Synthesis method of cefathiamidine compound

A synthetic method, cefathiamidine technology, which is applied in the field of synthesis of cephalosporins and cefathiamidine compounds, can solve the problems of deepening color, low crude product content, complexity, etc., achieves improved purity and yield, easy separation and purification, and synthesis The effect of simple process
CN101704827BInactive Publication Date: 2012-01-11HAINAN LINGKANG PHARMA CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
HAINAN LINGKANG PHARMA CO LTD
Publication Date
2012-01-11
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides a novel route for cefathiamidine compounds. The new route comprises the following steps of: reacting N,N'-diisopropyl thiourea and sodium bicarbonate, adding 2-bromacetic acid in the mixture for reaction, adding triphosgene and triphenylphosphine oxide serving as catalysts, reacting the product of the previous reaction with N,N'-diisopropyl amidine sulfur radical acetic acid to obtain solution(A), and adding the solution(A) to aqueous solution of 7-ACA dropwise for reaction to obtain the target product. The cefathiamidine compounds prepared by the method have the advantages of higher purity and yield, low-priced raw materials, simple synthesis process, simple equipment and easy separation and purification of products.
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Description

technical field

[0001] The invention relates to a cephalosporin compound, in particular to a synthesis method of a cefathiamidine compound, and belongs to the technical field of chemical synthesis. Background technique

[0002] Cefathiamidine, its chemical name is: (6R,7R)-3[(acetoxy)methyl]-7-[α-(N,N'-diisopropylamidinothio)-acetamido]8- Oxo-5-thia-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylate betaine, molecular formula C 19 h 28 N 4 o 6 S 2 , molecular weight 472.59, structural formula:

[0003]

[0004] It is a β-lactam antibiotic, the first-generation cephalosporin, and its antibacterial spectrum is similar to that of cephalothin. It has strong antibacterial effect on G+ bacteria, especially has a unique effect on G+ enterococci. A cephalosporin exclusive to cocci. It is mainly used for respiratory tract infection, biliary tract, urinary tract, gynecological diseases, sepsis, pneumonia, meningitis and other infections caused by sensitive bacteria. Sterile crystall...

Claims

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