Synthesis method of cefpodoxime proxetil intermediate

A technology of cefpodoxime axetil and a synthesis method is applied in the field of intermediate preparation of cefpodoxime axetil, can solve the problems of low yield, inability to proceed, low yield and purity, etc., and achieves high product yield and purity, high post-processing Uncomplicated and cost-effective
CN105669701AInactive Publication Date: 2016-06-15陕西思尔生物科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
陕西思尔生物科技有限公司
Publication Date
2016-06-15
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a synthesis method of a cefpodoxime proxetil intermediate, namely (6R,7R)-7-[2-(2-amino-4-thiazolyl)-(Z)-2-(methoxyimino)acetamido]-3-methoxymethyl-8-oxo-5-thio-1-azabicyclo[4.2.0]oct-2-ene-2-methanoic acid. The synthesis method includes: enabling chlorosulfonic acid and methanol to react to prepare methoxy sulfonic acid; under the action of the methoxy sulfonic acid and dimethylformamide, etherifying 7-ACA (7-aminocephalosporanic acid) and trimethyl borate prior to aftertreatment, adding into a water and methanol solution reversely to guarantee that the obtained intermediate isn't sticky and is loose, drying and grafting with AE active ester so as to obtain a target product, namely the cefpodoxime proxetil intermediate. The synthesis method of the cefpodoxime proxetil intermediate has the advantages that synthesis steps of 3-position and 7-position protection and desorption of 7-ACA can be omitted, so that low step cost, high yield and high purity are achieved, all materials are cheap and available, and industrial production and little pollution are benefited.
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Description

technical field

[0001] The invention belongs to the technical field of preparation of cefpodoxime axetil intermediate, in particular to a cefpodoxime axetil intermediate (6R,7R)-7-[2-(2-amino-4-thiazolyl)-(Z)-2 Synthetic method of -(methoxyimino)acetamido]-3-methoxymethyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid . Background technique

[0002] Cefpodoxime axetil is an oral third-generation cephalosporin with a broad antibacterial spectrum. After entering the body, it is hydrolyzed into cefpodoxime by non-specific enzymes to exert antibacterial effects. It has a wide range of antibacterial effects on Gram-positive and Gram-negative bacteria. Spectrum, stable against β-lactamases.

[0003] Cefpodoxamic acid is the premise intermediate of cefpodoxime axetil. Patent WO2013041999A once reported that it was synthesized with expensive methanesulfonic acid and 7-aminocephalosporin acid, but according to literature reports, the yield and purity were low, and the ...

Claims

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