发明名称 CARBAPENEM ESTER DERIVATIVE
摘要 PROBLEM TO BE SOLVED: To obtain a new carbapenem ester derivative exhibiting pharmacokinetics with excellent absorbing property and persistency when administered to organisms and useful as an active ingredient for medicines for treating bacterial infectious diseases due to various kinds of pathogenic bacteria by modifying hydroxyl group of hydroxyethyl group at a specific position of carbapenem skeleton with a group hydrolyzed in vivo. SOLUTION: This compound is represented by formula I [R1 is a group of formula II to formula IV (R4 and R5 are each H, a 1-4C alkyl or the like) or the like, R2 is H, a 1-10C alkoxycarbonyloxy-1-4C alkyl or the like; R3 is a 1-20C alkanoyl or the like], e.g. pivaloyloxymethyl 6-(1-acetoxyethyl)-1- methyl-2-(2-oxo-4-pyrrolidinylthio)-1-carbapen-2-em-3-carboxylate. The compound of formula I is obtained by reacting a compound of formula V with a reactive derivative of R3 (e.g. an alkoxycarbonyl halide) in a solvent (e.g. xylene) in the presence of a base (e.g. pyridine), preferably at -10 to 50 deg.C for 10 min to 10 hr.
申请公布号 JP2000239275(A) 申请公布日期 2000.09.05
申请号 JP19990365787 申请日期 1999.12.24
申请人 SANKYO CO LTD 发明人 KAWAMOTO ISAO;SHIMOJI YASUO;SUGANO OSAMU;NAKAGAWA AKIHIKO;TERAO TOSHIO
分类号 C07D477/00;A61K31/397;A61K31/407;A61K31/4188;A61K31/427;A61P31/04;C07D519/00;(IPC1-7):C07D477/00;A61K31/418 主分类号 C07D477/00
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