5679-00-5Relevant academic research and scientific papers
Synthesis method of minocycline hydrochloride
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, (2021/06/21)
The invention relates to a synthesis method of minocycline hydrochloride, which comprises the following steps of: (1) reacting demeclocycline with an amination reagent in a first organic solvent in the presence of a palladium metal complex to obtain 7-amino-6-demethyltetracycline; (2) carrying out a dehydroxylation reaction on the 7-amino-6-demethyltetracycline in a second organic solvent in the presence of a first acid reagent and a first catalyst, so as to obtain 7-amino-6-demethyl-6-deoxytetracycline; and (3) in a third organic solvent, in the presence of a second acid reagent and a second catalyst, carrying out alkylation reaction on the 7-amino-6-demethyl-6-deoxytetracycline and an alkylation reagent to obtain minocycline hydrochloride. The minocycline hydrochloride prepared by the method disclosed by the invention has the advantages of simple synthesis process, high yield, high purity and easiness in large-scale production.
Preparation method of 7-amino-6-demethylation-6-deoxy tetracycline and minocycline hydrochloride
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Paragraph 0324; 0325; 0330; 0331; 0334; 0335, (2021/04/14)
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.
Preparation method of 7-aminominocyclin
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Paragraph 0026-0028, (2019/10/02)
The invention discloses a preparation method of 7-aminominocycline (Formula I). Sancycline is used as the raw material, tetrahydrofuran is used as solvent under strong acid condition (trifluoromethanesulfonic acid) and sancycline directly reacts with dibenzyl azodicarboxylate, and the 7-aminominocyclin is obtained. The invention has the advantages of low cost and easy availability of raw materials, short synthesis steps, mild reaction conditions and simple post-treatment. The process is stable and reproducible, which greatly reduces the production cost and is beneficial to batch production.
Substituted Tetracycline Compounds
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Page/Page column 114, (2010/12/29)
The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms.
SUBSTITUTED TETRACYCLINE COMPOUNDS
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Page 28, (2010/02/10)
The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.
