Preparation method of 7-amino-6-demethylation-6-deoxy tetracycline and minocycline hydrochloride

A technology of minocycline hydrochloride and deoxytetracycline, which is applied in the preparation of carboxylic acid amides, the preparation of organic compounds, organic chemical methods and other directions, can solve the problems of small safety risk and complicated process operation.
CN112645832AActive Publication Date: 2021-04-13台州达辰药业有限公司
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
台州达辰药业有限公司
Publication Date
2021-04-13

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Abstract

The invention relates to a preparation method of 7-amido-6-demethylation-6-deoxy tetracycline and minocycline hydrochloride, and particularly provides a preparation method of 7-amido-6-demethylation-6-deoxy tetracycline. The preparation method comprises the following steps: (1) carrying out chlorination reaction on 6- preparation method-6-deoxy tetracycline and a chlorination reagent, and obtaining a chlorination product; carrying out azo reaction on the chlorination product and an azo reagent to obtain a reaction solution containing 7-p-benzenesulfonic acid azo group-11a-chloro-6-demethylation-6-deoxy tetracycline; and (2) adding a reducing reagent into the reaction solution containing the 7-p-benzenesulfonic acid azo group-11a-chloro-6-demethylation-6-deoxy tetracycline obtained in the step (1), and carrying out a reaction to obtain the 7-amido-6-demethylation-6-deoxy tetracycline. The synthesis method of minocycline hydrochloride has the advantages of simple synthesis process, high yield, high purity, easiness in large-scale production and the like.
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Description

technical field

[0001] The invention relates to the field of drug synthesis, in particular to a preparation method of 7-amino-6-desmethyl-6-deoxytetracycline and minocycline hydrochloride. Background technique

[0002] Minocycline hydrochloride, also known as minocycline or minocycline, is a broad-spectrum antibacterial tetracycline antibiotic. It can combine with t-RNA to achieve antibacterial effect. Minocycline has a broader antibacterial spectrum than similar drugs and has antibacterial activity. The antibacterial spectrum is similar to that of tetracycline, and it has a strong effect on Gram-positive bacteria including tetracycline-resistant Staphylococcus aureus, Streptococcus and Neisseria gonorrhoeae in Gram-negative bacteria; it also has a strong effect on Chlamydia trachomatis and Mycoplasma urealyticum Good inhibitory effect.

[0003] Minocycline hydrochloride, Minocycline hydrochloride, CAS: 13614-98-7, light yellow-orange amorphous solid, soluble in water, sl...

Claims

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