Preparation method of 17a-dehydroxy prednisolone acetate product

A technology of prednisolone dehydroxyacetate and prednisolone acetate, which is applied in the production process field of synthesizing 17a-prednisolone dehydroxyacetate, can solve the problems of high production cost, low synthesis yield and many side reactions and other problems, to achieve the effect of simple and convenient production operation, high yield and reduced preparation cost
CN109734765AActive Publication Date: 2019-05-10HUNAN KEREY BIOTECH
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
HUNAN KEREY BIOTECH
Publication Date
2019-05-10

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Abstract

The invention provides a preparation method of a 17a-dehydroxy prednisolone acetate product. The method includes the following steps: step A, dissolving prednisolone acetate in a first organic solvent, and subjecting the solvent and trimethylchlorosilane to 11th-position silicon etherification reaction under the catalysis of organic base to obtain a protector; step B, in a second organic solvent,subjecting the protector and SO3 to 17th-position dehydration reaction under the catalysis of the organic base, directly adding acid for treatment after the reaction to deprotect the 11th position, and obtaining a crude 17a-dehydroxy prednisolone acetate product; subjecting the crude product to decolorization and recrystallization in the presence of C4-below low carbon alcohol and activated carbonto obtain the 17a-dehydroxy prednisolone acetate product. The preparation method has the advantages that the problems such as many side reactions and impurities and difficulty in impurity refining inthe dehydration reaction in a traditional production process of 17a-dehydroxy prednisolone acetate are solved, the total synthesis yield is remarkably increased, and the production cost is reduced.
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Description

technical field

[0001] The invention belongs to the preparation technology of steroid hormone drug intermediates, and specifically refers to a production technology for synthesizing 17a-dehydroprednisolone acetate by using prednisolone acetate as a raw material. Background technique

[0002] 17a-prednisolone dehydroxyacetate (molecular formula C 23 h 26 o 6 ), chemically named 11b,21-dihydroxypregna-1,4,16-triene-3,20-dione-21-acetate, is a steroid that produces deflazacort and nedd The key intermediate of corticosteroid drugs, using it as a raw material, can synthesize deflazacort through 3-step reactions, and can also prepare desonide and budesonide through 3-step reactions. Deflazacort, a third-generation steroidal glucocorticoid drug, is mainly used clinically for primary and secondary adrenal cortical insufficiency, rheumatism, collagen disease, skin disease, fulminant and The treatment of disseminated pulmonary tuberculosis, hematopoietic system diseases, ulcerativ...

Claims

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