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Production technology of hydrocortisone acetate

A technology of hydrocortisone acetate and hydrocortisone, which is applied in the directions of organic chemistry, steroids, etc., can solve the problems of large amount of catalyst, long reaction time, low yield, etc. Shortened time, good appearance effect

Active Publication Date: 2015-06-17
HENAN LIHUA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] The purpose of the present invention is to overcome defects such as poor quality, low yield, long reaction time and large catalyst consumption in the current production of hydrocortisone acetate, and provide a production process for hydrocortisone acetate

Method used

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  • Production technology of hydrocortisone acetate

Examples

Experimental program
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Effect test

Embodiment 1

[0021] Add 1kg of hydrocortisone, 0.04kg of barium acetate, and 3L of dimethylformamide into a dry and clean reaction tank replaced with nitrogen three times in advance, stir and dissolve, and heat up to 30°C, then add 0.4 times of hydrocortisone Loose weight of acetic anhydride, heat preservation reaction for 3 hours, nitrogen protection throughout the whole process, keep anhydrous, TLC detection of complete reaction, pour into ice water pre-cooled to 0-10 ℃, stir for 30 minutes, filter and dry to obtain 1.102kg of acetic acid hydrogenation cortisone. The yield is 110.2%, the largest single impurity is 0.30%, and the total impurity is 0.8%.

Embodiment 2

[0023] Add 3kg of hydrocortisone, 0.18kg of barium acetate, and 12L of dimethylformamide into a dry and clean reaction tank replaced with nitrogen three times in advance, stir and dissolve, and heat up to 40°C, then add 0.6 times of hydrocortisone Loose weight of acetic anhydride, heat preservation reaction for 3 hours, nitrogen protection throughout the whole process, keep anhydrous, TLC detection of complete reaction, pour into ice water pre-cooled to 0-10 ℃, stir for 30 minutes, filter and dry to obtain 3.309kg of acetic acid hydrogenation cortisone. The yield is 110.3%, the largest single impurity is 0.29%, and the total impurity is 0.78%.

Embodiment 3

[0025] Add 1kg of hydrocortisone, 0.1kg of barium acetate, and 4L of dimethylformamide into a dry and clean reaction tank replaced with nitrogen three times in advance, stir and dissolve, and heat up to 50°C, then add 1 times of hydrocortisone Loose weight of acetic anhydride, heat preservation reaction for 1 hour, nitrogen protection throughout the whole process, keep anhydrous, TLC detection of complete reaction, pour into ice water pre-cooled to 0-10 ℃, stir for 30 minutes, filter and dry to obtain 1.10kg of acetic acid hydrogenation cortisone. The yield is 110%, the largest single impurity is 0.29%, and the total impurity is 0.70%.

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Abstract

The invention discloses a production technology of hydrocortisone acetate, which belongs to the technical field of chemical pharmacy. The technology employs reaction of hydrocortisone and acetic anhydride to prepare the product, a reaction of hydrocortisone and acetic anhydride is carried out in a dipolar aprotic solvent, an alkali salt acetate is taken as a catalyst, the reaction is carried out under nitrogen or inert gas protection, and the dipolar aprotic solvent is dimethyl formamide or dimethyl sulfoxide. The technology has the advantages of high yield and good product quality.

Description

technical field [0001] The invention relates to a production process of cortisone hormone drugs, in particular to a production process of hydrocortisone acetate, which belongs to the technical field of chemical pharmacy. Background technique [0002] Hydrocortisone acetate is an important adrenal glucocorticoid drug, mainly used in the treatment of rheumatoid arthritis, rheumatic fever, gout, bronchial asthma and so on. Injections are used for tuberculous or suppurative meningitis, tuberculous pleurisy, empyema, arthritis, tenosynovitis, tendon strain, sprains, prurigo nodosa, lichen planus, etc. Eye drops are used for various ophthalmic conditions. Creams are used for allergic or seborrheic dermatitis, pruritus, etc. [0003] Hydrocortisone acetate is mainly prepared by the reaction of hydrocortisone and acetic anhydride, and the traditional process mostly uses pyridine as a solvent and catalyst for reaction to prepare hydrocortisone acetate. (see "Pharmaceutical Industr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J5/00
CPCC07J5/0053
Inventor 孟栋梁
Owner HENAN LIHUA PHARMA
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