86401-80-1Relevant articles and documents
Preparation method of glucocorticoid key intermediate
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Paragraph 0060-0117, (2021/03/31)
The invention provides a preparation method of a compound (III), which comprises the following steps: in an organic solvent, in the presence of a phase inversion catalyst and an organic acid, controlling the pH value of a reaction system to be 2-6, and oxidizing a compound (II) by potassium permanganate to obtain the compound (III). The invention also provides application of the preparation methodin preparation of budesonide.
Preparation method of 16a-prednisolone hydroxyacetate
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Paragraph 0036; 0037; 0046; 0047; 0056; 0057, (2019/04/17)
Disclosed is a preparation method of 16a-prednisolone hydroxyacetate. The method comprises dissolving 17-prednison dehydroxylated acetate as the raw material into organic solvent, under catalysis of acids, oxidizing 16th and 17th double bonds through potassium permanganate to obtain an oxide, and dissolving the oxide into acetone for acid-catalyzed reaction to obtain a protector; dissolving the protector into organic solvent, adding in reducing agent to reduce 11th ketone, then directly adding in acid aqueous solution for hydrolysis and deprotection to obtain the 16a-prednisolone hydroxyacetate. Although the preparation method of the 16a-prednisolone hydroxyacetate adds the two reaction steps of protection and deprotection, every unit reaction is high in yield, the third and fourth reaction steps can be completed within on pot, so that the production operation can be simple and convenient, the production processes are economical and environmentally friendly, the problems of many side reactions and impurities and difficulty impurity refining of oxidation reaction in traditional production process can be greatly solved, the total synthesizing yield can be greatly increased, and compared with traditional production methods, the preparation method of the 16a-prednisolone hydroxyacetate can reduce the production cost by 20-25%.
A budesonide industrial preparation method (by machine translation)
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, (2019/03/10)
The invention relates to a cloth budesonide industrial preparation method. Specifically, the invention relates to a hydrochloric acid aqueous solution, dichloromethane and in acetonitrile, 16 α - hydroxy prednisolone with butyraldehyde by the reaction of the budesonide. In the method of the present invention has the industrial can be implemented on, repeatability and the like. (by machine translation)