Spirodiclofen Crystalline Modification I Storage Stability
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Solution Overview
Problem
The commercially available spirodiclofen in its amorphous state has a high tendency to aggregate during prolonged storage, making it unsuitable for formulations and requiring a novel form with improved storage stability.
Innovation Solution
A novel crystalline form of spirodiclofen, termed 'crystalline modification I', is developed through a process involving dissolution in solvents like toluene or acetone, followed by crystallization, which enhances storage stability and allows for easier filtration and grinding, enabling the preparation of stable formulations such as suspension concentrates and water-dispersible granules.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If spirodiclofen is manufactured in amorphous state, then it can be produced by conventional processes, but it exhibits high tendency of aggregation after prolonged storage
Solution Approach 1:
The patent changes the physical state parameter of spirodiclofen from amorphous to crystalline form. This parameter change fundamentally alters the molecular arrangement and intermolecular forces, resulting in improved storage stability and reduced aggregation tendency while maintaining manufacturability through established crystallization processes
Solution Approach 2:
The invention utilizes phase transition from amorphous to crystalline state during the formulation process. By controlling crystallization conditions (solvent selection, temperature, evaporation rate), the spirodiclofen transforms from a disordered amorphous phase to an ordered crystalline phase, which provides enhanced stability and reduced aggregation during storage
2Adaptability or versatility
If spirodiclofen is used in amorphous form, then it can be prepared by existing methods, but it is not suitable for being prepared as compositions or formulations
Solution Approach 1:
The patent modifies the physical state parameter of spirodiclofen from amorphous to crystalline, which fundamentally improves its suitability for formulation. The crystalline form provides better compatibility with various formulation excipients, carriers, and adjuvants while maintaining stability during storage and application
3Reliability
If crystalline modification I is used, then storage stability is improved with reduced aggregation, but additional crystallization steps are required
Solution Approach 1:
The patent performs preliminary crystallization action during the synthesis process itself. By selecting appropriate solvents and controlling crystallization conditions in advance, the spirodiclofen is converted to its stable crystalline modification I form before formulation, preventing aggregation issues downstream without requiring separate stabilization steps
Solution Approach 2:
The patent uses solvents as intermediaries to facilitate the transformation from amorphous to crystalline form. Solvents like ethanol, methanol, or acetone serve as mediators that enable controlled crystallization during the formulation process, achieving the desired crystalline modification I without complex additional processing steps
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 modification I of spirodiclofen exhibits improved storage stability with reduced aggregation, allowing for longer storage periods of formulations and easier processing into commercial formulations like suspension concentrates and water-dispersible granules.
Implementation Method 1
A novel crystalline form of spirodiclofen, termed 'crystalline modification I', is developed through a process involving dissolution in solvents like toluene or acetone, followed by crystallization
Data Source
AI summary
A new crystalline form of spirodiclofen of formula (I), the crystal preparation process, the analyzes of the crystal through various analytical methods and using the crystal to prepare stable agrochemical formulation. The invention also describes the use of various solvents towards the crystalline form preparation conditions.