3-Alkoxybenzamide Derivatives for Low-Toxicity Pest Control

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Solution Overview

Problem

Existing pest control agents face challenges in providing effective pest control at low dosages while ensuring safety for workers and the environment, and they struggle to combat pests with acquired resistance, often having high human and animal toxicity.

Innovation Solution

Development of 3-alkoxybenzamide derivatives and their agriculturally acceptable salts, which exhibit excellent pest control effects as insecticides, nematicides, and acaricides, suitable for various crops and environments, including paddy fields, dry fields, lawns, orchards, and greenhouses, with improved safety and residual effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional pest control agents are used to achieve sufficient pest control effect, then pest control efficacy is improved, but human and animal toxicity increases and safety deteriorates

Engineering Contradiction:
Improvepest control effectVSAvoidhuman and animal toxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of benzamide derivatives through systematic variation of substituents at different positions (R1, R2, R3, R4, R5, R6) and functional groups (A, B, C, D, E). This structural optimization achieves high pest control efficacy while reducing toxicity to humans and animals, as evidenced by the selective toxicity profile of the compounds described in the patent.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If high dosage of pest control agents is applied to ensure sufficient control effect, then pest control efficacy is improved, but environmental impact and safety deterioration increases

Engineering Contradiction:
Improvepest control effectVSAvoidenvironmental impact
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent employs parameter changes by optimizing the chemical structure of 3-alkoxybenzamide derivatives to achieve high biological activity at low concentrations. The compounds exhibit potent pest control effects with reduced dosages, thereby minimizing environmental impact and residue concerns while maintaining effective pest management.

Inventive Principle:
Principle #35Parameter changes

3Duration of action of stationary object

If long-term use of existing pest control agents is continued to maintain control, then pest control coverage is improved, but pest resistance develops and control effectiveness deteriorates

Engineering Contradiction:
Improvepest control coverageVSAvoidcontrol effectiveness
Core Design Contradiction:
Duration of action of stationary objectVSReliability

Solution Approach 1:

The patent addresses pest resistance by introducing structurally novel 3-alkoxybenzamide derivatives with modified chemical parameters compared to existing pest control agents. The unique substitution patterns and functional group combinations create new modes of action that are effective against resistant pest populations, restoring and maintaining control effectiveness.

Inventive Principle:
Principle #35Parameter changes

4Adaptability or versatility

If broad-spectrum pest control is achieved to cover multiple pest types, then pest control versatility is improved, but selectivity decreases and harmful effects on non-target organisms increase

Engineering Contradiction:
Improvepest control versatilityVSAvoidharmful effects on non-target organisms
Core Design Contradiction:
Adaptability or versatilityVSObject-affected harmful factors

Solution Approach 1:

The patent achieves broad-spectrum pest control through systematic parameter changes in the benzamide derivative structure, allowing activity against multiple pest orders including Hemiptera, Lepidoptera, Coleoptera, Diptera, Hymenoptera, and Acari. The optimized compounds demonstrate selective toxicity that spares beneficial organisms and non-target species while maintaining efficacy across diverse pest types.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP4098650B13-alkoxy benzoic acid amide derivative, and pest control agent
Publication Date: 2025.12.10 KUMIAI CHEM IND CO LTD
  • EP4098650B1 patent drawing
  • EP4098650B1 patent drawing
  • EP4098650B1 patent drawing

AI summary

The present invention provides: a 3-alkoxybenzoic acid amide derivative having an excellent pest control effect, or a salt thereof; and a pest control agent and a production intermediate which contain the same as an active ingredient. Provided are: a 3-alkoxybenzoic acid amide derivative represented by general formula [I] [In the formula, A represents an oxygen atom or a sulfur atom, G represents a hydrogen atom, a halogen atom, or a C1-C6 alkyl group, R1 represents a C1-C6 alkyl group, a C3-C6 cycloalkyl group, etc., R2 represents a hydrogen atom, etc., R3 represents a halogen atom, C1-C6 alkyl group, etc., R4 represents a halogen atom, C1-C6 alkyl group, etc., and R5 represents a C1-C12 alkyl group, etc.], or a salt thereof; and a pest control agent characterized by containing said derivative or salt thereof as an active ingredient.