Parallel Saccharide Synthesis via Vapor-Phase Glycosylation

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Solution Overview

Problem

Current methods for synthesizing saccharides are laborious and costly, limiting the availability of complex saccharide libraries needed for high-throughput screenings and diagnostics, as they require sequential and time-consuming processes, making it difficult to access high-density saccharide arrays for identifying biomarkers and vaccine development.

Innovation Solution

A method involving the application of saccharide building blocks onto a solid support followed by a vapor of a glycosylation reagent at low temperatures to initiate coupling reactions, allowing for simultaneous synthesis of saccharides at discrete locations, thereby enabling cost-effective and efficient high-throughput synthesis of saccharides and high-density arrays.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If traditional sequential synthesis methods are used for saccharides, then each saccharide can be synthesized step-by-step, but the process becomes laborious and time-consuming, limiting the number of saccharides that can be produced

Engineering Contradiction:
Improvethroughput of saccharide synthesisVSAvoidtime required for sequential synthesis
Core Design Contradiction:
ProductivityVSLoss of time

Solution Approach 1:

The solid support is divided into multiple discrete locations, each capable of holding a different saccharide building block. This segmentation allows parallel synthesis of multiple saccharides simultaneously at different locations, transforming a sequential process into a parallel one and dramatically increasing throughput while reducing total synthesis time.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

Multiple saccharide building blocks are applied to different locations on the same solid support and subjected to a common vapor-phase glycosylation reaction. This merging of multiple synthesis operations into a single parallel process enables simultaneous production of multiple saccharides, resolving the contradiction between productivity and time loss.

Inventive Principle:
Principle #5Merging (Combining)

2Adaptability or versatility

If complex saccharide libraries are synthesized using traditional methods, then structurally diverse saccharides can be produced, but the costs become very high (up to thousands of euros per substance)

Engineering Contradiction:
Improvediversity of saccharide libraryVSAvoidcost of synthesis
Core Design Contradiction:
Adaptability or versatilityVSEase of manufacture

Solution Approach 1:

A single solid support serves as a universal platform that can simultaneously produce multiple different saccharides through parallel vapor-phase reactions. This multi-functional approach allows one synthesis system to generate diverse saccharide libraries that would otherwise require multiple separate synthesis processes, reducing overall costs while maintaining structural diversity.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Solution Approach 2:

The vapor-phase glycosylation method creates identical reaction conditions across multiple discrete locations on the solid support, effectively copying the synthesis process for each saccharide. This allows parallel production of multiple saccharide variants at reduced cost compared to sequential synthesis, as reagents and conditions are replicated efficiently across all locations.

Inventive Principle:
Principle #26Copying

3Quantity of substance

If high-density saccharide arrays are produced for high-throughput screenings, then biomarkers can be identified more efficiently, but traditional synthesis methods cannot provide sufficient density due to sequential processing limitations

Engineering Contradiction:
Improvedensity of saccharide arrayVSAvoidthroughput of array synthesis
Core Design Contradiction:
Quantity of substanceVSProductivity

Solution Approach 1:

The synthesis approach transitions from sequential time-based production to parallel spatial-based production on the solid support. By distributing multiple saccharide building blocks across discrete spatial locations and applying vapor-phase reagents simultaneously, the method achieves high-density arrays with improved throughput, utilizing spatial dimensionality to overcome sequential processing limits.

Inventive Principle:
Principle #17Another dimension (Dimensionality change)

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 rapid and cost-effective synthesis of saccharides and high-density arrays, facilitating the identification of biomarkers and vaccine development by allowing for the simultaneous synthesis of multiple saccharides at discrete locations on a solid support, reducing the complexity and time associated with traditional methods.

Implementation Method 1

The vapor condenses on the solid support and initiates the coupling reaction

Methodology Applied
Scientific EffectCondensation: Condensation

Data Source

PatentUS11772063B2Method and device for producing saccharides and saccharide arrays
Publication Date: 2023.10.03 MAX PLANCK GESELLSCHAFT ZUR FOERDERUNG DER WISSENSCHAFTEN EV
  • US11772063B2 patent drawing
  • US11772063B2 patent drawing
  • US11772063B2 patent drawing

AI summary

The present invention relates to a method and a device for producing saccharides and saccharide arrays. Said method is particularly useful for the synthesis of saccharides in parallel and of high-density saccharide arrays, such as microarrays, which are required for high-throughput screenings.