Synthesis process of hydrocortisone hemisuccinate

A technology of hydrocortisone and succinate, applied in steroids, organic chemistry, etc., can solve the problem of triethylamine catalytic reaction activity, low selectivity, large amount of succinic anhydride and reaction solvent, pine hemisuccinic acid, etc. The problem of low ester yield is to achieve the effect of process optimization, simple post-processing operation and reduction of processing cost.
CN112225772AInactive Publication Date: 2021-01-15安徽海洋药业有限公司
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
安徽海洋药业有限公司
Publication Date
2021-01-15
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides a synthesis process of hydrocortisone hemisuccinate, which comprises the steps of: sequentially adding a solvent, hydrocortisone, succinic anhydride and a catalyst to a reactionkettle according to a feeding ratio, heating the reaction system, starting stirring, carrying out thermal insulation, carrying out a sufficient reaction, cooling, adding purified water, carrying outcrystal precipitation, and carrying out centrifugal filtration, and finally, drying the product in vacuum. Through solvent and catalyst selection and proportion optimization, a single solvent is adopted, the reaction selectivity is high, almost quantitative completion is achieved, the yield reaches 98-99%, and the impurity content is far lower than the limit of BP2013 (British Pharmacopoeia 2013 edition).
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Description

technical field

[0001] The invention relates to the field of chemical drug synthesis, in particular to a synthesis process of hydrocortisone hemisuccinate. Background technique

[0002] Hydrocortisone hemisuccinate is an esterification product of hydrocortisone, which belongs to adrenal glucocorticoid drugs, and has anti-inflammatory, anti-shock and anti-allergic effects. Clinically, it is mainly used for adrenal glucocorticoid insufficiency, allergic diseases such as acute bronchial asthma, bronchitis, and acute ophthalmia, etc. It is also used for high fever caused by some serious infections. Compared with hydrocortisone, its Longer half-life, longer duration of curative effect. In addition, hydrocortisone hemisuccinate can also be used for the preparation of clinical water-soluble corticosteroid hydrocortisone sodium succinate except supplying clinical application, so successfully synthesized hydrocortisone hemisuccinate and improve its output namely appears to be parti...

Claims

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