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Method of synthesizing antibiotics cefamandole nafate

A technology of cefamandide sodium and a synthesis method, which is applied in directions such as organic chemistry, can solve problems such as affecting acylation reaction, increase manufacturing cost, increase operation steps, etc., and achieves simple process operation, good product quality and product yield high effect

Active Publication Date: 2008-01-23
苏州盛达药业有限公司
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  • Abstract
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Problems solved by technology

In this method, the by-product ammonia gas produced in the silylation reaction needs to be removed from the silylation reaction system as much as possible, otherwise it will affect the acylation reaction. Additional fulvic acid agent is used to neutralize the hydrogen chloride produced, and the used phosphonic acid agent N, N-dimethylaniline has carcinogenic toxicity, and cefamandoleic acid needs to be separated separately in the process, which increases the operation steps and reduces Yield, thus increasing the manufacturing cost of the product

Method used

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  • Method of synthesizing antibiotics cefamandole nafate

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Embodiment

[0025] In a 500ml four-necked reaction flask, add 300ml ethyl acetate, 30g 7-ATCA (0.092mol), control the temperature at 20~25℃, add 13.5ml HMDS (0.064mol), add 8.2ml dropwise while stirring Trimethylchlorosilane (0.064mol). After the dropwise addition is completed, the temperature is raised to 35-40°C for reaction, and after 3 to 4 hours of reaction, the temperature is lowered to 25-30°C to obtain a silicon ester solution of 7-ATCA.

[0026] Add 15.6ml D-(-)-2-formyloxy-2-phenylacetyl chloride (0.092mol) dropwise to the above-mentioned 7-ATCA silicon ester solution. After 30 minutes of dropping, keep the temperature at 25 At -30°C, the reaction was carried out with stirring for 1.5 to 2 hours, and the end of the reaction was detected by HPLC (the concentration of remaining 7-ATCA in the reaction solution was less than 1 mg / ml).

[0027] 200ml of deionized water was added to carry out the hydrolysis reaction, stirred for 20 minutes, the water layer was removed, the organic layer c...

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Abstract

The invention relates to a synthetic method of the antibiotic cefamandole nafate, which adopts the 7-amino-3-(1-methyl-1H-tetrazoline-5-base)-sulfomethyl-3-cef-4-carboxylic acid as raw material and gains the solid of the cefamandole nafate through such five steps as the silylation reaction, acylation reaction, hydrolysis reaction, decolorization and salifying. The silanizing agent used in the silylation reaction adopts the mixture of the silicon amine alkane and the alkylogen silane. Compared with the prior art, the invention is characterized by simple in process operation, low in cost, high in product yield, good in product quality and suitable for industrial production.

Description

Technical field [0001] The invention relates to a method for synthesizing antibiotic cefmendol sodium, which belongs to the field of drug synthesis. Cefmendolin sodium is mainly used to prepare injection powder injections and oral preparations and other dosage forms, and is widely used in clinical practice. Background technique [0002] Cefmendol sodium belongs to the second-generation cephalosporin antibiotics, and its chemical name is 7-D-(2-formyloxyphenylacetamide)-3-[(1-methyl-1H-tetrazol-5yl )Sulfomethyl]-3-cephem-4-carboxylic acid sodium salt, this product is the second-generation cephalosporin antibiotic originally developed by Lilly Company of the United States. [0003] Cefmendol Sodium is a prodrug of Cefmendol, its antibacterial activity is only 1 / 5 of Cefmendol. Cefmendol sodium enters the body and rapidly hydrolyzes to Cefmendol, so the antibacterial effects of the two in the body are basically the same. . Cefmendole has a strong antibacterial effect on most gram-po...

Claims

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Application Information

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IPC IPC(8): C07D501/36
Inventor 方长明
Owner 苏州盛达药业有限公司
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