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Synthetic method of 11alpha hydroxy-canrenone

A technique for the synthesis of hydroxycanrenone, which is applied in the field of biochemistry, can solve the problems of low feed concentration, poor canrenone specificity, and low yield, and achieve high feed concentration, good substrate specificity, and high product yield. The effect of high yield

Inactive Publication Date: 2010-09-29
TAIZHOU NANFENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] The technical problem solved by the present invention is to provide a synthetic method for 11α-hydroxycanrenone, more specifically, to solve the above-mentioned third synthetic method with poor specificity of invertase to canrenone, low feeding concentration and low yield The problem

Method used

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  • Synthetic method of 11alpha hydroxy-canrenone

Examples

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Effect test

Embodiment 1

[0029] A method for synthesizing 11α-hydroxycanrenone. The raw materials canrenone, propylene glycol, and Tween 80 are heated and dissolved to form a substrate, which is then added to a culture medium, and then put into the culture medium for fermentation. After the fermentation is completed, the mycelium Body extraction, refined to get 11α hydroxycanrenone. Specifically include:

[0030] 1) Selection of strains: after artificial induction (15 minutes of ultraviolet radiation with a wavelength of 254nm) and natural mutation of ochratos (original strains) into excellent ochratos strains with high selectivity to the substrate canrenone Store freeze-dried tubes at low temperature.

[0031] 2), the cultivation of strains: subculture solid medium ratio: 0.07% peptone, 1% maltose, 1.5% glucose, 2.5% agar, adjust the pH to 5.2, culture conditions: 25 ° C, culture for 7 days, obtained by three generations of subculture The strains used in the production are stored in a low-temperatu...

Embodiment 2

[0036] A method for synthesizing 11α-hydroxycanrenone. The raw materials canrenone, propylene glycol, and Tween 80 are heated and dissolved to form a substrate, which is then added to a culture medium, and then put into the culture medium for fermentation. After the fermentation is completed, the mycelium Body extraction, refined to get 11α hydroxycanrenone. Specifically include:

[0037] 1. Selection of strains: Ochratos (original strain) is artificially induced (15 minutes of ultraviolet radiation with a wavelength of 254nm) and naturally mutated into an excellent strain of Ochras with high selectivity to the substrate canrenone, and then frozen Store in a dry tube at low temperature.

[0038] 2. Cultivation of strains: subculture solid medium ratio: 0.1% peptone, 2% maltose, 2% glucose, 2% agar, adjust the pH to 5.3, culture conditions: 25-30°C, culture for 9 days, take three generations of passage The strains used for production are obtained, and stored in a low-temperat...

Embodiment 3

[0043] A method for synthesizing 11α-hydroxycanrenone. The raw materials canrenone, propylene glycol, and Tween 80 are heated and dissolved to form a substrate, which is then added to a culture medium, and then put into the culture medium for fermentation. After the fermentation is completed, the mycelium Body extraction, refined to get 11α-hydroxycanrenone. Specifically include:

[0044] 1. Selection of strains: Ochratos (original strain) is artificially induced (18 minutes of ultraviolet radiation with a wavelength of 254nm) and naturally mutated into an excellent Ochras strain with high selectivity to the substrate canrenone, and then frozen Store in a dry tube at low temperature.

[0045] 2. Cultivation of strains: subculture solid medium ratio: 0.12% peptone, 1.5% maltose, 2.5% glucose, 1.8% agar, adjust the pH to 5.0, culture conditions: 25-30°C, culture for 7 days, take three generations of passage The strains used for production are obtained, and stored in a low-temp...

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Abstract

The invention discloses a synthetic method of 11alpha hydroxy-canrenone, comprising the following steps of: heating and dissolving canrenone, propylene glycol and tween 80 to obtain a substrate; adding the substrate into a culture medium; adding an apergillus ochraceus strain and fermenting; and after the fermenting is finished, extracting and refining from a mycelium to obtain the 11alpha hydroxy-canrenone. By adopting a biosynthesis technology, novel invertase can be selected, thereby greatly reducing the cost of the 11alpha hydroxy-canrenone. The specificity of the invertase on the canrenone is improved to over 85 percent from the traditional 75 percent; the feeding concentration of the canrenone is improved to over 0.8 percent from 0.6 percent; the yield of the 11alpha hydroxy-canrenone is improved to over 60 percent from 50 percent; and main quality indexes of the 11alpha hydroxy-canrenone reach that: the content (HPLC-High Performance Liquid Chromatography) is not less than 98 percent, the content of total impurities is not more than 2.0 percent and the content of single impurity peak is not more than 1.5 percent.

Description

technical field [0001] The invention relates to a synthesis method of 11α hydroxycanrenone, which belongs to the field of biochemistry. Background technique [0002] Since the compound patent of eplerenone has expired, the pharmaceutical industry all over the world has imitated the product in recent years. At present, several non-standard markets such as Argentina have been approved, and four companies in my country have applied for registration. The analysis of all synthetic routes of eplerenone found that although there are many synthetic routes of eplerenone, almost all routes are inseparable from a key intermediate, namely 11α hydroxycanrenone. Currently, eplerenone is expensive due to the high cost of 11αhydroxycanrenone. In view of the above situation, it is extremely promising to study the biosynthesis of 11α-hydroxycanrenone, the key intermediate of eplerenone, and reduce its cost significantly to meet the needs of the industrialization of eplerenone. Since the cos...

Claims

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Application Information

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IPC IPC(8): C12P33/20C12R1/66
Inventor 王喜情
Owner TAIZHOU NANFENG PHARMA
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