Method for preparing 9,11beta-epoxy steroid compound

A technology of epoxy steroids and compounds, which is applied in the field of preparation of key intermediates 9,11β-epoxy steroids, and can solve problems affecting product quality and yield
CN103588853AInactive Publication Date: 2014-02-19AURISCO PHARMACEUTICAL CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
AURISCO PHARMACEUTICAL CO LTD
Publication Date
2014-02-19
Estimated Expiration
Not applicable · inactive patent

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Abstract

The present invention provides a method for preparing a 9,11beta-epoxy steroid compound represented by a formula 1. According to the method, a 9,11-double bond-21-ester steroid compound is adopted as a raw material, and reacts with a halogenating agent in a suitable organic solvent containing 70% perchloric acid to produce a 9alpha-halo-11beta-ester-21-ester steroid compound, and the 9alpha-halo-11beta-ester-21-ester steroid compound reacts with a strong base in an organic solvent to obtain the 9,11beta-epoxy steroid compound. The 9,11beta-epoxy steroid compound can be used for preparation of dexamethasone, betamethasone and series other drugs. According to the present invention, the 9,11beta-epoxy steroid compound can be prepared from the almost equimolar amount of the 9,11-double bond-21-ester steroid compound, such that the method is the synthesis method with characteristics of economy, efficiency and environmental protection.
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Description

technical field

[0001] The present invention relates to medicinal chemistry, in particular to a preparation method of a pharmaceutical intermediate, in particular to a preparation method of a key intermediate 9,11β-epoxy steroid used in the preparation of dexamethasone and betamethasone series medicines. Background technique

[0002] 9,11β-epoxy steroids are key intermediates of dexamethasone series and betamethasone series of drugs, and their structural formula (Formula 1) is as follows:

[0003]

[0004] Dexamethasone or betamethasone can be easily prepared from 9,11β-epoxy steroids by fluorination at the 9-position, and a series of drugs can be prepared through a series of modifications at the 3-position, 6-position, 16-position, and 21-position.

[0005] In Chinese patent CN101397319, a kind of 9,11β-epoxy steroid is prepared by generating halides in aliphatic alcohol, halogenated hydrocarbon, ketones or ether solvents, then using alkali to epoxidize and then hydrolyz...

Claims

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