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Production method of benfotiamine

A technology of benfotiamine and its production method, which is applied in the fields of chemical instruments and methods, compounds of group 5/15 elements of the periodic table, organic chemistry, etc., and can solve the difficulty of direct precipitation of vitamin B1 phosphate monoester products and the potential safety hazards , Inconvenient hydrolysis operation, etc., to achieve the effect of reducing solvent consumption, reducing production costs, and reducing emissions

Active Publication Date: 2014-05-07
HUBEI RUISI TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The separated solid phosphate is mixed with products, which brings about a large loss
[0007] Phosphorus oxychloride in CN102911208 is used as a phosphating agent, because the activity of phosphorus oxychloride is too high, the hydrolysis operation is inconvenient, and there are potential safety hazards. After the phosphatization is completed, it is very difficult to directly separate out the vitamin B1 phosphate monoester product which is hydrolyzed, which is not conducive to operation.

Method used

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  • Production method of benfotiamine

Examples

Experimental program
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Effect test

Embodiment 1

[0027] After adding 4000kg polyphosphoric acid into the reaction kettle, raise the temperature to 100-120°C, add 1000kg of vitamin B1 to the reaction kettle in batches, keep it in this temperature range for 8 hours after adding, add 3000kg of water to quench After the reaction, heat up to 80-90°C for 10 hours of hydrolysis; cool down to room temperature, add 5000kg of trioctylamine / methyl tert-butyl ether = 1 / 1 mixture to extract phosphoric acid; add 5000kg of methanol to the water phase Precipitate solids and centrifuge to obtain 1200kg of crude vitamin B1 phosphate monoester; mix 1200kg of vitamin B1 phosphate monoester crude with 6000kg of water for beating, cool down to 0-5°C, and add liquid alkali dropwise within this temperature range to adjust the pH value of the system to 12.0 to 14.0; after pH adjustment, ensure that the temperature in the reactor is 10 to 25°C and add 1200kg of benzoyl chloride dropwise. After the addition is completed, keep warm until the reaction is...

Embodiment 2

[0029] After adding 5000kg of polyphosphoric acid into the reaction kettle, raise the temperature to 80-100°C, add 1000kg of vitamin B1 to the reaction kettle in batches, keep it in this temperature range for 6 hours after adding, add 5000kg of water to quench After the reaction, heat up to reflux and hydrolyze for 5 hours; drop to room temperature, add 4000kg of trioctylamine / methyl tert-butyl ether=1 / 1 mixed solution to extract twice; add 6000kg of ethanol to the water phase to precipitate solids , centrifuged to obtain 1200kg of crude vitamin B1 phosphate monoester; after mixing 1200kg of vitamin B1 phosphate monoester crude product with 6000kg of water for beating, the temperature was lowered to 0-5°C, and liquid alkali was added dropwise within this temperature range to adjust the pH value of the system to 10.0 ~12.0; After pH adjustment, ensure that the temperature in the reactor is 10-25°C, add 1200kg of benzoyl chloride dropwise, keep warm until the reaction is complete...

Embodiment 3

[0031] After adding 3000kg of polyphosphoric acid into the reaction kettle, raise the temperature to 90-110°C, add 1000kg of vitamin B1 to the reaction kettle in batches, keep it in this temperature range for 5 hours after adding, add 5000kg of water to quench After the reaction, heat up to 90-100°C for hydrolysis for 5 hours; cool down to room temperature, add 5000kg of trioctylamine / methyl tert-butyl ether=1 / 1 mixed solution to the kettle for extraction twice; add 7000kg Acetone precipitated solids and centrifuged to obtain 1230kg of crude vitamin B1 phosphate monoester; after mixing 1200kg of vitamin B1 phosphate monoester crude with 6000kg of water for beating, the temperature was lowered to 0-5°C, and liquid alkali was added dropwise within this temperature range to adjust the pH of the system value to 11.0~13.0; after pH adjustment, ensure that the temperature in the reactor is 10~25°C, add 1200kg of benzoyl chloride dropwise, keep warm until the reaction is complete afte...

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Abstract

The invention relates to a production method of benfotiamine. The production method comprises the following steps: by taking polyphosphoric acid as a phosphoric acid esterification reagent, reacting with vitamin B1, performing hydrolysis at high temperature after the end of reaction, extracting phosphoric acid of a system by using a mixed solution of trioctylamine and an organic solvent after the end of hydrolysis, and then directly adding the organic solvent to precipitate a phosphate monoester crude product of vitamin B1. The obtained crude product is not purified, water is directly used for pulping, the pH value is adjusted by using liquid alkali, the reaction is performed with benzoyl chloride, and solids are filtered. The pH value of filtrate is adjusted to 3.5-4.0, the solids are precipitated, and separation and drying are performed to obtain the white solids, namely benfotiamine. The yield of benfotiamine produced by using the process is high, the product purity is high, the operation is simple, and the production method is environment-friendly and suitable for industrial production.

Description

technical field [0001] The invention relates to the field of chemical industry, and relates to an improved production process of vitamin B1 derivatives, in particular to a production method of benfotiamine. Background technique [0002] Benfotiamine is a fat-soluble derivative of vitamin B1, slightly soluble in water. The difference between benfotiamine and vitamin B1 is that benfotiamine has an open thiazole ring in its structure, which forms physiologically active vitamin B1 through ring closure in the body. After ingestion, dephosphorylation occurs in the gastrointestinal tract to form a lipophilic molecule, which is easy to diffuse into the cell membrane, so it is easier to absorb than vitamin B1. This lipophilicity allows for greater absorption in the gut and target organs than vitamin B1 itself. After being absorbed into the cells, the dephosphorylated benfotiamine is reduced in the cells, closing the thiazole ring, and releasing active vitamin B1 into the cells and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6512
Inventor 陈文肖福贵杨海峰
Owner HUBEI RUISI TECH
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