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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: 2006-11-01
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 l

[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 the 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 remo...

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. Adopt the method of centrifugal separation to separate the immobilized enzyme preparation from the completed reaction liquid, and then distill the cleared finished reaction liquid to recover the tert-butanol solvent. The distilled product is crystallized, centrifuged,...

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Abstract

The invention provides a method for enzymatically preparing inositol nicotinate, comprising the following steps: dehydrating tert-butanol, activating 4A molecular sieves in a drying oven, cooling in a desiccator, adding tert-butanol, and filtering Dehydrated tert-butanol is obtained after molecular sieve; lipase catalyzed reaction is carried out in dehydrated tert-butanol, and inositol, nicotinic acid and immobilized lipase Novozyme435 are added to dehydrated tert-butanol to form a reaction system, and non-aqueous lipase catalyzed reaction is carried out; The obtained reaction completion liquid is refined to obtain inositol nicotinate product; the invention adopts non-aqueous phase enzyme catalyzed reaction to prepare inositol nicotinate, the reaction conversion rate is high, the recycling of enzyme preparation and organic solvent is realized, and the preparation process is simplified. No waste liquid, no pollution, easy to realize clean production; using the difference in solubility of the product and the substrate in water, it is easy to realize the separation and purification of the product, the refining separation and purification process is greatly simplified, and the refining cost is reduced by more than 10%.

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 v...

Claims

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Application Information

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Patent Type & Authority Patents(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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