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Biological dehydrogenation preparation method of steroid drug intermediate

A technology of steroidal drugs and intermediates, which is applied in the field of biological dehydrogenation preparation of pregnant drug intermediates, can solve the problems of prolonging reaction time, reducing conversion rate, and producing dehydrogenation products, so as to shorten reaction time and improve conversion rate, the effect of overcoming toxicity

Inactive Publication Date: 2010-06-30
TIANJIN JINYAO GRP
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  • Abstract
  • Description
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Problems solved by technology

However, the technical solution disclosed in this application neither discloses any preservation information of the strains used for biological dehydrogenation, nor discloses the formula of the medium used for biological dehydrogenation. Because in the prior art, different bacterial strains and different mediums There is a big difference in the yield of producing dehydrogenate during production, which causes the technical scheme disclosed in this patent application to be unable to be implemented.
In addition, we found in the experiment that the method of using solvent to dissolve the substrate is easy to affect the reproduction of the strain, thereby prolonging the reaction time and reducing the conversion rate; and the use of micronized substrate, although the effect is better, but in industrial production However, it is very time-consuming and energy-consuming to micronize a large amount of intermediates, thus affecting the application of micronized substrates for biodehydrogenation.

Method used

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  • Biological dehydrogenation preparation method of steroid drug intermediate
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-1

[0049] Example 1-1: Using 6α-methyl-11β,17α-dihydroxy-pregn-4-ene-3,20-dione as a substrate

[0050] The simple Arthrobacter (AS 1.94*) was cultured in inclined plane, primary culture and secondary culture in sequence. The culture temperature was 30°C. The micronized substrate was put into a 5L fermentor with a feed concentration of 4% and a reaction temperature of 30 ℃. The reaction time is 48 hours. After the reaction is completed, the temperature is raised to 70° C. to terminate the reaction. The fermentation broth is extracted with ethyl acetate, and the organic phase is concentrated. The substrate conversion rate is measured to be 71.3%.

Embodiment 1-2

[0052] Using the substrate and fermentation process of Example 1-1, adding 150ml Tween-80 as a solvent during feeding, the reaction time was shortened to 36 hours, the fermentation broth was extracted with ethyl acetate, and the organic phase was concentrated. The product conversion rate was 76.2%.

Embodiment 2

[0053] Example 2: Using 6α-methyl-17α,21-dihydroxy-pregn-4-ene 3,11,20-trione-21-acetate as a substrate;

[0054] The simple Arthrobacter (AS 1.754) was cultured in slope, primary culture and secondary culture in sequence. The culture temperature was 31℃. The micronized substrate was put into a 5L fermentor with a feed concentration of 2% and a reaction temperature of 32℃. . The reaction time is 42 hours. After the reaction is completed, the temperature is raised to 70° C. to terminate the reaction. The fermentation broth is extracted with ethyl acetate, and the organic phase is concentrated. The measured substrate conversion rate is 75.5%.

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Abstract

A biological dehydrogenation preparation method of steroid drug intermediate takes the formula (1) compound as a substrate, and adopts an arthrobacter simplex biological dehydrogenation method to obtain formula (2) compound; the special process comprises the following steps: smashing or dissolving the formula (1) compound with solvent, putting into a fermentation tank in which arthrobacter is cultivated for biotransformation, extracting, separating and refining, and drying to obtain dehydrogenated polymer, i.e. compound (2); and the dehydrogenation transformation rate can reach 70 to 90 percent.

Description

Technical field: [0001] The invention relates to a preparation method of steroid drug intermediates, in particular to a biological dehydrogenation preparation method of pregnant steroid drug intermediates. Background technique: [0002] Glucocorticoids are steroid compounds secreted by the adrenal cortex, and their physiological effects are manifested in their effects on sugar, protein, fat, water and electrolytes. It can inhibit the synthesis and release of inflammatory mediators such as bradykinin, prostaglandin E2, serotonin, histamine, etc., reduce vascular permeability, stabilize lysosome membrane, and inhibit phagocytosis. It has a strong anti-inflammatory effect on inflammation caused by various reasons. It can reduce exudation, edema, telangiectasia, leukocyte infiltration and phagocytosis in the early stage of inflammation, and can inhibit the proliferation of capillaries and fibroblasts in the late stage of inflammation, and inhibit immunity Response to the pathologica...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12P33/02C12R1/06
Inventor 陈立营陈松赵琳
Owner TIANJIN JINYAO GRP
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