Preparation method for compound cortisone acetate

Abstract

The invention discloses a preparation method of a compound cortisone acetate. The method takes a compound 4-pregnen-11(alpha),17(alpha)-alcohol-3,20-diketone (I) as a raw material and a mixed solution of chromic anhydride, sulfuric acid and water as an oxidation reagent, and comprises the following steps of: oxidizing the eleventh site to obtain a compound 4-pregnen-17(alpha)-alcohol-3,11,20-triketone (II); then iodizing the twenty-first site to obtain a compound 4-pregnen-21-iodine-17(alpha)-alcohol-3,11,20-triketone (III); and finally performing a replacement reaction to enable the compound 4-pregnen-21-iodine-17(alpha)-alcohol-3,11,20-triketone (III) to react with potassium acetate in a replacement reaction solvent to obtain a compound 4-pregnen-21-iodine-17(alpha),21-diol-3,11,20-triketone-21-acetate (IV), namely cortisone acetate. Through the invention, the dangerous operation of bromination and hydrogenation reaction can be avoided, the product yield can be improved, the process cost can be lowered, and the production is more economical, safer and more environment-friendly, thus the method is more suitable for industrial production.

Description

technical field

[0001] The invention relates to a chemical synthesis method of a medicine, in particular to a preparation method of a compound cortisone acetate. Background technique

[0002] The compound cortisone acetate is an adrenal cortical hormone drug, which has effects on glucose metabolism, anti-inflammatory, anti-allergic, and anti-toxic effects. It is mainly used for the treatment of primary or secondary adrenal insufficiency and various types of congenital adrenal hyperplasia caused by the deficiency of the enzymes required for the synthesis of glucocorticoids. If necessary, its pharmacological effects can also be used to treat various diseases. , including: 1. Autoimmune diseases: such as systemic lupus erythematosus, vasculitis, polymyositis, dermatomyositis, Still's disease, Graves' eye disease, autoimmune hemolysis, thrombocytopenic purpura, myasthenia gravis; 2. Allergic diseases, such as severe bronchial asthma, anaphylactic shock, serum sickness, atopic ...

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