The preparation method of ceftizoxime propivoxil and its intermediate and the preparation method of the intermediate

A technology of ceftizoxime propivoxil and esterification, which is applied in the field of preparation of intermediates and intermediates, and can solve problems such as high cost and harsh reaction conditions
CN105017284BActive Publication Date: 2018-05-11ZHEJIANG YONGNING PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZHEJIANG YONGNING PHARMA
Publication Date
2018-05-11

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Abstract

The present invention discloses a preparation method for ceftizoxime alapivoxil by using a mixture anhydrides method, intermediates 3a / 3b / 3c thereof and a preparation method for the intermediates . The method comprises: putting an ammonia cefotaxime acid ester compound in an organic solvent to react with BOC-alanine by using a mixture anhydrides method; hydrolyzing under condition of organic alcohol; generating intermediates 3a / 3b / 3c; the intermediates 3a / 3b / 3c condensation reacting with 7-ANCA in an organic solvent; generating BOC-alanyl ceftizoxime acid by esterification; the BOC-alanyl ceftizoxime acid reacting with halogenated pentanoic acid methyl ester in the presence of an acid-binding agent, to prepare BOC-alanyl ester ceftizoxime valproate; removing a BOC protection group; and after concentrating, obtaining the target compound ceftizoxime alapivoxil by crystal precipitation in the organic solvent. The preparation method for ceftizoxime alapivoxil has the advantages that raw materials are readily available, the reaction condition is mild, byproducts are fewer, purity is reliable, the yield is high, and the preparation method for ceftizoxime alapivoxil is suitable for large-scale industrial production.
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Description

technical field

[0001] The invention relates to a method for preparing ceftizoxime propivoxil by a mixed acid anhydride method, an intermediate and a preparation method of the intermediate. Background technique

[0002] Ceftizoxime propivoxil is a bifunctional oral prodrug of ceftizoxime for injection developed by Kyoto Pharmaceutical Company in Japan. It has a broad-spectrum antibacterial effect on Gram-negative bacteria and Gram-positive bacteria. Enzymes are stable. Its structure is characterized by the addition of fat-soluble groups and water-soluble groups, with balanced fat-soluble and water-soluble (fat-water partition coefficient is 1.5), which is conducive to its absorption in the intestinal tract, not only improves the oral absorption rate, but also reduces the The dosage is high, and it has high sweetness and low toxicity, so it is suitable for children.

[0003] At present, the synthesis of ceftizoxime propivoxil mainly contains the following three approaches: ...

Claims

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