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Method for synthesizing cefotiam

A kind of technology of cefotiam and synthesis method, which is applied in the field of drug synthesis and achieves the effect of high yield

Inactive Publication Date: 2013-01-30
南通康鑫药业有限公司
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  • Abstract
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Problems solved by technology

At present, there are few domestic research reports on the industrialization of cefotiam

Method used

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  • Method for synthesizing cefotiam
  • Method for synthesizing cefotiam
  • Method for synthesizing cefotiam

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Embodiment Construction

[0040] In order to enable the public to fully understand the technical essence and beneficial effects of the present invention, the applicant will describe in detail the specific embodiments of the present invention below, but the applicant's description of the embodiments is not a limitation to the technical solution. Changes in form rather than substance should be regarded as the protection scope of the present invention.

[0041] A synthetic method for cefotiam, comprising the following reaction steps:

[0042] (1) Preparation of 7-aminocephalosporanic acid-3-1-(2-dimethylaminoethyl)-1H-5-mercapto-tetrazolium 2HCl (Ⅰ)

[0043] At room temperature, successively add 180ml of acetonitrile, 30g of 7-aminocephalosporanic acid and 20.9g of 1-(2-dimethylaminoethyl)-1H-5-mercapto-tetrazolium in a three-necked flask, stir and mix well , drop into 130ml BF 3 Acetonitrile, dropwise, react at 20-25°C for 5 hours, after the reaction is over, add 400ml of acetone and 24g of concentrate...

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Abstract

The invention discloses a method for synthesizing cefotiam. The method comprises the following steps of: reacting acetonitrile, 7-aminocephalosporanic acid and 1- (2-bimethylaminoethyl)-1H-5-mercapto-tetrazole raw materials to obtain a 7-amino-3-[1-(2-bimethylaminoethyl)-1H-tetrazol-5-yl)thiomethyl]cefozopran dihydrochloride; reacting the product with pure water and isopropanol, decoloring the product of the reaction to obtain 7-amino-3-[1-(2-bimethylaminoethyl)-1H-tetrazole-5-yl)thiomethyl]cefozopran hydrochloride; reacting the compound and processing the product of the reaction to obtain formylamino cefotiam; reacting formylamino cefotiam with isopropanol, pure water and hydrochloric acid to obtain coarse cefotiam; and refining twice to obtain finished cefotiam. The method has the advantages that the prepared cefotiam is white powder and the cefotiam yield is as high as 33%; and the method is suitable for industrial production application.

Description

technical field [0001] The invention belongs to the field of drug synthesis, in particular to a method for synthesizing cefotiam. Background technique [0002] Cefotiam, the chemical name is (6R,7R)-7-[(2-amino-4-thiazolyl)acetamido]-3-[[1-[2-(dimethylamino)ethyl]- 1H-tetrazol-5-yl]thio]methyl]-8-oxo-5-thio-1-azabicyclo[4.2.0]octene-2-carboxylic acid, the second Substitute this synthetic cephalosporin. Clinically, its dihydrochloride is mainly used to treat various infections caused by sensitive bacteria. At present, there are few research reports on the industrialization of cefotiam in China. Contents of the invention [0003] The purpose of this invention is to provide a kind of synthetic method of cefotiam. [0004] In order to solve the problems of the technologies described above, the technical scheme adopted in the present invention is: a kind of synthetic method of cefotiam, it is characterized in that: comprise following reaction steps: [0005] (1) Preparatio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/36C07D501/04
Inventor 唐子安
Owner 南通康鑫药业有限公司
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