Insecticide Polymorph Stability and Crystal Growth Control
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Solution Overview
Problem
Existing N-alkyl amide substituted spiroheterocyclic pyrrolidine dione derivatives have limitations in their solid forms, leading to instability and unwanted crystal growth in formulations, which affects their physical and biological properties, making them less effective as insecticides.
Innovation Solution
Development of novel crystalline polymorphs with specific unit cell parameters and powder X-ray diffraction patterns, characterized by unique 2θ angle values and melting points, which are more stable and suitable for agrochemical compositions, enhancing their physical and biological properties.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing solid forms of N-alkyl amide substituted spiroheterocyclic pyrrolidine dione derivatives are used, then they can be formulated as insecticides, but they exhibit instability and unwanted crystal growth affecting physical and biological properties
Solution Approach 1:
The patent applies parameter changes by discovering and characterizing new polymorphic forms (Form I, Form II, Form III) with distinct unit cell parameters, space groups, and powder X-ray diffraction patterns. Each polymorph exhibits different physical properties including melting points (120°C, 133°C, and 145°C respectively), allowing selection of the most stable form for formulation purposes. This resolves the contradiction by providing multiple crystalline options with optimized stability characteristics.
2Productivity
If existing solid forms are used, then they can provide insecticidal activity, but they show unwanted crystal growth that reduces efficacy and increases phytotoxicity
Solution Approach 1:
The patent applies preliminary action by pre-characterizing and selecting specific polymorphic forms with optimal stability profiles before formulation. By identifying polymorphs with defined melting points and crystal structures that resist unwanted transformation, the invention prevents crystal growth issues before they occur in the formulation. This ensures consistent insecticidal efficacy while minimizing phytotoxicity risks associated with crystal transformation.
3Duration of action of stationary object
If existing solid forms are used, then they can be stored as insecticide formulations, but they exhibit reduced shelf life due to instability and crystal growth
Solution Approach 1:
The patent applies beforehand cushioning by selecting polymorphic forms with higher thermal stability margins (elevated melting points of 120°C, 133°C, and 145°C) that provide a buffer against temperature fluctuations during storage and transport. This preemptive selection of thermally stable forms cushions the formulation against degradation and unwanted crystal transformations, thereby extending shelf life while maintaining physical property stability.
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 new polymorphs provide improved stability and efficacy as insecticides, allowing for effective control of pests with reduced phytotoxicity and prolonged shelf life, preventing unwanted crystal growth and maintaining formulation stability.
Implementation Method 1
The crystalline polymorph may also be characterised by a powder X-ray diffraction pattern expressed in terms of 2θ angles or d spacings
Implementation Method 2
a powder X-ray diffraction pattern comprising one 2θ angle value at 9.4±0.2, one 2θ angle value at 10.3±0.2 and at least three, at least six, at least nine, at least twelve, at least fifteen or all 2θ angle values
Data Source
AI summary
The present invention relates to solid forms of the insecticide of formula (I):compositions comprising the solid forms and methods of their use as insecticides.