Cyclic Amine Insecticides With Tuned Substituents for Specificity

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Solution Overview

Problem

Existing pesticidal compounds for controlling pests such as insects and arthropods are inadequate in efficacy and specificity, particularly in agricultural applications.

Innovation Solution

Development of novel pesticidally active azetidinyl, piperidinyl, and piperazinyl aryl carbonyl compounds with specific structural modifications, including various substituents and potential salt forms, to enhance their acaricidal and insecticidal properties.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing pesticidal compounds are used, then pest control is provided, but efficacy and specificity are inadequate

Engineering Contradiction:
Improvepest control efficacyVSAvoidspecificity
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent introduces specific substituent groups (R1-R5) at different positions on the aromatic ring and cyclic amine structure, creating localized variations in molecular properties. This allows optimization of both efficacy (through electron-withdrawing groups like CN and halogens) and specificity (through spatial arrangement and steric effects), resolving the contradiction between general effectiveness and targeted action.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent systematically varies chemical parameters including substituent types (cyano, halo, alkoxy), ring sizes (azetidinyl, piperidinyl, piperazinyl), and linkage positions to optimize both pesticidal efficacy and specificity. By changing molecular parameters such as electron density distribution and steric configuration, the compounds achieve enhanced reliability while maintaining adaptability to different pest targets.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If novel compounds with specific structural modifications are developed, then acaricidal and insecticidal properties are enhanced, but compound complexity increases

Engineering Contradiction:
Improveacaricidal and insecticidal propertiesVSAvoidcompound structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent designs a universal molecular scaffold (aryl carbonyl connected to cyclic amine) that can perform multiple pesticidal functions. By varying substituents R1-R5 on this core structure, the same basic framework achieves both acaricidal and insecticidal activity, reducing the need for entirely separate compound classes and managing complexity through a unified structural platform.

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

Solution Approach 2:

The complex molecule is divided into functional segments: the aromatic ring system (providing structural stability), the carbonyl linker (providing connectivity), and the cyclic amine (providing basicity and binding capability). Each segment can be independently optimized through substituent selection, allowing enhanced pesticidal properties while managing overall complexity through modular design.

Inventive Principle:
Principle #1Segmentation

Data Source

PatentUS12604895B2Pesticidally active cyclic amine compounds
Publication Date: 2026.04.21 SYNGENTA CROP PROTECITON AG
  • US12604895B2 patent drawing
  • US12604895B2 patent drawing
  • US12604895B2 patent drawing

AI summary

Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides.