allows independent optimization of different molecular regions: the core provides the essential fungicidal activity, while peripheral substituents fine-tune specificity and potency against different fungal groups, simplifying the design process for broad-spectrum compounds.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs systematic parameter variation of substituent groups (alkyl, haloalkyl, alkoxy, heterocyclic, aryl groups) at defined positions on the amidine core. This structured approach to parameter changes enables methodical optimization of fungicidal properties without requiring completely new molecular scaffolds, thereby controlling development complexity while achieving broad-spectrum activity.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS20240000075A1Fungicidal aryl amidines
Publication Date: 2024.01.04 CORTEVA AGRISCIENCE LLC
  • US20240000075A1 patent drawing
  • US20240000075A1 patent drawing
  • US20240000075A1 patent drawing

AI summary

This disclosure relates to aryl amidines of Formula I and their use as fungicides.