Method for preparing hydrocortisone

A technology of hydrocortisone and hydrocortisone acetate, applied in the directions of organic chemistry, steroids, etc., can solve the problem of inability to improve the primary mass yield of the crude product directly precipitated, time-consuming concentration and evaporation of the solvent, difficulty in crystallization of the product, etc. problems, to avoid the phenomenon of foam overflow, novel process route, and simplify the post-processing operation process.
CN105367618AInactive Publication Date: 2016-03-02HUAZHONG PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
HUAZHONG PHARMA
Publication Date
2016-03-02
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a method for preparing hydrocortisone. The method includes: subjecting a cortisone acetate raw material to sites No. 3,20-keto protective reaction, site No.11-keto reduction reaction, site No.21-hydroxy esterification reaction, sites No. 3,20-ketone deprotection reaction, and site No. 21-acetate hydrolysis to obtain hydrocortisone. The method provides a new synthetic route containing esterification and deprotection in order, greatly improves the reaction selectivity, easily separates deprotection reaction products and avoids the posttreatment of tedious several times of extraction of a large amount of solvents in the traditional deprotection reaction process, and also avoids the side reaction caused by quenching reaction in the posttreatment of the traditional process; and the ester hydrolysis reaction is carried out under protection of inert gases in a mixed solvent, so as to avoid by-products produced in the hydrolysis reaction. The process route of the invention is novel, simple for operation, low in production cost, and applicable to industrial scale production.
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Description

Technical field

[0001] The invention belongs to the field of chemical pharmacy, and specifically relates to a preparation method of hydrocortisone. Background technique

[0002] The structural formula of hydrocortisone (11β, 17α, 21-trihydroxy-pregna-4ene-3,20-dione) is:

[0003] .

[0004] Hydrocortisone belongs to the adrenal cortex hormone drug, which has various pharmacological effects such as anti-inflammatory, immunosuppressive, anti-toxic and anti-shock. The 11β-hydroxyl group in the structure of steroids is a necessary group for anti-inflammatory drugs. How to introduce 11β-hydroxyl group during the preparation of hydrocortisone is a key step of the whole process. The existing processes mainly include microbial transformation and chemical methods. Two kinds. Absidia is widely used as an oxidizing strain in China, and 11β-hydroxyl is introduced into the substrate RSA through one-step microbial transformation. This process has the disadvantages of low conversion rate, many...

Claims

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