Active Carbonate Ester Synthesis via In-Situ Purification
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Solution Overview
Problem
Current methods for synthesizing water-soluble polymers with active ester groups are inefficient due to the need for excess low molecular weight reagents, which introduce impurities and reduce yields, and require multiple purification steps, making large-scale production costly and time-consuming.
Innovation Solution
A method involving the combination of an amine- or hydroxy-terminated water-soluble polymer with an excess of an activated carbonate reagent, followed by the addition of a reactive molecule to consume excess reagent, allowing for the formation of active carbonate esters without the need for additional purification steps.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If excess low molecular weight reagents are used in synthesis, then reaction completeness is improved, but product purity deteriorates due to introduced impurities
Solution Approach 1:
The patent applies extraction by using a purification step that removes low molecular weight reagents and impurities from the reaction mixture. The purified polymer is precipitated from the reaction solution, separating it from soluble impurities, thereby achieving high product purity while maintaining reaction completeness.
Solution Approach 2:
The patent changes physical parameters during purification, specifically using precipitation by adding a non-solvent to change the solubility parameters. This causes the polymer to precipitate while impurities remain in solution, enabling separation and purification without compromising reaction completeness.
2Manufacturing precision
If multiple purification steps are implemented, then product purity is improved, but production time and cost increase
Solution Approach 1:
The patent combines multiple purification objectives into a single precipitation step. By carefully selecting the precipitation conditions and non-solvent, the method simultaneously removes low molecular weight reagents, byproducts, and other impurities in one operation, avoiding the need for multiple sequential purification steps while maintaining high purity.
Solution Approach 2:
The purification method utilizes the inherent solubility differences between the polymer product and impurities. The polymer self-precipitates when the non-solvent is added, effectively purifying itself without requiring complex external purification equipment or multiple processing steps, thereby improving production efficiency.
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
This approach enables the efficient synthesis of active carbonate esters with high purity and yield, eliminating the need for multiple purification steps and reducing production costs, while allowing for the formation of water-soluble polymer-active agent conjugates with improved stability and reduced immunogenicity.
Implementation Method 1
combining an amine- or hydroxy-terminated water-soluble polymer with an excess of an activated carbonate reagent... to form active carbonate esters
Data Source
AI summary
Methods for preparing active carbonate esters of water-soluble polymers are provided. Also provided are other methods related to the active carbonate esters of water-soluble polymers, as well as corresponding compositions.