Aqueous Peptide Synthesis with Water-Soluble Condensing Agents

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Solution Overview

Problem

Existing solid-phase peptide synthesis methods consume large amounts of organic solvents and require additional steps or specialized equipment when using aqueous solutions, limiting their applicability and efficiency.

Innovation Solution

A peptide synthesis method involving a mixed dispersion of protected amino acids, a base, a water-soluble condensing agent, and an aqueous solvent is used to facilitate a condensation reaction, eliminating the need for surfactants and specialized equipment.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If aqueous solutions are used in solid-phase peptide synthesis methods, then environmental impact is reduced and solvent consumption is lowered, but additional steps or specialized equipment are required, increasing operational complexity

Engineering Contradiction:
Improveenvironmental impactVSAvoidoperational complexity
Core Design Contradiction:
Object-affected harmful factorsVSEase of operation

Solution Approach 1:

The patent uses surfactants as intermediary substances to enable the condensation reaction between protected amino acids and peptides in aqueous media. The surfactant forms micelles that solubilize the hydrophobic protected amino acids and facilitate their reaction with peptides, thereby allowing environmentally friendly aqueous synthesis without requiring specialized equipment or complex additional steps

Inventive Principle:
Principle #24Intermediary (Mediator)

2Extent of automation

If conventional solid-phase peptide synthesis methods are used, then peptide synthesis can be automated, but large amounts of organic solvents are consumed

Engineering Contradiction:
Improveautomation capabilityVSAvoidsolvent consumption
Core Design Contradiction:
Extent of automationVSLoss of substance

Solution Approach 1:

The patent changes the fundamental parameter of the reaction medium from organic solvents to aqueous solutions. By using water as the solvent and incorporating surfactants to enable reactant solubility and reaction efficiency, the method maintains automation capability while dramatically reducing organic solvent consumption and eliminating the need for repeated washing steps

Inventive Principle:
Principle #35Parameter changes

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 method achieves simpler, more efficient, and environmentally friendly peptide synthesis with high purity in aqueous solvents, reducing solvent consumption and operational complexity.

Implementation Method 1

allowing a condensation reaction between the protected amino acid for peptide synthesis and the amino acid and/or the peptide

Methodology Applied
Scientific EffectCondensation reaction:

Data Source

PatentEP4596568A1Peptide synthesis method
Publication Date: 2025.08.06 KOBE GAKUIN EDUCATIONAL FOUND
  • EP4596568A1 patent drawingFigure 1
  • EP4596568A1 patent drawingFigure 2
  • EP4596568A1 patent drawingFigure 3

AI summary

Provided is a peptide synthesis method that is simpler, more efficient, and/or has a lower environmental impact. The peptide synthesis method includes bringing a mixed dispersion of a protected amino acid for peptide synthesis, a base, a water-soluble condensing agent, and an aqueous solvent into contact with an amino acid and/or a peptide to allow a condensation reaction between the protected amino acid for peptide synthesis and the amino acid and/or the peptide.