Synthesis method for biapenem

Abstract

The invention is a synthesis method of the biapenem, with the MAP ((1R, 5R, 6R) 2-(drophenyl phosphate)-6-[(R)-1- hydroxyethyl]-1-methyl-1-1 - carbapenems-2-en-3-formic acid benzyl ester of p-nitrophenol)) and the 6, 7-dihydro-6-mercapto-5 H-pyrazol [1,2 - a] [1,2 , 4]-triazole chloride ( the intermediate III) as the starting materials; after the condensation, hydrolysis and the fine preparation reaction and synthesis, the biapenem is made.

Description

technical field [0001] The invention relates to a synthesis method of antibiotic medicine, in particular to a synthesis method of biapenem. Background technique [0002] Carbapenem antibiotic drugs have a wide range of applications. Since the discovery of thiamycin in 1976, a series of new carbapenem antibiotics have been discovered and developed, such as imipenem, panipenem, meropenem, Faropenem, Biapenem, ritipenem acexil, etc. The most important feature of this kind of antibiotics is that they not only have strong antibacterial activity and broad antibacterial spectrum, but also are highly stable to various B-lactamases, and can still exert a strong antibacterial effect on cephalosporin-resistant bacteria. Bacteria do not have cross-resistance to this class of drugs and other B-lactam antibiotics. The development and application of carbapenem antibiotics is expected to become the first-line treatment drug for refractory severe infection. At present, all the drugs used...

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Problems solved by technology

[0008] The disadvantage of this process is that MAP ((1R,5R,6R)-2-(diphenylphosphonic acid)-6-[(1R)-1-hydroxyethyl]-1-methyl-1-1-carbon p-nitrobenzyl penicillin-2-ene-3-carboxylate)) and 6,7-dihydro-6-mercapto-5H-pyrazol[1,2-a][1,2,4]-triazol Azole chloride (intermediate III) is used as the starting material to synthesize biapenem through condensation, hydrolysis, and refining reactions. Although the raw material is easy to obtain and the reaction conditions are mild, it is difficult to synthesize, and the multi-step reaction needs to go through the column layer. Analysis, the yield is low, and the by-products that produce energy in the reaction process are not suitable for labor protection in industrialized production

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