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Preparation method of prednisone acetate

A prednisone acetate and compound technology, applied in the field of preparation of prednisone acetate, can solve the problems of difficult complete conversion, cumbersome chemical synthesis steps, long process route, etc.

Active Publication Date: 2021-02-09
HUNAN NORCHEM PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, the biotransformation is obtained through the dehydrogenation of cortisone acetate by biofermentation, and the "National Compendium of Raw Materials Processes" edited by Ye Songlin et al. discloses that cortisone acetate is synthesized from acetic acid gestational dienolone via 8-step reaction , this traditional process has a long route and low yield, and it is difficult to completely transform the dehydrogenation of cortisone acetate by biological fermentation, and it is similar to prednisone acetate in nature, so it is difficult to remove during refining, which affects the purity and quality of the product
The chemical synthesis steps are cumbersome, the cost of starting materials is high, and usually involves the process of iodine replacement, and the cost of iodine element is high, and it will also cause the problem of three wastes, which is gradually eliminated in industry

Method used

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  • Preparation method of prednisone acetate
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  • Preparation method of prednisone acetate

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preparation example Construction

[0042] One embodiment of the present invention provides a synthesis method of prednisone acetate, comprising the following steps S10-S30.

[0043]Step S10: using the compound of formula (I) as a raw material to undergo a hydroxylation reaction through the first biological fermentation to prepare the compound of formula (II); wherein, the structures of the compound of formula (I) and the compound of formula (II) are as follows:

[0044]

[0045] Step S20: subjecting the compound of formula (II) to a second biological fermentation for dehydrogenation to prepare the compound of formula (III). The structure of the compound of formula (III) is as follows:

[0046]

[0047] Step S30: subjecting the compound of formula (III) to an oxidation reaction to prepare the compound of formula (IV) prednisone acetate, the structure of the compound of formula (IV) is as follows:

[0048]

[0049] The compound of formula (I) (RSA) has been industrially produced, but it is less used now,...

Embodiment 1

[0165] 1) Preparation of formula (II) compound

[0166] 1.1 Incline cultivation

[0167] Adopt Aspergillus ochraceus ATCC 18500 as the production strain, and the slant medium is potato medium: potato 200g / L (boil for 30 minutes, filter with four layers of gauze to get the filtrate), glucose 20g / L, and the pH value is 6.5, which will be preserved Streak inoculation on the slant and culture at 30°C for 6 days.

[0168] 1.2 Seed culture

[0169] Preparation of spore suspension: take a fresh slant that has been cultured for 6 days, wash the spores of the slant with 0.05% Tween-80 sterile water to make a spore suspension, and count the spore concentration by microscopic examination to be 2 to 3×10 7 pieces / ml.

[0170]Shake flask seed culture: the seed medium components are corn steep liquor 10g / L and glucose 30g / L, the pH value is 7.2, the inoculum size is 10%, 30 ℃, 180rpm culture 40h.

[0171] 1.3 Bacteria pre-cultivation

[0172] 10-liter fermenter, the volume of fermentat...

Embodiment 2

[0210] Example 2 is basically the same as Example 1, except that in step 1) of Example 2, Ochrax is replaced by Metarhizium anisopliae, other steps and process parameters are the same as in Example 1, and the obtained formula (II ) The compound yield is 94%, and the purity is 98.9%.

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Abstract

The invention relates to a preparation method of prednisone acetate and prednisone. 4-pregnene-17alpha,21-diol-3,20-dione 21-acetate (RSA) used as a raw material is sequentially subjected to fermentation hydroxylation reaction, fermentation dehydrogenation reaction and oxidation reaction, and prednisone acetate is prepared. The step of iodine addition and replacement is not needed; the preparationmethod is short in synthesis route, high in conversion rate, economic environmentally friendly and low in cost; and the yield and the purity can be effectively increased, so that the preparation method is suitable for industrial production, and has high industrial value.

Description

technical field [0001] The invention relates to the technical field of medicine synthesis, in particular to a preparation method of prednisone acetate. Background technique [0002] Prednisone acetate is an important class of adrenocortical hormone drugs, which has anti-inflammatory, anti-allergic, anti-rheumatic, and immunosuppressive effects. It is mainly used for various acute severe bacterial infections, severe allergic diseases, collagen diseases, and rheumatism. , rheumatoid arthritis, nephrotic syndrome, severe bronchial asthma, thrombocytopenic purpura, neutropenia, acute lymphoblastic leukemia, various adrenal insufficiencies, exfoliative dermatitis, pemphigus, neurodermatitis, Eczema etc. Elderly people with herpes zoster can be given a small amount of prednisone acetate in the early stage of onset to shorten the course of the disease and prevent the occurrence of postherpetic neuralgia. [0003] The preparation method of traditional prednisone acetate is divided...

Claims

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Application Information

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IPC IPC(8): C12P33/10C12P33/02C12P33/00C12P39/00C07J5/00C12R1/66C12R1/645C12R1/845C12R1/06C12R1/365
CPCC12P33/10C12P33/02C12P33/00C12P39/00C07J5/0053
Inventor 吴亚克孟浩刘喜荣曾春玲靳志忠刘家贝
Owner HUNAN NORCHEM PHARMACEUTICAL CO LTD
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