Synthetic method for high-purity tigecycline

A technology of tigecycline and its synthesis method, which is applied in the fields of chemical instruments and methods, preparation of organic compounds, organic chemistry, etc., and can solve problems such as difficulty in purity, high adverse reactions of patients, difficulty in meeting the quality requirements of injection raw materials, etc.
CN102391148AActive Publication Date: 2012-03-28NANJING HAIRUN PHARM CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
NANJING HAIRUN PHARM CO LTD
Publication Date
2012-03-28

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Abstract

The invention relates to a novel preparation method for antibioticdrug tigecycline. 9-amino minocycline and N-tert-butyl group glycine are taken as starting materials. The novel preparation method is characterized in that the N-tert-butyl group glycine is dissolved in indifferent solvent, under the existence of an acidic acceptor and an amino acid condensating agent, reaction with 9-amino minocycline is carried out along the route of amino acid condensation for 3 hours to 10 hours, and then an indifferent solvent is cooled to a room temperature. Tigecycline is obtained through acidification, neutralization, extraction, drying, concentration and refining. In the preparation method disclosed by the invention, the operation is simplified, the purity of the obtained product reaches more than 99.5 percent, individual impurities are controlled to be lower than 0.1 percent, and an epimer is controlled to be lower than 0.5 percent; and the yield is high, the stability of the product is good, and the preparation method is suitable for industrial production.
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Description

technical field

[0001] The invention relates to a preparation method of antibiotic drug tigecycline, which belongs to the technical field of medicinal chemistry. Background technique

[0002] Tigecycline (tigecycline) chemical name (4S, 4aS, 5aR, 12aS)-4,7-bis(dimethylamino)-9-[(tert-butylamino)acetamido]-3,10,12, 12a-tetrahydroxy-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide is the first intravenous drug approved for clinical use Glycylcycline antibiotics administered internally, similar in structure to tetracyclines, were approved by the US FDA in June 2005 for complex skin and soft tissue infections in adults and complicated intra-abdominal infections in adults. The structural formula of tigecycline is:

[0003]

[0004] Although tigecycline and minocycline have many similarities in structure, the former is obviously superior to traditional tetracyclines in terms of antibacterial spectrum range and drug-resistant bacteria, and has broad-spectrum an...

Claims

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