Method for synthesizing benfotiamine

A synthesis method and benfotiamine technology are applied in the field of organic compound preparation process improvement, can solve problems such as increasing process steps, increasing production cycle, reducing production efficiency and the like, and achieve the effects of high purity, improved production efficiency and low price
CN102911208AInactive Publication Date: 2013-02-06TONGJI UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
TONGJI UNIV
Publication Date
2013-02-06
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a method for synthesizing benfotiamine, in particular to a process for synthesizing benfotiamine which is an anti-diabetic medicament by the phosphorylation of thiamine which severs as the raw material, the opening of the thiazole ring and the reaction of multiple steps. Benfotiamine is subjected to phosphorylation under the control of appropriate temperature and other conditions in a short time by taking phosphorus oxychloride as a phosphorylation reagent to obtain monophosphothiamine, and finally the steps of ring opening and benzoylation are carried out to obtain benfotiamine. The process has the advantages of high conversion rate of raw materials, low-cost, high product purity and greatly reduced production cycle and is suitable for industrial production.
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Description

technical field

[0001] The invention belongs to the improvement of the preparation process of organic compounds, in particular to a synthesis method of benfotiamine. Background technique

[0002] Benfotiamine is a fat-soluble derivative of thiamine, a synthetic vitamin B1 derivative that is slightly soluble in water. Synthesized in Japan in the 1960s, it was gradually used in the treatment of neuropathy, sciatica and other neuropathic pains caused by alcoholism after 1962. Since the 1990s, European scholars have conducted a series of studies on thiamine, especially benfotiamine, in the treatment and prevention of diabetes and its complications, and have made significant progress in recent years. The drug has been used in Europe for more than a decade to treat various conditions, including nerve damage associated with diabetes. Benfotiamine was developed by the Japanese company Akira. The chemical name of benfotiamine is: S-[2-[[(4-amino-2-methyl-5-pyrimidinyl)methyl]formyl...

Claims

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