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Preparation method of high-quality prednisone acetate and intermediate thereof

A technology of prednisone acetate and intermediates, which is applied in the field of preparation of high-quality prednisone acetate and intermediates thereof, can solve problems such as unsatisfactory conditions, and achieve the effects of simple and convenient operation, convenient operation and high feeding concentration

Inactive Publication Date: 2020-03-06
HUAZHONG PHARMA
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] For the existing problems in the above actual production, the present invention aims to provide a kind of production method of prednisone acetate, particularly a kind of production method of high-quality prednisone acetate, take epihydrocortisone as raw material, take the first The post-fermentation synthesis method is used to produce prednisone acetate, which solves the unsatisfactory technical difficulty of introducing C1,2 double bonds in the fermentation production process of prednisone acetate, and the process has the characteristics of low cost and easy operation

Method used

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  • Preparation method of high-quality prednisone acetate and intermediate thereof
  • Preparation method of high-quality prednisone acetate and intermediate thereof

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preparation example Construction

[0031] The invention provides a method for preparing high-quality prednisone acetate. The specific steps are as follows: taking epihydrocortisone as a raw material, first performing microbial dehydrogenation to obtain 11α, 17α, 21-trihydroxy-pregna-1,4 -diene-3,20-dione intermediate, and then through esterification to obtain 11α, 17α, 21-trihydroxy-pregna-1,4-diene-3,20-dione-21-acetate, and finally through Oxidation reaction makes prednisone acetate, and concrete technical route is as follows:

[0032] 1) Using epihydrocortisone as a raw material, dehydrogenating epihydrocortisone by simple Arthrobacter dehydrogenation, and preparing epihydrocortisone dehydrogenate as 11α, 17α, 21-trihydroxy-pregna-1,4-diene-3, 20-diketone, its concrete preparation steps are:

[0033] A. Culture of Arthrobacter simplex

[0034] Add culture medium into the shake flask, insert Arthrobacter simplex, culture at 28-35°C, 120-200rpm for 20-28 hours for later use;

[0035] B. Putting in raw mater...

Embodiment 1

[0048] A kind of preparation method of high-quality prednisone acetate intermediate, described prednisone acetate intermediate is 11α, 17α, 21-trihydroxy-pregna-1,4-diene-3,20-dione, Its concrete preparation steps are:

[0049] Add culture medium in shake flask, insert Arthrobacter simplex, 30 ℃, 160rpm culture 20-28 hour; Add raw material table hydrocortisone in cultured bacterial culture medium, add 7% ethanol, feeding amount 40g / L, 33°C, 180rpm after conversion for 1-2 days, TLC analysis and detection, until the conversion of raw materials is complete; separation and purification, the target product 11α, 17α, 21-trihydroxy-pregna-1,4-diene-3,20- Diketone has a purity of 99.16% as detected by HPLC.

Embodiment 2

[0051] A kind of preparation method of high-quality prednisone acetate and its intermediate, described prednisone acetate intermediate is 11α, 17α, 21-trihydroxy-pregna-1,4-diene-3,20-di Ketone, its specific preparation steps are:

[0052] 1) Culture of Arthrobacter simplex

[0053] Add culture medium in shake flask, insert Arthrobacter simplex, 30 ℃, 180rpm culture 20-28 hour; Add raw material table hydrocortisone in cultured bacterium culture medium, add 7% ethanol, feeding amount 40g / L, 33°C, 180rpm after conversion for 1-2 days, TLC analysis and detection, until the conversion of raw materials is complete; separation and purification, the target product 11α, 17α, 21-trihydroxy-pregna-1,4-diene-3,20- The diketone has a purity of 98.8% as detected by HPLC.

[0054] 2) Esterification reaction

[0055] Using the above-mentioned epihydrodehydrogenate as raw material, carry out esterification reaction to prepare intermediate 11α, 17α, 21-trihydroxy-pregna-1,4diene-3,20dione-...

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Abstract

The invention discloses a preparation method of high-quality prednisone acetate and an intermediate thereof. The method includes the steps of: taking epihydrocortisone as the raw material, firstly conducting microbial dehydrogenation to obtain 11alpha, 17alpha, 21-trihydroxy-pregn-1, 4-diene-3, 20-dione intermediate, then carrying out esterification reaction to obtain 11alpha, 17alpha, 21-trihydroxy-pregn-1, 4-diene-3, 20-dione-21-acetate, and finally carrying out oxidation reaction to obtain prednisone acetate. The method provided by the invention solves the technical difficulty of non-idealintroduction of C1, 2 double bond in the traditional fermentation production process of prednisone acetate. The cortisone acetate prepared by the method provided by the invention has high quality andextremely low impurity content, greatly improves the multidirectional application of prednisone acetate, and meanwhile, the process route has the characteristics of low cost and simple operation.

Description

technical field [0001] The invention relates to the technical field of preparation of steroid medicines and intermediates thereof, in particular to a preparation method of high-quality prednisone acetate and intermediates thereof. Background technique [0002] Among all kinds of drugs in the world, steroid drugs are the second largest class of drugs after antibiotics. The molecular structures of different steroid drugs are all derived from steroid hormone intermediates. Steroid hormones have strong pharmacological effects of anti-infection, anti-virus, anti-allergy, and anti-shock. They are important drugs for treating rheumatism, cardiovascular, lymphatic leukemia, cellular encephalitis, skin diseases, anti-tumor and rescuing critically ill patients. Wherein, prednisone acetate is a kind of important steroid drug, and its structural formula is: [0003] [0004] Prednisone acetate, a corticosteroid drug, acts on glucose metabolism, reduces the pathological response of t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J5/00C12P33/02C12R1/06
CPCC07J5/0053C12P33/02
Inventor 徐明琴廖俊付林冯蕾曾建华田玉林
Owner HUAZHONG PHARMA
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