| 摘要 |
PURPOSE: Provided is a method for synthesizing 3-substituted vinyl cephalosporin derivatives showing the improved antimicrobial activity for beta-lactam tolerant microorganisms. CONSTITUTION: The 3-substituted vinyl cephalosporin derivatives are represented by formula (I), in which R is aminothiazol, aminothiodiazol, alkylophenylthio, or piperidyldithiocarbonyl; R1 is hydrogen, Na, K, para-methoxybenzyl; and R2 is phenyl, methylthiobenzyl, 3,5-dibromo-2-hydroxy. The 3-substituted vinyl cephalosporin derivatives of formula (I) are produced by the steps of: reacting aldehyde compounds of formula (III) with phosphonium salts of formula (II) to produce 3-cephem compounds of formula (IV); deacylation reacting the compound of formula (IV) to produce 7-amino-3-cephem derivatives of formula (V); and acylation reacting the compounds of formula (VI) with the compounds of formula (V) to produce the title compounds of formula (I).
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