Method for preparing hydrocortisone acetate

Abstract

The invention relates to a method for preparing hydrocortisone acetate. Three to twenty parts of dipolar aprotic solvent (including but not limited to dimethyl formamide or dimethyl sulfoxide and the like) is taken as the solvent, 0.1 to 1.5 parts of cheap organic amine (including but not limited to triethylamine, ethanediamine or piperidine and the like) is taken as the catalyst, one part of hydrocortisone and 0.4 to 1.0 part of acid anhydride react for 2 to 8 hours at 15 to 80 DEG C, and the hydrocortisone acetate can be prepared through adding water. The method replaces pyridine with low-toxic solvents, thereby reducing the environmental pollution and increasing the yield. The yield of the hydrocortisone acetate can reach more than 95 percent, the single maximum impurity is 0.82 percent, and the total impurity is 1.68 percent. The method stabilizes the product quality, reduces the cost, and is more suitable for large-scale industrialized production.

Description

technical field [0001] The invention belongs to the technical field of organic chemical synthesis, and relates to a preparation method of hydrocortisone acetate. Background technique [0002] Hydrocortisone acetate is mainly used to treat rheumatoid arthritis, rheumatic fever, gout, and bronchial asthma. 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. Is an important corticosteroid drugs. [0003] Hydrocortisone acetate is mainly prepared by the reaction of hydrocortisone and acetic anhydride. Traditionally, pyridine is used as a solvent and catalyst for reaction to prepare hydrocortisone acetate. Its disadvantage is that pyridine is highly toxic, has an unpleasant smell, and is easy to cause harm to the human body. Co...

AI Technical Summary

Problems solved by technology

Its disadvantage is that pyridine is highly toxic, smells bad, and is easy to cause harm to the human body.

Although acetone, methyl ethyl ketone and other low-toxic solvents have been used instead of pyridine, the synthesis process is more complicated, the solvents used are flammable and explosive, and the safety is poor, and there are potential safety hazards in large-scale industrial production.