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A kind of preparation method of ursodeoxycholic acid

A technology of ursodeoxycholic acid and hyodeoxycholic acid, which is applied in the field of medicine, can solve problems such as rising market prices, high cost of synthetic routes, limited CDCA resources, etc., to achieve simple operation, solve the shortage of raw materials, and low cost Effect

Active Publication Date: 2019-08-02
青州市欣泰生物制品有限公司
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  • Abstract
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  • Application Information

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Problems solved by technology

[0005] At present, the production process of UDCA is to use chenodeoxycholic acid (CDCA) as the raw material, and it is prepared through esterification, oxidation and reduction. This product has a large demand in domestic and foreign markets, but CDCA resources are limited, and its market price is increasing year by year. The cost of the synthetic route using chenodeoxycholic acid as raw material remains high

Method used

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  • A kind of preparation method of ursodeoxycholic acid
  • A kind of preparation method of ursodeoxycholic acid
  • A kind of preparation method of ursodeoxycholic acid

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Embodiment 1

[0058] The preparation of ursodeoxycholic acid shown in embodiment 1, formula I

[0059] 1. Compound shown in formula II (R 1 for the preparation of ethyl)

[0060] The starting material hyodeoxycholic acid (HDCA) 50g was dissolved in 500mL of absolute ethanol, added dropwise to 2mL of concentrated sulfuric acid, stirred and reacted at room temperature for 24 hours, concentrated under reduced pressure to dryness, and obtained 52g of the compound shown in formula II (R 1 is ethyl), a colorless oil, with a yield of 98%.

[0061] or

[0062] Compound shown in formula II (R 1 For the preparation of methyl)

[0063] Dissolve 50 g of the starting material hyodeoxycholic acid (HDCA) in 500 mL of anhydrous methanol, add dropwise 5.5 mL of 36% concentrated hydrochloric acid, heat up to reflux, stir and react for 8 hours, and concentrate to dryness under reduced pressure to obtain 51 g of the formula II Shown compound (R 1 is methyl), colorless oil, yield 98%.

[0064] 2, compoun...

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Abstract

The invention belongs to the field of medicine, and particularly relates to a method for preparing an ursodeoxycholic acid. The method comprises the following steps: performing esterification reaction to obtain a compound shown in formula II by taking an HDCA (hyodeoxycholic acid) as a starting raw material; performing selective hydroxy protection reaction to obtain a compound shown in formula III; performing hydroxy protection reaction to obtain a compound shown in formula IV; performing elimination reaction to obtain a compound shown in formula V; performing oxidation reaction on the compound shown in formula V under the action of tert-butyl hydroperoxide and pyridinium chlorochromate to obtain a compound shown in formula VI; performing hydrolysis to obtain a compound shown in formula VII; performing reduction to obtain the ursodeoxycholic acid shown in formula I. According to the method, the ursodeoxycholic acid is prepared by taking the HDCA as the starting raw material, so that not only can the problem of raw material shortage be solved, but also the method is convenient to operate, low in byproduct rate and cost, mild in reaction condition and suitable for large-scale production of the ursodeoxycholic acid.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a preparation method of ursodeoxycholic acid. Background technique [0002] Ursodeoxycholic acid (UDCA, represented by chemical formula I) is the main component of the traditional Chinese medicine bear bile, which was once mainly used for the treatment of gallstone disease. In recent years, foreign countries have reported the application of UDCA in the treatment of various acute and chronic liver diseases. New research shows that UDCA not only has a good curative effect on the treatment of primary biliary cirrhosis, primary sclerosing cholangitis, and chronic active hepatitis, but also can be used to treat chronic hepatitis and rejection after liver transplantation. [0003] Traditional Chinese medicine bear bile is made from harvesting the gallbladder of bears. The source is limited and it violates animal protection. At present, artificial breeding is adopted in our country...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J9/00
CPCC07J9/005
Inventor 曹建华国晶
Owner 青州市欣泰生物制品有限公司
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