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Method for preparing cefazolin compounds

A technology of cefazolin and cefamycin, which is applied in the field of preparation of antibacterial compounds, can solve problems such as environmental pollution and difficult treatment, and achieves the effects of high yield, simple recovery process and short operation steps

Active Publication Date: 2014-04-16
哈药集团股份有限公司 +1
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  • Summary
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AI Technical Summary

Problems solved by technology

[0010] However, the methods in the prior art use more toxic organic solvents and reagents, which are difficult to handle and cause some pollution to the environment. In addition, in order to obtain a high-purity product and a high-yield route to eliminate pollution simultaneously, it is necessary Using suitable solvents and reagents in the synthesis process, the present invention has found a synthesis method after screening, which solves the above problems

Method used

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Examples

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Embodiment 1

[0028] Step 1 cefazolin sodium three-position intermediate (TDA) is synthesized,

[0029] Add 50g of dimethyl carbonate and 69g of boron trifluoride-dimethyl carbonate into the condensation tank, start stirring, put 13g of thiadiazole and 25g of 7-ACA into the tank, and raise the temperature at the same time, the reaction temperature is 30-40°C, and react to The residue of 7-ACA was less than 1.0%. After the reaction, lower the temperature to below 10°C, transfer the reaction solution into a three-necked flask filled with 300ml of deionized water, add sodium carbonate solution dropwise to pH 2-4, lower the temperature to 10°C, and stir for 1 hour to grow crystals. Filter, wash with acetone and dry.

[0030] The preparation of step 2 acid anhydride

[0031] Dichloromethane 150ml, add 8.9g tetrazolium acetic acid, cool down to -50±1°C, add triethylamine dropwise within 15 minutes and stir until tetrazolium acetic acid is completely dissolved, maintain the temperature at -55±1°...

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Abstract

The invention belongs to the field of pharmacy and relates to a method for preparing cefazolin compounds. The method comprises the following steps that: 1, cefazolin sodium imidazo (toluene diamine TDA) is synthetized, thiadiazole and 7-ACA are obtained through reaction, dimethyl carbonate is used as solvents in the reaction, boron trifluoride-dimethyl carbonate is used as catalysts, and reagents used for regulating the pH of the reaction liquid are inorganic alkali after the reaction is completed; 2, anhydride is prepared, and the anhydride is obtained through the reaction between tetrazole acetic acid and pivaloyl chloride, and 3, the cefazolin is synthesized, TDA solution reacts with the anhydride, and the reaction solution is subjected to decoloration and purification through an aluminium oxide column.

Description

Technical field: [0001] The invention relates to a preparation method of an antibacterial compound, in particular to a preparation method of a cefazolin compound. Background technique: [0002] Cefazolin, the chemical name is (6R,7R)-3-[(5-methyl-1,3,4-thiadiazol-2-yl)thiomethyl]-8-oxo-7-[[ 2-(tetrazol-1-yl)acetyl]amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, cefazolin is the first generation semi-synthetic cephalosporin Bacterin has the same antibacterial spectrum as cephalexin, but its effect is stronger, and its blood concentration is higher at the same dose. The feature of this product is that it has a strong effect on Gram-negative bacteria, and has the advantages of acid resistance, high efficiency and low toxicity. It is clinically applicable to respiratory tract, urethra, pneumonia, cholecystitis, liver abscess, peritonitis, pelvic inflammatory disease, endocarditis, otitis media, sepsis and soft tissue infection caused by sensitive bacteria. [00...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D501/36A61P31/04
Inventor 王喜军王彪余威杨新春翁艳军
Owner 哈药集团股份有限公司
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