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Preparing method of 11alpha-hydroxy-16alpha, 17alpha-epoxy progesterone dehydrogenation substance

The technology of epoxy progesterone and hydroxyl group is applied in the field of preparation of 11α-hydroxy-16α, 17α-epoxyprogesterone dehydrogenate, and can solve the problems of difficulty in effective contact of biological enzymes, influence and high process cost

Active Publication Date: 2017-03-22
HENAN ZAITI BIO TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] However, in the prior art, microorganisms are used to carry out C 1,2 During the dehydrogenation reaction, microorganisms are usually dispersed in sterile water, because the solubility of 11α-hydroxyl-16α, 17α-epoxyprogesterone in water ranges from 1×10 -5 mol / L~1×10 -6 mol / L, which is an insoluble compound, so it is very difficult for 11α-hydroxyl-16α, 17α-epoxy progesterone to come into contact with biological enzymes in microbial cells, which seriously affects the C 1,2 Dehydrogenation reaction rate and yield of dehydrogenated product of 11α-hydroxy-16α,17α-epoxyprogesterone
At present, in order to increase the solubility of 11α-hydroxy-16α, 17α-epoxyprogesterone in water, methods such as cyclodextrin embedding, substrate micronization, ultrasonic treatment, and microemulsification are usually used, but these methods still have microbial catalytic effects. low defect, and the process cost of the above method is high, it is difficult to realize industrial production

Method used

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  • Preparing method of 11alpha-hydroxy-16alpha, 17alpha-epoxy progesterone dehydrogenation substance
  • Preparing method of 11alpha-hydroxy-16alpha, 17alpha-epoxy progesterone dehydrogenation substance

Examples

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Embodiment 1

[0021] This example provides the preparation method of 11α-hydroxyl-16α, 17α-epoxy progesterone dehydrogenate, the process flow chart of the preparation method is as follows figure 1 As shown, the method specifically includes the following steps:

[0022] 1. Preparation of toluene-tolerant Ochra

[0023] First, inoculate the strain of Ochraus ochrax test tubes on the potato slant medium, culture at 28°C for 7 days to generate yellow spores, then transfer the yellow spores to the slant of the yeast extract slant medium, and cultivate at 28°C for 7 days to obtain the production Use the slant; then use sterile water to rinse the production slant to obtain a spore suspension, and control the concentration of the spore suspension to be 8×10 6 each / ml; wherein, the potato slant medium includes: potato 200 g / L, glucose 20 g / L, agar 20 g / L, yeast extract 1 g / L, sterile water 1000 ml, and the potato The pH value of the slant medium is 6.8;

[0024] Then the spore suspension was inse...

Embodiment 2

[0032] This example provides a method for preparing 11α-hydroxyl-16α, 17α-epoxyprogesterone dehydrogenate. The specific preparation steps are roughly the same as those in Example 1, except that in this example,

[0033] In the conversion step in the two-phase system, the inoculum of the toluene-tolerant Ochratos is controlled to account for 7% of the water / toluene two-phase fermentation solution; 1g of the 11α-Hydroxy-16α,17α-epoxyprogesterone.

[0034] In this example, after the water / toluene two-phase fermentation solution was catalyzed by microorganisms for 30 hours, the 11α-hydroxyl-16α,17α-ring in the water / toluene two-phase fermentation solution was analyzed by high-performance liquid chromatography (HPLC). The conversion rate of oxyprogesterone to 11α-hydroxy-16α, 17α-epoxy progesterone dehydrogenation is 98.7%; The recovery yield of the product was 90%, and the purity was 91%. The recovery rate of 11α-hydroxyl-16α, 17α-epoxy progesterone was 10%, and the purity was 98...

Embodiment 3

[0036] This example provides a method for preparing 11α-hydroxyl-16α, 17α-epoxy progesterone dehydrogenate, the specific preparation steps are roughly the same as those in Example 1, the difference is that in the two In the conversion step in the phase system, the inoculum amount of the toluene-tolerant ochratos is controlled to account for 8% of the water / toluene two-phase fermentation solution; 1.5g of the 11α-hydroxyl is added in every 100 ml of the fermentation broth -16α,17α-epoxyprogesterone.

[0037] The water / toluene two-phase fermentation solution described in this example was subjected to microbial catalysis for 20 hours, and analyzed by high performance liquid chromatography (HPLC), the 11α-hydroxyl-16α, 17α-epoxy progesterone The conversion rate of 11α-hydroxyl-16α, 17α-epoxy progesterone dehydrogenation was 98.6%; The yield was 90.5%, and the purity was 91%. The recovery of 11α-hydroxy-16α, 17α-epoxyprogesterone was 11%, and the purity was 98.2%.

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Abstract

The invention provides a preparing method of an 11alpha-hydroxy-16alpha, 17alpha-epoxy progesterone dehydrogenation substance. The preparing method comprises the steps of conducting methylbenzene-resistant aspergillus ochraceus microbial catalytic treatment on 11alpha-hydroxy-16alpha, 17alpha-epoxy progesterone in a two-phase fermentation solution which uses sterile water as an aqueous phase and methylbenzene as an organic phase, and obtaining the 11alpha-hydroxy-16alpha, 17alpha-epoxy progesterone dehydrogenation substance. According to the preparing method of the 11alpha-hydroxy-16alpha, 17alpha-epoxy progesterone dehydrogenation substance, by dissolving 11alpha-hydroxy-16alpha, 17alpha-epoxy progesterone in a molecular state into a methylbenzene solution, the contact area of 11alpha-hydroxy-16alpha, 17alpha-epoxy progesterone and biological enzyme in methylbenzene-resistant aspergillus ochraceus cells is increased, and thus time for conversion is shortened, and efficiency of a C1,2 dehydrogenation reaction conducted on 11alpha-hydroxy-16alpha, 17alpha-epoxy progesterone is sharply increased. The preparing method of the 11alpha-hydroxy-16alpha, 17alpha-epoxy progesterone dehydrogenation substance is simple in process and easy for industrialization production.

Description

technical field [0001] The invention relates to the technical field of microbial fermentation, in particular to a preparation method of 11α-hydroxyl-16α, 17α-epoxy progesterone dehydrogenate. Background technique [0002] The 1, 2, 4, 5, 7, 8, 9, 11, 14, 15, and 16α, 17 positions of the steroid nucleus can be dehydrogenated by microorganisms, and the dehydrogenation reaction is carried out in these microorganisms process, especially with the C 1,2 Dehydrogenation is most important. At present, there are many clinically used steroid compounds that need to pass through microbial C 1,2 Dehydrogenation for production, such as hydroprednisone, triamcinolone, dexamethasone, betamethasone, paramethasone, etc. Among them, the 11α-hydroxy-16α, 17α-epoxy progesterone in the steroid nucleus is an important hormone drug intermediate, and the C 1,2 The dehydrogenated 11α-hydroxy-16α,17α-epoxyprogesterone prepared by dehydrogenation is widely used in the synthesis of hormone drugs. ...

Claims

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Application Information

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IPC IPC(8): C12P33/20C12P33/10
Inventor 程绍国
Owner HENAN ZAITI BIO TECH
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