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-hydroxy prednisolone acetate product
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Paragraph 0031; 0038-0041; 0048-0049; 0051; 0058-0059, (2019/05/22)
A preparation method of a 16a-hydroxy prednisolone acetate product includes dissolving 17-dehydroxy prednisone acetate as a raw material in an organic solvent, oxidizing 16 and 17 double bonds by potassium permanganate under acid catalysis to obtain an oxide, dissolving the obtained oxide in an organic solvent, adding acetone, and carrying out acid catalyzed reaction to obtain a protector; dissolving the protector in an organic solvent, adding a reducing agent to reduce ketone at the 11th position, directly adding an acid water solution for hydrolysis and deprotection after the reduction reaction to obtain 16a-hydroxy prednisolone acetate, and subjecting the crude product to decoloration and recrystallization by low-carbon-alcohol heating reflux to obtain the 16a-hydroxy prednisolone acetate product. Although two reaction steps, protection and deprotection, are added, the reaction yield of units in each step is high, the method is simple and convenient to operate, the process is economical and environmentally friendly, and the total synthesis yield is increased remarkably; the preparation cost of the preparation method is 20-25% lower than that of conventional production methods.
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)