发明授权
US4419284A Preparation of halomethyl esters (and related esters) of penicillanic
acid 1,1-dioxide
失效
制备青霉烷酸1,1-二氧化物的卤甲基酯(和相关酯)
- 专利标题: Preparation of halomethyl esters (and related esters) of penicillanic acid 1,1-dioxide
- 专利标题(中): 制备青霉烷酸1,1-二氧化物的卤甲基酯(和相关酯)
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申请号: US246453申请日: 1981-03-23
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公开(公告)号: US4419284A公开(公告)日: 1983-12-06
- 发明人: Thomas C. Crawford , Vytautas J. Jasys
- 申请人: Thomas C. Crawford , Vytautas J. Jasys
- 申请人地址: NY New York
- 专利权人: Pfizer Inc.
- 当前专利权人: Pfizer Inc.
- 当前专利权人地址: NY New York
- 主分类号: C07D519/06
- IPC分类号: C07D519/06 ; A61K31/43 ; A61P31/04 ; C07D499/00 ; C07D499/21 ; C07D499/32 ; C07D499/86 ; C07D499/87 ; C07D499/897 ; A61K31/425
摘要:
Process for preparation of halomethyl esters (and related esters) of penicillanic acid 1,1-dioxide of the formula ##STR1## where X is Cl, Br, I, certain alkylsulfonyloxy or arylsulfonyloxy groups, useful as intermediates in production of antibiotics having beta-lactamase activity, which comprises hydrogenolysis of an ester of the formula ##STR2## where n is zero, 1 or 2; Y and Z are each Cl, Br or I, or Y is H and Z is Cl, Br, I, C.tbd.N-- or SCN--, or Y is arylselenyl and Z is Cl or Br; and when n is zero or 1, oxidation of the hydrogenolysis product; a process for preparing compounds of formula (VI, n=2) by oxidation of the corresponding compound (VI) wherein n is zero or 1, and certain novel intermediates useful in the above processes.
公开/授权文献
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