Substituted Pyrimidine Ammonia Compounds for Low-Dose Fungicidal Control

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Solution Overview

Problem

Current fungicides are inadequate for effectively controlling harmful diseases in agrarian, civil, and zoo-technical fields, necessitating the development of novel compounds with improved fungicidal activity at low dosages.

Innovation Solution

Substituted pyrimidine ammonia compounds with specific structural formulas, which exhibit fungicidal activity against various plant pathogens, are developed for use in agriculture and other fields to control diseases such as cucumber downy mildew and wheat powdery mildew.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional fungicides are used, then disease control is achieved, but the dosage required is high and effectiveness is insufficient

Engineering Contradiction:
Improvefungicidal effectivenessVSAvoiddosage
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent modifies the chemical structure of pyrimidine ammonia compounds by changing parameters such as substituting hydrogen atoms with halogen atoms (fluorine, chlorine, bromine), introducing alkyl groups, alkoxy groups, and other functional groups at specific positions (R1-R5) in the molecular structure. These structural parameter changes enhance the compound's biological activity and fungicidal effectiveness, allowing for reduced dosage requirements while maintaining or improving disease control performance.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If novel compounds are developed to improve fungicidal activity, then disease control effectiveness increases, but development complexity increases

Engineering Contradiction:
Improvefungicidal activityVSAvoidcompound structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent employs a systematic approach to molecular design by segmenting the pyrimidine ammonia core structure and independently modifying various positions (R1-R5) with different functional groups. This segmentation allows for modular development where each position can be optimized for specific biological activities, facilitating the discovery of novel compounds with enhanced fungicidal properties through a structured rather than random approach.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent develops a universal pyrimidine ammonia compound framework that can be applied to control multiple types of plant diseases through systematic substitution at different positions. The core structure serves as a multi-functional platform where varying R1-R5 groups can target different pathogens (fungi, oomycetes) and disease types, reducing the need to design entirely new compounds for each application while maintaining high fungicidal activity.

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

Data Source

PatentUS9018218B2Substituted pyrimidine ammonia compounds and uses thereof
Publication Date: 2015.04.28 SHENYANG SINOCHEM AGROCHEMICALS R&D CO LTD
  • US9018218B2 patent drawing
  • US9018218B2 patent drawing
  • US9018218B2 patent drawing

AI summary

The invention relates to substituted pyrimidine ammonia compounds. The structure of the compounds is represented as the general formula (I):The groups are as defined as specification.The compound represented by formula (I) can be used in the prevention of plants diseases caused by a plurality of pathogenic bacteria such as oomycota, basidiomycota, ascomycota, and fungi imperfecti, and due to these compounds have good bioactivity, which make them have very good effects at very low doses, especially more effective to powdery mildew of wheat. Therefore, the present invention relates to the use of the compounds having general formula I as fungicides, both in agriculture and other fields.