Preparation method for Aspoxicillin

A technology of apicillin and aspartic acid, which is applied in the field of the preparation of the first product of apicillin, can solve the problems of increasing the preparation cycle, unsafe industrial production, inconvenient deprotection and the like, and achieves easy operation, toxicity and environmental impact. The effect of low pressure, easy storage and transportation
CN102408437AInactive Publication Date: 2012-04-11SOUTHWEST JIAOTONG UNIV
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SOUTHWEST JIAOTONG UNIV
Publication Date
2012-04-11
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a preparation method for Aspoxicillin. D-aspartic acid is added into a mixture liquid of sulfuryl chloride and carbinol under a low temperature of zero to prepare D-aspartic acid methyl ester hydrochloride; the obtained D-aspartic acid methyl ester hydrochloride and triethylamine are reacted in ethanol to obtain D-aspartic acid methyl ester educt; the D-aspartic acid methyl ester educt and methylamine aqueous liquid with a concentration of 40 percent are reacted in a room temperature to prepare aspartic formamide; the aspartic formamide, ethyl acetoacetate and potassium hydroxide are reacted in isopropanol to prepare diene salt (D-2-amino-3N-methylamino oxo-propionic acid diene formamide); the diene salt and pivaloyl chloride are reacted in acetone under the catalysis of pyridine to obtain active anhydride; then the active anhydride is condensed and further protected by deacidification to obtain a target product-crude product of Aspoxicillin. The preparation method for Aspoxicillin has the advantages of cheap and easily-obtained reagent, lower toxicity and lower environment pressure, stable and simple technological operation and high yield.
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Description

technical field

[0001] The invention relates to the technical field of chemical pharmacy, especially the preparation of primary apoxicillin. Background technique

[0002] Apoxicillin is a synthetic penicillin that inhibits the synthesis of bacterial cell walls. Using different parts of Escherichia coli K-12 membrane, the results of affinity for penicillin-binding protein show that this product has high affinity for PBPS-2, 1A, 1BS, and 3 sites, and has strong inhibition on the formation of peptidoglycan bridging effect. This product has strong antibacterial effect on Staphylococcus, Streptococcus, Enterococcus, and Pneumococcus of Gram-positive bacteria, excellent antibacterial effect on Escherichia coli and influenza bacilli of Gram-negative bacteria, and has excellent antibacterial effect on anaerobic bacteria Bacteroides have antimicrobial properties. Combined use with aminoglycoside system antibiotics can achieve synergistic effect. Especially when combined with gent...

Claims

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