Fructoborate Di-Complex Synthesis Yield Optimization

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Solution Overview

Problem

Current methods for producing calcium fructoborate (CF) and other borocarbohydrate complexes face challenges in achieving high yields with low residual boric acid and fructose content, and optimal di-complex to free boric acid ratios, which are essential for biological relevance and safety.

Innovation Solution

A method involving reacting fructose with boric acid in water, followed by neutralization with an alkaline or earth alkaline metal hydroxide or carbonate, at a molar ratio of at least 1.8:1 and a preparative scale of at least 1000 ml, to form a composition with a di-complex to boric acid ratio of at least 10:1, thereby maximizing di-complex content and minimizing residual boric acid.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If conventional synthesis methods are used, then calcium fructoborate can be produced, but the yield is low and residual boric acid content is high

Engineering Contradiction:
Improveyield of calcium fructoborateVSAvoidresidual boric acid content
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by optimizing the molar ratio of fructose to boric acid (1.8:1 to 2.4:1), controlling reaction temperature (60-80°C), adjusting pH levels during neutralization, and specifying reaction time (1-3 hours). These parameter optimizations simultaneously increase di-complex yield and reduce residual boric acid content to below 10 wt%, resolving the contradiction between productivity and harmful residual content.

Inventive Principle:
Principle #35Parameter changes

2Manufacturing precision

If conventional synthesis methods are used, then calcium fructoborate can be produced, but the ratio of di-complex to mono-complex is unfavorable

Engineering Contradiction:
Improveratio of di-complex to mono-complexVSAvoidyield of di-complex calcium fructoborate
Core Design Contradiction:
Manufacturing precisionVSProductivity

Solution Approach 1:

The patent uses parameter changes to achieve both high manufacturing precision and productivity. By controlling the molar ratio of fructose to boric acid within 1.8:1 to 2.4:1, maintaining reaction temperature at 60-80°C, and adjusting pH to 6.5-7.5 during neutralization, the process achieves a di-complex to mono-complex ratio of at least 10:1 while maintaining high overall yield through optimized reaction conditions.

Inventive Principle:
Principle #35Parameter changes

3Manufacturing precision

If conventional synthesis methods are used, then calcium fructoborate can be produced, but the di-complex to boric acid ratio is low

Engineering Contradiction:
Improvedi-complex to boric acid ratioVSAvoidtoxicity concerns from boric acid
Core Design Contradiction:
Manufacturing precisionVSObject-affected harmful factors

Solution Approach 1:

The patent achieves a di-complex to boric acid ratio of at least 10:1 through parameter optimization including molar ratio control (1.8:1 to 2.4:1), temperature control (60-80°C), and pH adjustment (6.5-7.5). This simultaneously improves manufacturing precision by ensuring the desired complex formation while reducing toxic boric acid residues to below 10 wt%, addressing both the ratio requirement and safety concerns.

Inventive Principle:
Principle #35Parameter changes

4Device complexity

If small scale synthesis is used, then reaction complexity can be managed, but the process is not suitable for preparative production

Engineering Contradiction:
Improvereaction control complexityVSAvoidpreparative scale production capacity
Core Design Contradiction:
Device complexityVSProductivity

Solution Approach 1:

The patent applies segmentation by dividing the synthesis process into distinct controlled stages: (1) mixing fructose and boric acid in specific molar ratios, (2) heating at controlled temperatures for specific durations, (3) neutralization in stages with pH monitoring, and (4) filtration and concentration. This segmentation allows the process to be scaled from small to preparative volumes (at least 1000 ml) while maintaining manageable complexity through standardized procedural steps.

Inventive Principle:
Principle #1Segmentation

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 results in a composition with a high content of di-complexes (>65 wt%), low residual boric acid (<10 wt%), and a favorable di-complex to mono-complex ratio, enhancing the biological relevance and safety of the product.

Implementation Method 1

the boric acid molecule forms diester complex bonds with two hydroxyl groups of a sugar molecule

Methodology Applied
Scientific EffectEsterification: Chemical Bonding

Implementation Method 2

neutralizing the reaction with at least one of an alkaline metal hydroxide, an earth alkaline metal hydroxide, an alkaline metal carbonate, and an earth alkaline metal carbonate to provide a cation to form a salt of the fructose complexes

Methodology Applied
Scientific EffectNeutralization: Chemical Bonding

Implementation Method 3

drying the liquid composition to generate a dry product comprising fructoborate dicomplexes and borate

Methodology Applied
Scientific EffectEvaporation: Evaporation

Data Source

PatentEP3210628A1Improved compositions and methods for fructoborate complexes
Publication Date: 2017.08.30 VDF FUTURECEUTICALS INC
  • EP3210628A1 patent drawingFigure 1A~1C
  • EP3210628A1 patent drawingFigure 2A~2B
  • EP3210628A1 patent drawingFigure 3A~3B

AI summary

The present invention relates to a method of increasing di-complex content in a preparative reaction wherein the fructoborate complexes are a mixture of di-complexes and mono complexes, the method comprising: selecting a molar ratio between a fructose and boric acid of about 2:1; contacting the fructose and boric acid in an aqueous solution at the molar ratio to generate a liquid intermediate comprising fructoborate di-complexes and borate; and removing water from the liquid intermediate to generate a dry product comprising fructoborate di-complexes and borate, wherein the ratio of sodium fructoborate di-complexes to borate in the dry product is increased by at least about 13% relative to the ratio of sodium fructoborate di-complexes to borate in the liquid intermediate.