Novel preparation of budesonide

Abstract

The invention in particular relates to a new method to prepare budesonide, belonging to medicinal synthesis. The method simplifies production process through repeated tests and experiments, greatly improves yield, reduces prodiction cost and works out the optimum temperature, time and solvent for the reaction; the conditions during the reaction are easy to realize; therefore the method is applicable to large-scale industrial production to produce budesonide.

Description

technical field [0001] The invention belongs to the field of medicine synthesis, and in particular relates to a new preparation method of the anti-asthma drug budesonide. Background technique [0002] Budesonide was developed by AstraZeneca Pharmaceutical Co., Ltd. and launched in 1981. It is an acetal-type glucocorticoid with strong anti-inflammatory effect. It is significantly stronger than beclomethasone dipropionate and other glucocorticoids, has a long acting time and has no systemic adrenal cortex hormone effect, and is more suitable for local administration. It is the first-line drug for aerosol inhalation to treat asthma and nasal spray to treat allergic reactions. Budesonide has two configurations, R and S, of which the R configuration is more effective than the S configuration. The structural formula of budesonide is (V), [0003] [0004] There have been many reports on the synthetic route and process of (V) at home and abroad, and there are mainly two synthe...

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Problems solved by technology

[0005] In U.S. Patent No. 3,536,586, a method for synthesizing budesonide using hydrocortisone as a starting material and a semi-biosynthetic method using bacterial strains is disclosed, but the semi-biosynthetic method often requires continuous synthesis due to the complexity of the product of oxidative dehydrogenation. Multi-stage countercurrent extraction and separation, the process is complicated, the technology and equipment requirements are high, and the source and screening of bacteria are difficult to solve domestically within a period of time, and the cost of industrial production is too high

[0006] In European patent EP0164636 and U.S. patent US3929768, the chemical synthesis method and process route of preparing budesonide with prednisone acetate as the starting material are disclosed, but the general existence of high equipment requirements and low yield in the industrial process production process , The steps are cumbersome, the raw materials are expensive and not easy to obtain, and the industrial production cost is too high

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