| 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, cyano, -COOR<5> (R<5> is H or carboxyl-protecting group) or group of formula II (R<6> and R<7> are H or lower alkyl); R<4> is H or carboxyl- protecting group]. EXAMPLE:2-(2-Tritylaminothiazol-4-yl)-3-tert-butoxycarbonyl-acrylic acid allyl ester. USE:A modifying agent for antibiotic substance, especially penicillin-type antibiotics and cephalosporin-type antibiotics. It has broad antibacterial spectrum, and exhibits strong antibacterial activity even to the Gram-negative bacteria and Gram-positive bacteria. PREPARATION:The compound of formula I can be prepared, e.g. by reacting the compound of formula III with the phosphorane compound of formula IV in a solvent at a temperature between 0 deg.C and the boiling point of the solvent for 30min-10hr.</p> |
