发明名称 PROCESS FOR THE PREPARATION OF CHIRAL B-LACTAMS
摘要 1. A process for the manufacture of chiral beta-lactams of the general formula see diagramm : EP0120289,P14,F1 wherein R**1 signifies a readily cleavable protecting group, R**2 signifies azido, phthalimido or the group ROCO-CH=C(CH3 )-NH-, R signifies lower alkyl and R**3 and R**4 each individually signify hydrogen or lower alkyl or together signify alkylene with a maximum of 6 carbon atoms, and the groups denoted by lower have a maximum of 4 carbon atoms, characterized by reacting a lactone of the general formula see diagramm : EP0120289,P14,F2 wherein R**3 and R**4 have the above significance, with an alkali metal periodate, reacting the resulting aldehyde of the general formula see diagramm : EP0120289,P14,F3 wherein R**3 and R**4 have the above significance, with an amine of the general formula H2 N-R**1 wherein R**1 has the above significance, and reacting the thus-obtained compound of the general formula see diagramm : EP0120289,P14,F4 wherein R**1, R**3 and R**4 have the above significance, in the presence of a base with a reactive derivative of a carboxylic acid of the general formula R**2-CH2 -COOH wherein R**2 has the above significance.
申请公布号 DE3471306(D1) 申请公布日期 1988.06.23
申请号 DE19843471306 申请日期 1984.02.21
申请人 F. HOFFMANN-LA ROCHE & CO. AKTIENGESELLSCHAFT 发明人 HUBSCHWERLEN, CHRISTIAN, DR.
分类号 C07D307/32;C07D307/33;C07D317/20;C07D317/26;C07D317/28;C07D405/04;C07D405/14;C07D407/04 主分类号 C07D307/32
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