APC Hydrochloride Hemihydrate Crystallization for Low-Impurity Stability
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Solution Overview
Problem
Existing methods for producing (R)-2-amino-3-phenylpropyl carbamate (APC) hydrochloride result in high levels of contaminants, particularly 2-chloropropane, and lack a stable solvate form suitable for effective treatment of disorders.
Innovation Solution
The development of a hemihydrate solvate form of APC hydrochloride (Form B) prepared by slurrying in acetonitrile/water and minimizing 2-chloropropane contamination through controlled crystallization with aqueous HCl, along with formulations for improved purity and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Manufacturing precision
If conventional methods are used to produce APC hydrochloride, then production process is simple, but high levels of contaminants (particularly 2-chloropropane) are generated
Solution Approach 1:
The patent extracts and removes harmful contaminants (2-chloropropane) from the production process by implementing specific purification steps and process modifications that separate the desired APC hydrochloride from harmful byproducts, achieving high purity while eliminating harmful factors
Solution Approach 2:
The patent changes critical process parameters (temperature, pH, solvent composition) during crystallization and purification steps to optimize the separation of APC hydrochloride from contaminants, enabling high purity production by controlling physical and chemical parameters
2Stability of the object's composition
If conventional production methods are used, then manufacturing process is straightforward, but the product lacks stable solvate form and has poor stability
Solution Approach 1:
The patent identifies and utilizes specific parameter conditions (solvent composition, temperature, concentration) that promote the formation of stable solvate forms (hemihydrate, monohydrate) during crystallization, transforming the product into a stable form without requiring overly complex manufacturing processes
Solution Approach 2:
The patent introduces water as an intermediary substance that forms stable solvate structures with APC hydrochloride, using water molecules as mediators to stabilize the crystal structure and improve product stability through controlled hydration
3Reliability
If conventional methods are used, then production is efficient, but impurities reduce effectiveness and patient compliance
Solution Approach 1:
The patent extracts and removes impurities that would otherwise reduce treatment effectiveness, implementing purification steps that eliminate contaminants while maintaining high production efficiency through optimized process design
Solution Approach 2:
The patent incorporates monitoring and analysis steps that provide feedback on product purity and quality, allowing for real-time process adjustment to ensure both high effectiveness and efficient production by identifying and correcting issues promptly
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 solvate form (Form B) provides increased purity and stability, allowing for effective treatment of disorders with reduced impurities and improved patient compliance through controlled release dosage forms.
Implementation Method 1
The invention further relates to a process of preparing a solvate form of APC hydrochloride, comprising slurrying APC hydrochloride in acetonitrile/water (95%/5% v/v) and collecting the solvate by vacuum filtration.
Implementation Method 2
a new solvate form of APC and a method of preparing APC with minimal contaminants
Implementation Method 3
The present invention relates to the identification of a novel solvate form of APC which is a hemihydrate form
Implementation Method 4
collecting the solvate by vacuum filtration
Data Source
AI summary
The present invention relates to a newly identified solvate form of (R)-2-amino-3-phenylpropyl carbamate (APC) hydrochloride, a method of preparing APC hydrochloride, and methods of using the same to treat disorders. The invention further relates to methods of producing APC hydrochloride with increased purity.