Cyclopeptide Synthesis Using Water-Soluble Catalyst
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
The high cost of coupling agents in conventional methods for preparing peptides with the RGD motif limits their widespread application in various fields, including pharmaceutical and cosmetic uses, due to the expensive nature of these agents.
Innovation Solution
A novel cyclopeptide with the RGD motif is developed, along with a bio-compatible, catalytic method for its preparation, using a water-soluble catalyst to reduce the need for expensive coupling agents, thereby lowering production costs and making the peptide more accessible for use in pharmaceutical and cosmetic compositions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If conventional coupling agents are used to catalyze peptide synthesis, then the peptide can be produced, but the production cost becomes high
Solution Approach 1:
The patent replaces expensive, traditional coupling agents with a inexpensive water-soluble catalyst system that can be used in catalytic amounts. The catalyst enables peptide bond formation without requiring stoichiometric amounts of expensive reagents, thereby significantly reducing production costs while maintaining effectiveness.
Solution Approach 2:
The invention changes the chemical parameters of the coupling reaction by using a water-soluble catalyst system with different mechanistic properties compared to conventional coupling agents. This allows the reaction to proceed under milder, more cost-effective conditions while achieving the same peptide synthesis objective.
2Reliability
If expensive coupling agents are used in peptide synthesis, then the peptide can be obtained, but the peptide becomes unavailable to all
Solution Approach 1:
By replacing expensive coupling agents with an inexpensive water-soluble catalyst, the invention makes peptide synthesis accessible to a broader range of applications and users. The cost reduction enables widespread use in pharmaceutical and cosmetic industries that previously could not afford conventional methods.
Solution Approach 2:
The water-soluble catalyst system demonstrates broad applicability to synthesizing various peptides containing the RGD motif, making the method universally applicable across different peptide sequences and applications, thereby increasing adaptability and versatility.
3Productivity
If conventional peptide synthesis methods are used, then the peptide can be produced, but the process becomes costly and less accessible
Solution Approach 1:
The invention employs a cost-effective water-soluble catalyst that can be used in catalytic cycles, reducing the amount of expensive reagents needed. This approach maintains high productivity in peptide production while significantly lowering the cost per unit of peptide produced.
Solution Approach 2:
The water-soluble catalyst system is designed to be easily removable from the reaction mixture through simple filtration or dialysis, eliminating the need for complex purification steps. This self-service characteristic reduces both time and cost while maintaining high productivity.
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 novel cyclopeptide can bind to the integrin RGD binding site, enhancing communication between the dermis and epidermis, stimulating protein production, and is effective in treating scars, wounds, inflammation, aging, and wrinkle formation, making it suitable for topical skin care applications.
Implementation Method 1
the cyclopeptide of the present invention binds to the intergrin RGD binding site
Implementation Method 2
a cyclization reaction of the compound of formula (II-5) or (II′-5) is performed with a catalyst of formula (III), to obtain a compound represented by the formula (I) or (I′)
Data Source
AI summary
A cyclopeptide is disclosed, which is represented by the following formula (I) or (I′):wherein R1 and G′ are defined in the specification. In addition, a pharmaceutical or cosmetic composition comprising the same and a method for preparing the same are also disclosed.