Method for preparing intermediate in cephalosporins, and method for preparing ceftizoxime alapivoxil

This invention relates to a method for preparing cephalosporin intermediate, and ceftizoxime alapivoxil from the intermediate. The cephalosporin intermediate is 7-[[(Z)-2-protective amino-1-oxopropyl] amino-4-thiazole]-2-methoxyliminoacetyl] amino]-3-cephem-4-carboxylic acid or its ester. The method...

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Bibliographic Details
Main Authors PENG WEI, DONG CHUANMING, TANG BINZHEN, LIU YAOWU, LUO FAXIN, ZHANG FENGXIA
Format Patent
LanguageChinese
English
Published 11.08.2010
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:This invention relates to a method for preparing cephalosporin intermediate, and ceftizoxime alapivoxil from the intermediate. The cephalosporin intermediate is 7-[[(Z)-2-protective amino-1-oxopropyl] amino-4-thiazole]-2-methoxyliminoacetyl] amino]-3-cephem-4-carboxylic acid or its ester. The method comprises: reacting the compound shown in formula IV with dibenzothiazolesulfide and phosphate in the presence of organic solvent and catalyst to obtain active ester compound shown in formula II (intermediate II), acylating with the compound shown in formula III or its ester in the presence of organic solvent and appropriate alkaline substance to obtain the compound shown in formula I (intermediate I), and preparing ceftizoxime alapivoxil from intermediate I. The method has such advantages as abundant reagents, mild reaction conditions, high yield and no requirement for special equipment.
Bibliography:Application Number: CN2006137530