发明名称 2-(2-CYCLOPROPYLPYRROLIDIN-4-YLTHIO)CARBAPENEM DERIVATIVE
摘要 <p>NEW MATERIAL:The compound of formula I (R<1> is H or methyl; R<2> and R<3> are H, lower alkyl or together with adjacent N form aziridinyl, azetidinyl, pyrrolidinyl, piperidino, piperazinyl or morpholino; A is carbonyl or single bond; n is 0-3), its salt or ester. EXAMPLE:(5R,6S)-2[(2S,4S)-2-[2-(N, N-dimethylaminocarbonyl)- cyclopropyl]pyrrolidin-4-ylthio]-6-[(R)-1-hydroxyethyl]-1-carbapen-2-e m-3- carboxylic acid. USE:An antibacterial agent. It has strong antibacterial action against sensitive and resistant Gram-positive bacteria and Gram-negative bacteria and excellent stability to beta-lactamase and DHP-1. PREPARATION:The objective compound of formula I can be produced by reacting a compound of formula II (R<4> is H or COOH-protecting group; R<5> is H or OH-protecting group) with a compound of formula III (R<20> and R<30> are R<2>, R<3> or amino- or imino-protecting group) and, as necessary, deprotecting the reaction product.</p>
申请公布号 JPH04134082(A) 申请公布日期 1992.05.07
申请号 JP19900414636 申请日期 1990.12.27
申请人 BANYU PHARMACEUT CO LTD 发明人 NAKAGAWA SUSUMU;YAMADA KOJI;USHIJIMA RYOSUKE
分类号 C07D477/00;A61K31/397;A61K31/40;A61P31/04;C07D207/12 主分类号 C07D477/00
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