| 摘要 |
NEW MATERIAL:A compound (salt) shown by the formula I [R1 is H, or hydroxy lower alkyl; R2 is carbamimidoyl lower alkyl, guanidino lower alkyl, or group shown by the formula II (Q1 is lower alkylene; Q2 is lower alkylene, or NH); R3 is H, or ester residue]. EXAMPLE:p-Nitrobenzyl( 5R,6S,8R )-2-ethylsulfinyl-6-( 1-hydroxyethyl)penem-3-carboxylate. USE:An antibacterial agent against Gram-positive bacteria and Gram-negative bacteria including Pseudomonas aeruginosa. PREPARATION:For example, a penem derivative shown by the formula III (R4 is alkyl, aryl, or aralkyl) shown by the formula III is oxidized with an oxidizing agent in a solvent to give a sulfoxide derivative shown by the formula IV, which is reacted with a thiol compound shown by the formula R2-SH, and the protecting group is eliminated, to give a compound shown by formula I . |
