Heterocyclic Compounds for Broad-Spectrum Pest Control

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Solution Overview

Problem

Current plant protection products face challenges in terms of broad spectrum efficacy, resistance, toxicity, compatibility, and synthesis effort, necessitating the development of new compounds with improved properties for effective pest control.

Innovation Solution

Development of novel heterocyclic compounds of the formula (I), specifically designed to combat animal pests such as insects, arachnids, and nematodes, through specific synthesis processes involving amines and acid derivatives, utilizing various coupling reagents and solvents to achieve effective pesticide formulations.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If existing heterocyclic pesticide compounds are used, then pest control activity is achieved, but the spectrum of efficacy is limited and resistance occurs

Engineering Contradiction:
Improvespectrum of pest control efficacyVSAvoidpest resistance
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The invention divides the pest control problem into multiple target sites by designing compounds that can inhibit different enzymes (phosphatases, esterases, proteases). The heterocyclic core structure serves as a platform for creating multiple analogs with different specificities, allowing simultaneous targeting of multiple pest physiological pathways rather than relying on a single mode of action.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent systematically varies chemical parameters of the heterocyclic compounds including substituent types (halogen, alkyl, alkoxy), positions (R1-R7), and molecular weight (150-500 g/mol) to optimize activity against different pest species and resistance profiles. This parameter optimization enables tuning of compound properties to achieve broad-spectrum efficacy while managing resistance development.

Inventive Principle:
Principle #35Parameter changes

2Adaptability or versatility

If new heterocyclic compounds are synthesized, then broad-spectrum pest control is achieved, but synthesis effort and complexity increase

Engineering Contradiction:
Improvebroad-spectrum pest controlVSAvoidsynthesis process complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The heterocyclic core structure serves as a universal platform that can be modified with different substituents to create multiple active compounds targeting different pests. The core structure itself (with nitrogen atoms in 5-membered ring) provides the fundamental pesticidal activity, while substituents fine-tune specificity and potency, allowing one synthetic route to generate multiple useful pesticides.

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

Solution Approach 2:

The patent establishes a preliminary heterocyclic core structure that already possesses pesticidal activity, upon which further substitutions are made to optimize for specific pests. This preliminary structure reduces synthesis complexity compared to building entire molecules from scratch, as the core framework and key functional groups are pre-established.

Inventive Principle:
Principle #10Preliminary action

3Object-affected harmful factors

If conventional pesticide compounds are used, then pest control is achieved, but toxicity and environmental compatibility issues arise

Engineering Contradiction:
Improvepest control effectivenessVSAvoidtoxicity and environmental impact
Core Design Contradiction:
Object-affected harmful factorsVSObject-generated harmful factors

Solution Approach 1:

The patent optimizes molecular weight (150-500 g/mol) and substituent selection (halogen, alkyl, alkoxy groups) to achieve the right balance between pesticidal activity and environmental compatibility. These parameter changes allow tuning of compound properties to reduce non-target toxicity while maintaining effectiveness against pests, addressing both sides of the toxicity-effectiveness trade-off.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP3113618B1Heterocyclic compounds as pest controllers
Publication Date: 2018.07.04 BAYER CROPSCIENCE AG
  • EP3113618B1 patent drawing
  • EP3113618B1 patent drawing
  • EP3113618B1 patent drawing

AI summary

The invention relates to novel heterocyclic compounds, to their use for controlling animal pests, which include arthropods, insects and nematodes, and to methods and intermediate products for producing said novel compounds.