About a kind of preparation method of pregna-16-ene-3,20-dione steroid derivative

A technology of diketone steroids and derivatives, which is applied in the field of steroid synthesis, can solve the problems of being unsuitable for industrial production, cumbersome, difficult to refine, etc., and achieve the effects of environmental protection and cost reduction
CN104710496BActive Publication Date: 2017-11-07TIANJIN JINYAO GRP
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
TIANJIN JINYAO GRP
Publication Date
2017-11-07

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Abstract

The invention relates to a preparation method for a pregna-16-ene-3, 20-dione steroid derivative (II). The method is characterized by: reacting 17alpha-ethynyl-17beta-hydroxysteroid derivative I with a reagent A or an organic solvent containing the reagent A to obtaining the derivative (II). The reaction temperature ranges from 25DEG C to a solvent reflux temperature, and the reagent A is a solution formed by dissolving 5%-15% of phosphorus pentoxide in methanesulfonic acid.
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Description

technical field

[0001] The invention belongs to the technical field of steroid synthesis and relates to the preparation of pregna-16-ene-3,20-dione steroid derivatives from 17α-ethynyl-17β-hydroxy steroid derivatives. Background technique

[0002] Pregna-4,16-diene-3,20-dione and its derivatives are key intermediates in the synthesis of steroids, used in the manufacture of dexamethasone, betamethasone, methylprednisolone, and hydrocortisone , prednisone and other steroid drugs have high economic value. Now the common method for industrial production of pregna-4,16-diene-3,20-dione and its derivatives is to use pregna-5,16-diene-20-one-3-hydroxyl-3-acetate (referred to as diene) as raw material preparation. Dienes are produced from diosgenin through three steps of cracking, oxidation, and hydrolysis. First, this production process requires a large amount of sulfuric acid, which is likely to cause a lot of pollution to the environment; second, with the continuous improvement...

Claims

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