Dihydropyrimidine Compound Composition for Safe Microbial Control

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Solution Overview

Problem

Existing agricultural and horticultural fungicides face challenges in achieving high efficacy without causing drug resistance, phytotoxicity, soil contamination, and toxicity to livestock and fish, while also being industrially feasible to synthesize.

Innovation Solution

Development of 2,6-dioxo-3,6-dihydropyrimidine compounds with specific structural formulas and their salts, which exhibit excellent antimicrobial and bactericidal activity, suitable for use as active ingredients in fungicides, nematicides, and antifungal agents, ensuring safety and industrial synthesis.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing fungicide compounds are used to achieve high efficacy, then microbial control is improved, but drug resistance and phytotoxicity increase

Engineering Contradiction:
Improvemicrobial control efficacyVSAvoiddrug resistance and phytotoxicity
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent modifies the chemical structure of pyrimidine compounds by changing specific parameters (substituents at positions 5, 6, and nitrogen atoms) to achieve optimal balance between efficacy and safety. The general formula (I) with specific substituents represents parameter optimization to resolve the contradiction between microbial control and harmful effects.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates composite molecular structures by combining pyrimidine core with specific side chains and functional groups (formula I compounds). This composite approach allows integration of multiple functional characteristics: antimicrobial activity from the pyrimidine core and modified safety profile from the specific substituents.

Inventive Principle:
Principle #40Composite materials

2Productivity

If conventional fungicide synthesis methods are used, then production is achieved, but manufacturing complexity and cost increase

Engineering Contradiction:
Improvefungicide productionVSAvoidsynthesis process complexity
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent divides the synthesis process into modular steps: starting from commercially available pyrimidine derivatives and systematically adding specific substituents at defined positions. This segmentation allows each step to be optimized independently and facilitates scalable production.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs preliminary synthesis of key intermediates with predetermined structures, allowing the final active ingredients to be produced through straightforward transformations. This preliminary preparation simplifies the overall manufacturing process and reduces complexity.

Inventive Principle:
Principle #10Preliminary action

3Reliability

If existing agricultural chemicals are applied, then crop disease control is achieved, but toxicity to livestock and fish increases

Engineering Contradiction:
Improvecrop disease controlVSAvoidtoxicity to livestock and fish
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces specific local modifications at particular positions of the pyrimidine molecule (positions 5, 6, and nitrogen atoms) to create local functional zones that provide disease control activity while maintaining overall safety. The specific substituents at these locations are designed to achieve this localized functional differentiation.

Inventive Principle:
Principle #3Local quality

Data Source

PatentUS12593845B22,6-dioxo-3,6-dihydropyrimidine compound, agricultural and horticultural bactericide, nematicide, and medical and veterinary antifungal agent
Publication Date: 2026.04.07 NIPPON SODA CO LTD
  • US12593845B2 patent drawing
  • US12593845B2 patent drawing
  • US12593845B2 patent drawing

AI summary

An object of the present invention is to provide a 2,6-dioxo-3,6-dihydropyrimidine compound that has excellent bactericidal and antimicrobial activity, has excellent safety, and can be industrially favorably synthesized, and an agricultural and horticultural fungicide, a nematicide, and an antifungal agent for use in medicine/animals that contain the compound as an active ingredient.