Preparation method of R budesonide

Abstract

The invention relates to the field of medicinal chemistry, in particular to a preparation method of new R budesonide, which is characterized in that a budesonide product is synthesized by carrying out microwave catalytic reaction on the 16-alpha hydroxyl prednisolone and n-butanal in the presence of a mixed catalyst, wherein the content of the R budesonide is more than 95 percent.

Description

[0001] technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a preparation method of anti-asthma drug R budesonide. Background technique Budesonide was developed by AstraZeneca Pharmaceutical Co., Ltd. and launched in 1981. It is a corticosteroid drug with strong anti-inflammatory effect. Topical medication is the first-line drug for the treatment of asthma by aerosol inhalation and nasal spray for allergic reactions. Its 22-position carbon is R and S chiral stereoisomers. The anti-inflammatory effect of R is two to three times higher than that of S, the metabolism speed is twice as fast, and the pharmacokinetic performance is better. In particular, the side effects of the R isomer are relatively small when used for a long time. The structural formulas of R and S are as follows: For the synthesis of budesonide, there are a large number of relevant reports, and there are mainly the following synthetic methods for th...

AI Technical Summary

Problems solved by technology

Most of the above synthetic methods use highly corrosive hydrofluoric acid as a catalyst, and the reaction temperature is demanding, the steps are cumbersome, the reaction cycle is long, the total yield is not high, and the industrialization cost is high

Images