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Preparation technology for cefathiamidine

A cefathiamidine, preparation technology technology, applied in the field of cefathiamidine preparation technology, to achieve the effect of process stability

Active Publication Date: 2014-09-24
JIANGSU HI STONE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] In the preparation process of cefathiamidine, the crude product of cefathiamidine needs to be synthesized first, and then refined into finished cefathiamidine, especially the control of the freeze-drying step plays an important role in the quality and stability of the product, but the domestic This is rarely reported

Method used

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  • Preparation technology for cefathiamidine
  • Preparation technology for cefathiamidine
  • Preparation technology for cefathiamidine

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Embodiment Construction

[0030] The preferred embodiments of the present invention will be described in detail below in conjunction with the accompanying drawings, so that the advantages and features of the present invention can be more easily understood by those skilled in the art, so as to define the protection scope of the present invention more clearly.

[0031] see figure 1 and figure 2 The preparation process of cefathiamidine of the present invention comprises the synthesis of cefathiamidine crude product and the refining process of cefathiamidine, specifically comprising the following steps:

[0032] (1) Synthesis of crude cefathiamidine (based on a batch size of 90kg):

[0033] (110) Before the start of production, check that there are no products, documents or materials unrelated to the production of this batch of products left over from the previous batch in the workplace, and the equipment is in a clean and ready-to-use state; Valves, measuring instruments, monitoring instruments and au...

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Abstract

The invention discloses a preparation technology for cefathiamidine. The preparation technology specifically comprises the steps that dichloromethane and N,N'-Diisopropyl thiourea are evenly stirred, dichloromethane, acetyl bromide aminocephalosporanic acid and triethylamine are stirred and dissolved, the materials are sucked into the same reaction kettle after dissolution, a condensation reaction is carried out, then crude cefathiamidine is obtained after cooling crystallization, suction filtration washing and vacuum drying, and the crude cefathiamidine is refined through lyophilization to obtain the finished cefathiamidine. The technology is stable, the high-quality and high-purity cefathiamidine can be obtained, and the yield can reach 80.0% to 88.0%.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to a preparation process of cefathiamidine. Background technique [0002] Cephathiamidine, chemical name (6R,7R)-3-[(acetoxy)methyl]-7-[α-(N,N-diisopropylamidinothio)acetamido]- 8-Oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid betaine, the structural formula is , the molecular formula is C 19 h 28 N 4 o 6 S 2 , is white or off-white crystalline powder, almost odorless, hygroscopic, easily soluble in water, slightly soluble in ethanol, insoluble in acetone, chloroform or ether. The antibacterial spectrum of cefathiamidine is similar to that of cefalotin, and it has a stronger effect on Staphylococcus aureus, Streptococcus viridans, and pneumococcus, and has unique antibacterial activity against Enterococcus, and is mainly used for staphylococcus aureus, pneumococcus and streptococcus. Cause respiratory tract infection, biliary tract infection, urinary tract ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/04C07D501/12C07D501/28
CPCC07D501/04C07D501/12C07D501/28
Inventor 王多平
Owner JIANGSU HI STONE PHARMA
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