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Preparation method of inositol nicotinate by enzyme method

A technology for the preparation of inositol nicotinate and enzymatic method, which is applied in the field of enzymatic preparation of inositol nicotinate, can solve the problems of difficult refining separation and purification, high production cost, solvent residue, etc., and achieve the simplification of refining separation and purification process, refining Effect of cost reduction and simplification of production process

Inactive Publication Date: 2004-11-17
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since the end of the 1980s, foreign patents have expired one after another, and many countries, including some pharmaceutical factories in my country, have begun to imitate them. However, there are still problems such as low esterification rate, difficult refining separation and purification, solvent residues, and high production costs.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] (1) tert-butanol is dehydrated. Activate the 4A molecular sieve in a drying oven at 180°C for 3 hours, cool it in a desiccator, add it to tert-butanol, filter out the molecular sieve to obtain dehydrated tert-butanol;

[0019] (2) Carry out lipase-catalyzed reaction in dehydration tert-butanol. 1.0mmol / L inositol, 6.0mmol / L nicotinic acid and 5g / L immobilized lipase Novozyme435 were added to dehydrated tert-butanol to form a reaction system, and the non-aqueous phase lipase catalyzed reaction was carried out at a temperature of 40°C. Reaction 12 hours, the esterification rate of inositol nicotinate was 89.3%.

[0020] (3) The reaction completed liquid is further refined to obtain the inositol nicotinate product. The immobilized enzyme preparation is separated from the completed reaction liquid by centrifugation, and the cleared reaction liquid is then distilled to recover the tert-butanol solvent. The distilled product is crystallized, centrifuged, and washed with dis...

Embodiment 2

[0022] (1) tert-butanol is dehydrated. Activate the 4A molecular sieve in a drying oven at 200°C for 2 hours, cool it in a desiccator, add it to tert-butanol, filter out the molecular sieve to obtain dehydrated tert-butanol;

[0023] (2) Carry out lipase-catalyzed reaction in dehydration tert-butanol. Add 1.5mmol / L inositol, 8mmol / L nicotinic acid and 4g / L immobilized lipase Novozyme435 to dehydrated tert-butanol to form a reaction system, and carry out non-aqueous phase lipase-catalyzed reaction at a temperature of 45°C for 10 hours , the esterification rate of inositol nicotinate was 86.4%.

[0024] (3) The reaction completed liquid is further refined to obtain the inositol nicotinate product. The immobilized enzyme preparation is separated from the completed reaction liquid by centrifugation, and the cleared reaction liquid is then distilled to recover the tert-butanol solvent. The distilled product is crystallized, centrifuged, and washed with distilled water to remove i...

Embodiment 3

[0026] (1) tert-butanol is dehydrated. Activate the 4A molecular sieve in a drying oven at 190°C for 2.5 hours, cool it in a desiccator, add it to tert-butanol, and filter out the molecular sieve to obtain dehydrated tert-butanol;

[0027] (2) Carry out lipase-catalyzed reaction in dehydration tert-butanol. Add 1.2mmol / L inositol, 7.0mmol / L nicotinic acid and 6g / L immobilized lipase Novozyme435 to dehydrated tert-butanol to form a reaction system, and carry out the non-aqueous phase lipase-catalyzed reaction at a temperature of 35°C. Reaction 8 hours, the esterification rate of inositol nicotinate was 87.6%.

[0028] (3) The reaction completed liquid is further refined to obtain the inositol nicotinate product. The immobilized enzyme preparation is separated from the completed reaction liquid by centrifugation, and the cleared reaction liquid is then distilled to recover the tert-butanol solvent. The distilled product is crystallized, centrifuged, and washed with distilled w...

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PUM

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Abstract

The invention provides a process for preparing inositol nicotinate through enzymatical method which comprises the steps of, tert-butanol dehydration, activating the 4A molecular sieve in a drying cabinet, placing into the drying apparatus and cooling, charging into tert-butanol, filtering the molecular screen to obtain dehydration tert-butanol, carrying out lipolytic enzyme catalytic reaction into the dehydration tert-butanol, charging inositol nicotinate, nicotinic acid and immobilized lipolytic enzyme Novozyme435 to compose the reaction system, carrying out non-aqueous phase lipolytic enzyme catalytic reaction, refining the prepared reaction liquid to obtain the inositol nicotinate product.

Description

technical field [0001] The invention relates to a method for preparing inositol nicotinic acid ester by enzymatic method, and more specifically refers to a method for preparing inositol nicotinic acid ester by using inositol and nicotinic acid as raw materials and carrying out an enzyme-catalyzed reaction in a non-aqueous solvent. Background technique [0002] Inositol nicotinic acid ester is an important derivative of inositol, which can promote the metabolism of fat in the liver and tissues, lower blood lipids and expand peripheral blood vessels of nicotinic acid. Drugs for senile dementia, fatty liver, etc. can also be used in conjunction with other drugs; at the same time, it has a sustained release effect, slowly decomposed into inositol and niacin in the body, and the drug effect is stable for a long time, which solves the vasodilation that exists when niacin is used alone If the speed is too fast, it will easily cause the side effect of blood...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12P17/06
Inventor 扶雄杨连生罗发兴李文治
Owner SOUTH CHINA UNIV OF TECH
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