Sulfur-Substituted Fused Ring Insecticides for Broad Pest Control

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Existing fused heterocyclic compounds exhibit narrow application range and unsatisfactory insecticidal or acaricidal activity, necessitating the development of new compounds with improved biological and environmental characteristics for enhanced pest control.

Innovation Solution

Development of fused heterocyclic compounds with sulfur substituents, specifically compounds of formula (I), through a multi-step synthesis process involving reactions such as refluxing, coupling, and oxidation, to enhance insecticidal and acaricidal efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing fused heterocyclic compounds are used, then some pest control function is achieved, but the application range is narrow and insecticidal activity is unsatisfactory

Engineering Contradiction:
Improveinsecticidal activityVSAvoidapplication range
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent modifies the chemical structure of fused heterocyclic compounds by changing parameters such as introducing sulfur-containing substituents at specific positions (R1, R2, or both), varying heteroatom types (N, O, S), and adjusting substituent groups (alkyl, cycloalkyl, aryl, heteroaryl). These parameter changes in molecular structure result in improved insecticidal activity and expanded application range across different pest types while maintaining compatibility with crop plants.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates composite heterocyclic structures by combining different heteroatom types (nitrogen, oxygen, sulfur) within the same molecular framework. Examples include compounds with both nitrogen and sulfur atoms in the heterocyclic ring or as substituents, and structures combining multiple heterocyclic rings. This composite approach enhances biological activity and expands the range of effective pest control applications.

Inventive Principle:
Principle #40Composite materials

2Reliability

If new fused heterocyclic derivatives with sulfur substituents are developed, then insecticidal activity and application range are improved, but synthesis complexity increases

Engineering Contradiction:
Improveinsecticidal activityVSAvoidsynthesis process complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent divides the synthesis of complex fused heterocyclic compounds with sulfur substituents into multiple discrete steps. Each step focuses on introducing specific functional groups or modifying particular positions in the molecular structure. This segmentation allows for systematic development and optimization of synthesis routes, making the complex compound preparation more manageable and reproducible.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs intermediary compounds and reagents in the synthesis process. Intermediate heterocyclic compounds with specific substituents serve as precursors to the final target compounds. These intermediaries facilitate the stepwise construction of complex sulfur-containing heterocyclic structures, enabling controlled introduction of sulfur atoms and functional groups at desired positions.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If sulfur-containing substituents are introduced to enhance efficacy, then pest control effectiveness is improved, but manufacturing precision requirements increase

Engineering Contradiction:
Improvepest control effectivenessVSAvoidsynthesis precision
Core Design Contradiction:
ReliabilityVSManufacturing precision

Solution Approach 1:

The patent applies local quality modification by introducing sulfur-containing substituents at specific positions (R1, R2, or both) within the heterocyclic structure. Different positions are selected based on their impact on biological activity. This localized modification approach allows for precise control over which parts of the molecule are modified to achieve desired pest control effectiveness while minimizing unintended consequences.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent systematically varies parameters such as the type of sulfur-containing group (thioether, thiol, sulfone, etc.), the position of sulfur substitution, and the size and nature of attached substituents. These parameter changes enable optimization of pest control effectiveness while establishing clear synthetic targets that can be achieved with controlled precision in the laboratory.

Inventive Principle:
Principle #35Parameter changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The synthesized compounds demonstrate effective pest control, particularly against arthropods, with broad application range and compatibility with crop plants, even at low concentrations.

Implementation Method 1

reacting the compound of formula (VII) with a base to give the title compound

Methodology Applied
Scientific EffectElimination reaction:

Data Source

PatentUS20250361231A1Fused ring compounds with sulfur-containing substituents, preparation methods, insecticide compositions, and application
Publication Date: 2025.11.27 JIANGSU FLAG CHEM IND CO LTD
  • US20250361231A1 patent drawing
  • US20250361231A1 patent drawing
  • US20250361231A1 patent drawing

AI summary

A fused ring compound with a sulfur-containing substituent, a preparation method, an insecticide composition, and use are provided. Compared with the prior art, the fused ring compound with a sulfur-containing substituent has good prevention and treatment effect on many kinds of pests at a relatively low test concentration, providing a basis for research and development of new pesticides.