Substituted Acetophenone Amides for Broad-Spectrum Fungal Control

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Solution Overview

Problem

Existing amide compounds do not effectively address the control of various germs in agriculture, particularly for diseases such as Oomycetes, deuteromycete, basidiomycete, and ascomycete diseases, which are not covered by prior art compounds like CK1, CK2, CK3, and CK4.

Innovation Solution

Development of an amide compound with a substituted acetophenone structural fragment, represented by general formula I, which includes specific substitutions for R1, R2, R3, and R4, and B groups, providing enhanced fungal activity against a wide range of agricultural pathogens.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If existing amide compounds (CK1, CK2, CK3, CK4) are used, then some fungal diseases can be controlled, but they cannot effectively control Oomycetes, deuteromycetes, basidiomycetes, and ascomycetes

Engineering Contradiction:

Improvespectrum of fungal disease controlVSAvoideffectiveness against specific pathogen groups

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The patent modifies the chemical structure of existing amide compounds by introducing a substituted acetophenone structural fragment at the R1 position with specific substituents (halogen, alkyl, alkoxy, or hydroxyl groups). This structural parameter change transforms the compound's properties, enabling it to effectively control Oomycetes, deuteromycetes, basidiomycetes, and ascomycetes while maintaining activity against other fungal diseases.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention creates a hybrid molecular structure combining the amide core framework with a substituted acetophenone fragment. This composite structural approach integrates the beneficial properties of both structural elements, resulting in a fungicide with expanded spectrum and enhanced reliability across multiple pathogen groups including those previously poorly controlled.

Inventive Principle:

Principle #40Composite materials

2Reliability

If the chemical structure is modified to include substituted acetophenone fragment, then activity against Oomycetes and other difficult-to-control pathogens is improved, but the complexity of the molecule increases

Engineering Contradiction:

Improvefungal activity against Oomycetes, deuteromycetes, basidiomycetes, ascomycetesVSAvoidmolecular structure complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent introduces the substituted acetophenone fragment at a specific local position (R1 position) of the amide molecule rather than redesigning the entire structure. This localized modification with specific substituents (halogen, alkyl, alkoxy, or hydroxyl groups) achieves enhanced fungal activity while minimizing overall molecular complexity and maintaining synthetic feasibility.

Inventive Principle:

Principle #3Local quality

Data Source

PatentEP4052576B1Amide compound containing substituted acetophenone structure fragment, preparation method therefor and use thereof

Publication Date: 2026.02.18 SHENYANG SINOCHEM AGROCHEMICALS R&D CO LTD

AI summary

The present invention discloses an amide compound containing substituted acetophenone structural fragments, having a structure shown by general formula I: The definitions of substituents in the formula are shown in the description. The compound of the present invention has broad-spectrum fungal activity, and has excellent control effects on cucumber downy mildew, wheat powdery mildew, corn rust, cucumber anthracnose, cucumber botrytis and tomato botrytis.