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Benfotiamine related substance, preparation method, application and detection method

A technology of benfotiamine and related substances, which is applied in the field of drug impurities and preparation, and can solve problems affecting product quality and other issues

Inactive Publication Date: 2021-05-11
SHANGHAI RIXIN BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The starting materials, intermediates, by-products and degradation products in the synthesis of benfotiamine may become impurities remaining in the final product, thereby affecting product quality
[0005] At present, there are few literature reports on the research on related substances of benfotiamine and the research on quality control analysis methods

Method used

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  • Benfotiamine related substance, preparation method, application and detection method
  • Benfotiamine related substance, preparation method, application and detection method
  • Benfotiamine related substance, preparation method, application and detection method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029]

[0030] Add phosphoric acid (225g) to the reaction flask, within 100°C, add phosphorus pentoxide (150g) in batches, react at 100-110°C for 1-2h, then add compound 4 (150g) and keep warm until the reaction is complete, then cool down to 45 Add drinking water and acetone at about ℃ and keep stirring for 0.5-1 hour, then add the separated oily substance to the mixture of ethanol and water to crystallize and dry to obtain light yellow compound 3: 166g, the yield is 75%

Embodiment 2

[0032]

[0033] Add 6v of water and compound 3 (1.00eq) to the reaction flask in sequence, control the temperature at 0-15°C, add 30% sodium hydroxide solution dropwise, adjust the pH to 12.5-13.0 and keep stirring for 1 hour. After the system has a large amount of solids precipitated. Control the temperature at -1-6°C, add benzoyl chloride (1.00eq) dropwise, and keep the reaction for 1.5-2.5h. Control the temperature at 0-10°C, adjust the pH to 3.8-4.1 with hydrochloric acid and keep stirring for 3 hours. Filter to obtain compound 2, and the yield is 100% for the next step of feeding.

Embodiment 3

[0035]

[0036] Add water (6v) and compound 2 (1.00eq) to the reaction flask in sequence, control the temperature at 0-15°C, add 30% sodium hydroxide solution dropwise, adjust the pH to 8-9 and keep stirring for 1 hour. After a large amount of solids precipitate out of the system. Control the temperature at -1-6°C, add benzoyl chloride (1.00eq) dropwise, and keep the reaction for 1.5-2.5h. Control the temperature at 0-10°C, adjust the pH to 3.8-4.1 with hydrochloric acid and keep stirring for 3 hours. After filtration, the crude product of compound 1 was obtained, and after air-drying at 50°C, it was crystallized with 3v of methanol and 1v of water to obtain compound C with a yield of 40%. Compound C is carried out hydrogen spectrum detection, and the results are shown in figure 1 .

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Abstract

The invention discloses a benfotiamine related substance, a preparation method, application and a detection method. The benfotiamine related substance is a compound C, and the structure of the compound C is shown in the description. The preparation method provided by the invention is simple, and the compound C with the purity meeting the requirement can be prepared. The invention further provides the detection method of the benfotiamine related substance. The high-purity compound C can be used as a benfotiamine reference substance or standard substance, and has a good application prospect.

Description

technical field [0001] The invention relates to a drug impurity, a preparation method, an application and a detection method, in particular to a substance related to benfotiamine, a preparation method, an application and a detection method. Background technique [0002] Benfotiamine, developed by Akira in Japan, is a synthetic vitamin B1 derivative and is mainly used for the adjuvant treatment of multiple neuritis, peripheral neuritis, central nervous system injury, myocarditis, nutrition and dyspepsia. In recent years, Professor Zhong Chunjiu, deputy director of the Neurology Department of Zhongshan Hospital affiliated to Fudan University, led the members of the scientific research team to discover for the first time that benfotiamine is effective in the treatment of senile dementia in related research on the pathogenesis, pathogenic factors and treatment of senile dementia. The research paper has been published in the international authoritative academic journal "Brain" an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6512G01N30/02G01N30/06G01N30/34G01N30/36G01N30/74
CPCC07F9/6512G01N30/02G01N30/06G01N30/34G01N30/36G01N30/74G01N2030/042
Inventor 兰爱虎王晓飞林峰罗林
Owner SHANGHAI RIXIN BIOTECHNOLOGY CO LTD