发明名称 BETA-LACTAMS
摘要 1. Claims for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE. Optically uniform beta-lactams of the general formula see diagramm : EP0101598,P12,F5 wherein R**1 signifies lower 2- or 1-alkenyl or a group of the formula -CH2 -CH(OR**4 )2 -CH2 -CHO -CO-CH(OH)2 see diagramm : EP0101598,P13,F1 R**4 signifies lower alkyl, n signifies the number 0 or 1, R**2 signifies amino, azido, phthalimido. ROCO-CH=C(CH3 )-NH- or Z-NH- ; R signifies lower alkyl, Z signifies a readily cleavable acyl group and R**6 and R**7 each signify a lower hydrocarbon residue which optionally contains oxygen and which is attached via a carbon atom, said residues being optionally joined with one another, whereby R**1 signifies lower 2- or 1-alkenyl or one of the groups (a), (c) and (d) when R**2 signifies amino and the residues denotes as lower contain up ot 8 carbon atoms, and the corresponding optical antipodes thereof. 1. Claims for the Contracting State AT A process for the manufacture of optically uniform beta-lactams of the general formula see diagramm : EP0101598,P14,F6 wherein R**1 signifies lower 2- or 1-alkenyl or a group of the formula -CH2 -CH(OR**4 )2 -CH2 -CHO -CO-CH(OH)2 see diagramm : EP0101598,P14,F2 R**4 signifies lower alkyl, n signifies the number 0 or 1, R**2 signifies amino, azido, phthalimido, ROCO-CH=C(CH3 )-NH- or Z-NH- ; R signifies lower alkyl, Z signifies a readily cleavable acyl group and R**6 and R**7 each signify a lower hydrocarbon residue which optionally contains oxygen and which is attached via a carbon atom, said residues being optionally joined with one another, whereby R**1 signifies lower 2- or 1-alkenyl or one of the groups (a), (c) and (d) when R**2 signifies amino and the residues denoted as lower contain up to 8 carbon atoms, and of the corresponding optical antipodes thereof, characterized by reacting a reactive derivative of a carboxylic acid of the general formula R**20 -CH2 -COOH wherein R**20 signifies azido, phthalimido or the group ROCO-CH=C(CH3 )-NH- and R signifies lower alkyl, in the presence of a base with a compound or the general formula see diagramm : EP0101598,P14,F3 wherein R**11 signifies lower 2-alkenyl or one of the groups (a) and (d) defined above and R**6 and R**7 have the above significance, or the corresponding optical antipode thereof to give a compound of the general formula see diagramm : EP0101598,P14,F5 wherein R**11 , R**20 , R**6 and R**7 have the above significance, or the corresponding optical antipode thereof and, if desired, converting a lower 2-alkenyl group present as R**11 into the corresponding 1-alkenyl group or converting a group (a) present as R**11 into the group (b) or (c) or converting a group (d) present as R**11 into the vinyl group, whereby previously or subsequently the group R**20 is converted, if desired, into the amino group and, if desired, this is acylated with a readily cleavable acyl group.
申请公布号 AU1797983(A) 申请公布日期 1984.02.23
申请号 AU19830017979 申请日期 1983.08.15
申请人 HOFFMANN-LA ROCHE, F. + CO. AG. 发明人 SOLANGE ADAM-MOLINA
分类号 C07D205/08;C07D205/00;C07D205/085;C07D209/00;C07D317/00;C07D403/04;C07D405/04;C07D405/14;C07D417/12 主分类号 C07D205/08
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