Preparation of hydrocortisone and derivatives thereof

Abstract

The invention relates to a preparation method of steroids compounds, in particular to the preparation of hydrocortisone and derivatives thereof. The invention adopts 17-hydroxy-4, 9-diene-pregna-3, 20-diketone as the original material which is modified by 21 bits and 9, 11 bits so as to obtain anecortave acetate retaane, the hydrocortisone and hydrocortisone acetate, and the like. The technical process of the invention adopts the existing intermediates of manufacturers as the original material; the route is simple; the feasibility is high; the operability is strong; the materials are available; the use of expensive accessories is avoided so as to largely reduce the cost of industrial manufacturing; a plurality of products can be obtained on the same manufacturing line; the yield and the cost are dramatically better than that of the prior methods used for synthesizing the hydrocortisone and the derivatives thereof; moreover, the adoption of the existing intermediates realizes the combined-line production of triamcinolone acetonide series products, hydrocortisone series products and anecortave acetate series products so as to greatly reduce the manufacturing cost and the conditions for industrial manufacturing; wherein, R is equal to minus OCOR1 and R1 is equal to the alkyl with the carbon less than 11.

Description

technical field [0001] The present invention relates to a kind of preparation method of steroid compound, especially relates to the preparation of hydrocortisone and its derivative. Background technique [0002] Hydrocortisone and its derivatives are intermediate-acting adrenal cortex hormone drugs and are widely used clinically. Their products include: hydrocortisone and hydrocortisone acetate. Hydrocortisone Sodium Phosphate etc. Its curative effect is equivalent to that of prednisone, and its anti-inflammatory effect is stronger, which is 3 to 5 times that of cortisone. However, its water-salt metabolism effect is very weak, and it is generally not easy to cause side effects such as water and electrolyte disorders. At present, the products are oral and injection, and can also be applied externally to the skin. [0003] Synthetic technology of hydrocortisone and its derivatives has existed a long time ago, and the earliest hydrocortisone is taken out from animal adrenal ...

AI Technical Summary

Problems solved by technology

Secondly, in the part of chemical synthesis method, in the document 1 J.Am.Chem.Soc.72, 5793 (1950), the chemical method 4,5 dehydrogenation is used, the cost is high, and the pollution is relatively large

Document 2 The route of ZL92110286.0 is longer, and more expensive ethanedithiol is used to protect the 3-ketone, the cost is high, and the degree of industrialization is not high

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