发明授权
US5112967A Process for synthesizing antibacterial cephalosporin compounds
失效
用于合成抗生素CEPHOROSPORIN化合物的方法
- 专利标题: Process for synthesizing antibacterial cephalosporin compounds
- 专利标题(中): 用于合成抗生素CEPHOROSPORIN化合物的方法
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申请号: US515966申请日: 1990-04-27
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公开(公告)号: US5112967A公开(公告)日: 1992-05-12
- 发明人: Dennis D. Keith , Chung-Chen Wei , Kevin F. West
- 申请人: Dennis D. Keith , Chung-Chen Wei , Kevin F. West
- 申请人地址: NJ Nutley
- 专利权人: Hoffmann-La Roches Inc.
- 当前专利权人: Hoffmann-La Roches Inc.
- 当前专利权人地址: NJ Nutley
- 主分类号: C07D501/18
- IPC分类号: C07D501/18 ; A61K31/545 ; A61K31/546 ; A61P31/04 ; C07D501/00 ; C07D501/04 ; C07D501/26 ; C07D501/34
摘要:
A process for synthesizing 3-acryloxymethyl antibacterialcephalosporin compounds of formula ##STR1## wherein R is hydrogen or a carboxylic acid protecting group; R.sup.1 is hydrogen or an acyl group; R.sup.2 is hydrogen or lower alkoxy; and R.sup.3 is carbocyclic aryl substituted on the ring with one or more members selected from the group consisting of hydroxy, lower alkyl, amino, cyano, lower alkoxy, halogen and alkylcarboxy,as well as the corresponding readily hydrolyzable esters, pharmaceutically acceptable salts and hydrates of these compounds where R is hydrogen, in which a 2-carboxylic acid 3-hydroxymethyl cephalosporin compound is first treated with an organic base to form an organic salt therewith, followed by acylation of the 3-hydroxymethyl substituent.
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