Method for preparing ceftaroline side-chain acid

A hydrochloric acid aqueous solution, ethoxyiminoacetic acid technology, applied in the direction of organic chemistry, etc., can solve the problems of low yield of amino deprotection reaction, harsh process reaction conditions, low total yield, etc., and achieves great implementation value and social economy. Benefit, good stereo selection, high stereo selectivity
CN102558094AInactive Publication Date: 2012-07-11ZHEJIANG UNIV OF TECH +1
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ZHEJIANG UNIV OF TECH
Publication Date
2012-07-11
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a method for preparing ceftaroline side-chain acid shown as a formula (I). The method comprises the following steps of: performing oximation reaction on 5-amino-1,2,4-thiadiazole-3-acetamide derivative and nitrite under catalysis of concentrated hydrochloric acid, performing esterification reaction with an ethylation reagent in the presence of organic alkali, dissolving in an aqueous solution of inorganic alkali, and thus obtaining the ceftaroline side-chain acid. The method has the advantages of mild reaction conditions, simplicity and convenience in operation, good reaction selectivity, high yield, short production period, low 'three-waste' quantity, easiness in industrialization and high implementation value and social and economic benefits.
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Description

(1) Technical field

[0001] The invention relates to a preparation method of ceftaroline side chain acid. (2) Technical background

[0002] In recent years, the problem of antibiotic resistance has become increasingly serious. With the increasing drug resistance of bacteria, especially the strong drug resistance of methicillin-resistant Staphylococcus aureus (MRSA), the development of new antibiotics is challenged. Currently, the commonly used antibiotics against MRSA are vancomycin and Linezolid, but both antibiotics are relatively weak against Gram-negative bacteria.

[0003] Ceftaroline Fosamil, developed by Japan's Takeda Pharmaceutical Company, the US Forest Laboratories (Cerexa) company obtained market authorization, and was approved for marketing by the US Food and Drug Administration on October 29, 2010. It belongs to the fifth generation A cephalosporin antibiotic that has antibacterial activity against Staphylococcus aureus (MRSA), multidrug-resistant Streptococcu...

Claims

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