| 摘要 |
<p>NEW MATERIAL:The compound of formula I (R<1> is H or amino-protecting group; R<2> and R<3> are H or carboxyl-protecting group; R<4> is H, 1-4C alkyl, allyl, etc.) and its salt. EXAMPLE:7beta-{alpha-( 2-aminothiazol-4-yl )-alpha-[(Z)-carboxymethoximino]-acetamido}- 3-[(Z)-2-methoxycarbonylvinylthio]-3-cephem-4-carboxylic acid sodium salt. USE:An antibacterial agent for oral administration. It keeps high concentration in blood. It has strong antibacterial activity and broad antibacterial spectrum. PREPARATION:The starting compound of formula II (R<5> is amino-protecting group; Y is halogen, etc.) is made to react with NaSH in a solvent such as THF in the presence of a base to obtain a 3-thio-substituted compound of formula III. The protecting group R<4> removed from the produced compound and the product is made to react with the compound of formula IV in the presence of a condensation agent. The resultant compound of formula V is subjected to deprotection with trifluoroacetic acid-anisole, etc.</p> |
