| 摘要 |
<p>NEW MATERIAL:A compound shown by formula I (Y is CH or N; R1 is H or amino-protecting group; R2 is halogen, cyano, etc.; R3 is phthalidyloxy, carboxylate, etc.; R4 is H, carboxyl which may be protected, etc.; Z is CH2, C=O, etc.; n1 and n2 are 0-3) and a salt thereof. EXAMPLE:7beta-[2-(2-Aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-(2-p yrrolidon-3- yl)thio-3-cephem-4-carboxylate hydrochloride. USE:An antibacterial agent showing excellent antibacterial activity against Gram- positive bacteria and Pseudomonas aeruginosa. PREPARATION:First, a compound shown by formula II (R31 is protected COOH; w1 is methanesulfonyl, etc.) is condensed with a compound shown by formula III (R11 is amino-protecting group; R21 is cyano) and a reaction product is sulfoxidated to give a compound shown by formula IV. Then this compound is reacted with a compound shown by formula V (R41 is H, etc.; R51 is lower alkyl, etc.; X1 is SH) and a formed compound shown by formula VI is deprotected.</p> |
