Polymorphs of 5-fluoro-4-imino-3-methyl-1 -tosyl-3,4-dihydropyrimidin-2-one
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Solution Overview
Problem
Current fungicides, such as 5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, face challenges in providing effective control against various fungal pathogens in crops, particularly due to limitations in stability and solubility, which affect their efficacy and application methods.
Innovation Solution
Development of crystalline forms, including polymorphs, hydrates, and solvates of 5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, characterized by distinct spectral characteristics, which are more stable and soluble, allowing for improved control of fungal attacks on plants by application to roots, seeds, or foliage.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional fungicides are used, then fungal control is achieved, but stability and solubility are insufficient
Solution Approach 1:
The patent applies parameter changes by discovering and characterizing multiple polymorphic forms (Forms I, II, III, IV, V) and solvates (ethanol solvate, acetone solvate, isopropanol solvate) of the fungicide compound. Each polymorph and solvate exhibits distinct physical properties including solubility, stability, and crystalline structure, allowing selection of the optimal form for specific agricultural applications while maintaining the core fungicidal activity.
Solution Approach 2:
The patent creates composite material systems by formulating the fungicide in various crystalline forms combined with carriers and adjuvants. These composite formulations (emulsifiable concentrates, wettable powders, soluble concentrates, suspension concentrates) integrate the active ingredient in specific polymorphic forms with excipients that enhance solubility, stability, and delivery efficiency to crops.
2Reliability
If fungicide application is increased to improve control, then fungal pathogen control improves, but crop quality and value may be affected
Solution Approach 1:
The patent applies local quality by developing targeted formulations that deliver the fungicide in optimized polymorphic forms to specific plant parts (foliage, roots, seeds) where fungal threats are most critical. This localized delivery ensures effective fungal control at application sites while minimizing unnecessary exposure and potential quality impacts on other crop portions.
Solution Approach 2:
The patent employs disposable application formulations (emulsifiable concentrates, wettable powders, soluble concentrates, suspension concentrates) that are designed for single-use application. These formulations provide effective fungal control during the critical growth period and are then naturally degraded or washed away, avoiding long-term accumulation that could affect crop quality.
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 crystalline forms exhibit enhanced stability and solubility, leading to effective control of fungal pathogens like Septoria tritici and other economically important fungal diseases, with improved application methods that maintain crop quality and value.
Implementation Method 1
The present invention provides a crystalline form of the compound having the following structure:
Implementation Method 2
The present invention provides a crystalline form of the compound... The present invention also provides a fungicidal composition comprising a solution of the compound
Data Source
AI summary
The present subject matter provides a crystalline form of the compound having the following structure:wherein the crystalline form is a polymorph, hydrate or solvate.