发明名称 22THIO SUBSTITUTEDD11CARBAPENAMM33CARBOXYLIC ACID DERIVATIVE AND ITS PREPARATION
摘要 NEW MATERIAL:A compound shown by the formula I (R<1> is H, 1-6C alkyl, OH, acyloxy, etc.; R<2> is 1-6C alkyl, aryl, aralkyl, etc.; R<3> is H, ester residue, salt- forming group together with carboxyl). EXAMPLE:2-(2'-Aminoethyl)mercarto-1-carbapenam-3-carboxylic acid. USE:Antibiotics and a synthetic intermediate of thienamycin dirivative useful as antibacterial agents. PROCESS:1-Carba-2-penam compound shown by the formula II is reacted with a compound shown by the formula R<2>-S-R<4> (R<4> is H or alkali metal) in an inert solvent, e.g., THF at -78-30 deg.C to give a compound shown by the fomula I. The addition of a base, e.g., triethylamine, shortens the reaction time extremely. The compound shown by the formula II usable as a starting material is obtained by reacting a compound shown by the formula III (R9 is alkyl, etc.) with a compound shown by the formula IV (X is halogen, etc.).
申请公布号 JPS5573681(A) 申请公布日期 1980.06.03
申请号 JP19780148461 申请日期 1978.11.30
申请人 SANKYO CO 发明人 HIRAOKA TETSUO;KOBAYASHI TAKEO;WATANABE TAIICHIROU;HASHIMOTO TOSHIHIKO;MIYADERA TETSUO
分类号 C07D477/00;A61K31/397;A61K31/40;A61P31/04;C07D487/04 主分类号 C07D477/00
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