发明授权
- 专利标题: Selective stereospecific biologically active beta-lactams
- 专利标题(中): 选择性立体定向生物活性β-内酰胺
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申请号: US382531申请日: 1989-07-19
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公开(公告)号: US5006661A公开(公告)日: 1991-04-09
- 发明人: Richard A. Day , John Wallace
- 申请人: Richard A. Day , John Wallace
- 申请人地址: OH Cincinnati
- 专利权人: University of Cincinnati
- 当前专利权人: University of Cincinnati
- 当前专利权人地址: OH Cincinnati
- 主分类号: C07D263/44
- IPC分类号: C07D263/44 ; C07D499/00
摘要:
The present invention relates to a method for producing novel 4-[1-oxoalkyl]-2,5-oxazolidinediones, (4-1 OOD), and their use in a stereoselective method of producing beta-lactam-containing compounds which include several biologically active compounds such as the well-known families of pencillin and cephalosporin antibiotics. The method of the present invention involves generally the reaction of the above-described 4-[1-oxoalkyl]-2,5-oxazolidinediones so produced with a thiol amine having a geometry amenable to forming the precursor of the desired beta-lactam-containing compound or, in one scheme, forming the beta-lactam-containing compound itelf directly. This is done either by direct reaction of the 4-1 ODD with a thiol amine (which by one pathway proceeds directly to the beta-lactam-containing compound) or by first converting the 4-1 OOD to its 2-[1-oxoalkyl]-2-amino acid form before its reaction with the thiol amine; and then forming the beta lactam by action of cyanogen). The beta-lactam-containing compounds can be further modified according to methods known in the art to produce specific derivatives as desired.
公开/授权文献
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