Ionic Liquid Support for Peptide Synthesis Kinetics
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Solution Overview
Problem
Current methods for peptide synthesis using solid supports face issues such as increased steps for protection and deprotection, separation problems, non-linear reaction kinetics, low loading capacity, and high costs due to the use of auxiliary reagents and viscous ionic liquids, particularly when synthesizing peptides with multiple acidic or basic functionalities.
Innovation Solution
A functionalized ionic liquid-based support is developed, combining a heteroatom-containing cationic part with a halogen-containing polymeric solid support, followed by anion metathesis, to create an ionic liquid support that minimizes the use of volatile organic solvents and auxiliary reagents, allowing for efficient peptide synthesis with improved kinetics and yield.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If solid support materials are used for peptide synthesis, then easy purification and separation are achieved, but non-linear reaction kinetics and low loading capacity occur
Solution Approach 1:
The patent changes the physical state parameter of the support material from solid to liquid (ionic liquid), which fundamentally alters the reaction kinetics from non-linear to more uniform rates while maintaining the ability to separate and purify products through phase separation or extraction methods
2Adaptability or versatility
If viscous ionic liquids are used as support, then peptide synthesis is enabled, but reaction kinetics are retarded
Solution Approach 1:
The patent modifies the viscosity parameter of the ionic liquid support by selecting specific ionic liquid compositions and structures, achieving an optimal balance between maintaining peptide synthesis capability and ensuring adequate reaction kinetics through reduced viscosity
3Ease of manufacture
If auxiliary reagents like dehydrating and activating agents are used, then peptide bond formation is facilitated, but process cost and complexity increase
Solution Approach 1:
The patent extracts and eliminates the need for separate dehydrating and activating agents by incorporating their functional properties directly into the ionic liquid support structure, simplifying the overall process while maintaining peptide bond formation efficiency
4Productivity
If conventional homogeneous phase routes are used, then reaction kinetics are fast, but purification of excess reagents becomes difficult
Solution Approach 1:
The patent introduces an ionic liquid as an intermediary medium that provides homogeneous-phase reaction kinetics while enabling easy purification through its unique properties such as immiscibility with organic solvents or tunable solubility characteristics
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 ionic liquid-based support facilitates faster kinetics, higher yields, and reduced racemization, enabling the synthesis of peptides with multiple functionalities, while minimizing the use of dehydrating and activating agents, thus overcoming the limitations of existing methods.
Implementation Method 1
attaching a heteroatom containing cationic part (X+) of an ionic liquid with a halogen containing polymeric solid support
Implementation Method 2
subjecting the washed solid product to anion metathesis using an anionic source
Data Source
AI summary
The present invention relates to an ionic liquid based support of Formula-I: wherein: X+ is a heteroatom containing cationic part; W is a halogen containing polymeric solid support; n is an integer in the range of 2 to 8; Y is a hydrophobic anion; R is selected from CO—Z or Z; Z is selected from the group consisting of —Cl, —Br, —OH, —O-Alkyl and combinations thereof. The present invention also relates to a process for preparation of said ionic liquid based support used for di, oligo or polypeptide manufacture.