Aryl Sulfide Derivatives for Low-Rate Insecticidal Activity

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Solution Overview

Problem

Existing aryl sulfide and aryl sulfoxide derivatives have inadequate insecticidal and/or acaricidal activity against animal pests, especially at low application rates, and lack selectivity and compatibility in crops.

Innovation Solution

Development of novel aryl sulfide, aryl sulfoxide, and arylsulfone derivatives with specific structural features, including various substituents and ring systems, which provide enhanced insecticidal and acaricidal activity at low application rates with improved selectivity and compatibility in crops.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing aryl sulfide and aryl sulfoxide derivatives are used, then some insecticidal activity is achieved, but the activity is inadequate especially at low application rates

Engineering Contradiction:

Improveinsecticidal activityVSAvoidapplication rate

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

The patent modifies the chemical structure of aryl sulfide and aryl sulfoxide derivatives by introducing specific substituents (fluoro, cyano, amino groups) and varying molecular weights to optimize the insecticidal activity at low application rates. This involves changing chemical parameters such as substituent types and positions to enhance biological activity without increasing the quantity applied.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If existing aryl sulfide and aryl sulfoxide derivatives are used, then some acaricidal activity is achieved, but the activity is inadequate especially at low application rates

Engineering Contradiction:

Improveacaricidal activityVSAvoidapplication rate

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

The patent optimizes the chemical parameters of the compounds by introducing specific functional groups and molecular structures that enhance acaricidal activity. This allows achieving satisfactory activity at low application rates by modifying the molecular properties rather than increasing the application quantity.

Inventive Principle:

Principle #35Parameter changes

3Reliability

If existing aryl sulfide and aryl sulfoxide derivatives are used, then some insecticidal activity is achieved, but selectivity and compatibility in crops are insufficient

Engineering Contradiction:

Improveinsecticidal activityVSAvoidselectivity and compatibility

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent introduces specific local functional groups and structural features at particular positions in the molecule to enhance selectivity for target pests while improving compatibility with crops. This involves making different parts of the molecule have different properties - the core structure provides activity while specific substituents provide selectivity and safety characteristics.

Inventive Principle:

Principle #3Local quality

Data Source

PatentUS9981928B2Aryl sulfide derivatives and aryl sulfoxide derivatives as acaricides and insecticides

Publication Date: 2018.05.29 BAYER CROPSCIENCE AG

AI summary

The present invention relates to aryl sulfoxide derivatives, to the use thereof as acaricides and insecticides for controlling animal pests and to processes and intermediates for preparation thereof. The aryl sulfide and aryl sulfoxide derivatives have the general structure (I)in which the respective radicals are as defined in the description.