发明名称 OPTICALLY ACTIVE 3-AZIDO-AZETIDIN-2-ON-1-YLACETIC ACID DERIVATIVE
摘要 NEW MATERIAL:A compound shown by the formula I [X is OH, halogen, alkylsulfonyloxy, etc.; Y is O or NH; R<1> is H, 1-6C alkyl, phenyl, trityl, nitrobenzyl, etc.; R<2> is (esterified or amidated)carboxyl or its salt, 1-10C alkyl, cycloalkyl, phenyl, etc.]. EXAMPLE:(3S,4S)-3-Azido-1-[(R,S)-2,2-diethoxy-1-p-nitrobenzyl-carbamoy lethyl]-4- hydroxymethyl-acetidin-2-one. USE:An intermediate for synthesizing a beta-lactam compound showing antibacterial activity. PREPARATION:A compound shown by the formula II is reacted with an aromatic sulfonylazide to give a compound shown by the formula III, the N- protecting group of the compound is eliminated under acidic condition to give a compound shown by the formula IV, which is reacted with an equimolar mixture of an aldehyde shown by the formula R<1>-CHO and an isonitrile shown by the formula R<2>-NC, to give a compound shown by the formula I wherein X is OH and Y is NH.
申请公布号 JPS6168465(A) 申请公布日期 1986.04.08
申请号 JP19840190059 申请日期 1984.09.10
申请人 HATANAKA MINORU 发明人 HATANAKA MINORU;NITTA TAKESHI;ISHIMARU HISAYASU
分类号 C07D205/08;C07D205/00;C07D205/085;C07D303/00;C07D309/00;C07D405/06;C07D405/12;C07D498/04;C07D507/04;C07D507/06;C07D507/08;C07D513/04 主分类号 C07D205/08
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