发明名称 PENEM DERIVATIVE
摘要 NEW MATERIAL:A compound shown by the formula I [R1 is H, or (OH-substituted)1-6C alkyl; R2 is group shown by the formula II or III (Q is single bond, chain 1-6C alkylene; m is 3-6; n is 1-4; R4-R6 are H, 1-6C alkyl); R3 is H, or ester residue]. EXAMPLE:( 5R,6S,8R )-2-( 1-Carbamimidoylpyrrolidin-3-ylthio )-6-( hydroxyethyl ) penem-3-carboxylic acid. USE:An antibacterial agent. Having improved antibacterial power and stability, obtainable in high yield. PREPARATION:For example, a compound [e.g., p-nitrobenzyl(5R,6S,8R)-2-ethylsulfinyl-6-(1-hydroxyethyl)penem-3-carb oxylate, etc.] shown by the formula IV(R7 is organic group) is reacted with a compound (e.g., 3-mercapto-1-p-nitrobenzoyloxycarbamimidoylpyrrolidin, etc.) shown by the formula R8SH [R8 is (protected) R2; different from R7], and deprotected, to give a compound shown by the formula I.
申请公布号 JPS60222487(A) 申请公布日期 1985.11.07
申请号 JP19840078007 申请日期 1984.04.18
申请人 DAIICHI SEIYAKU KK 发明人 SATOU MAKOTO;TAKEMURA MAKOTO;AZUMA KUNIO
分类号 C07D499/897;A23K1/16;A61K31/425;A61K31/43;A61L2/16;A61P31/04;C07D499/00;C07D499/88 主分类号 C07D499/897
代理机构 代理人
主权项
地址