发明名称 |
O-2-Isocephem-4-carboxylic acid derivatives as antibacterial agents |
摘要 |
There is described the stereoselective total synthesis by a variety of routes of novel suitably substituted DELTA 2,3-1, 4-morpholine-2-carboxylic acids possessing a fused alpha -lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula <IMAGE> wherein Q is hydrogen, alkyl, aralkyl or -CH2COOZ where Z is hydrogen or the residue of an ester group and X is amino, azido or acylamino. Also included in the invention are compounds of the above formula in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds. Those compounds in which X is acylamino and their physiologically hydrolyzed esters and pharmaceutically acceptable salts are potent antibacterial agents.
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申请公布号 |
US4066831(A) |
申请公布日期 |
1978.01.03 |
申请号 |
US19760715942 |
申请日期 |
1976.08.19 |
申请人 |
BRISTOL-MYERS COMPANY |
发明人 |
BELLEAU, BERNARD R.;DOYLE, TERRENCE W.;LUH, BING YU;CONWAY, TERRY T. |
分类号 |
C07D205/08;A61K31/397;A61K31/535;A61P31/04;B01J23/00;B01J25/00;B01J31/00;C07B61/00;C07D205/085;C07D257/04;C07D317/30;C07D498/04;C07D505/00;C07D507/04;C07D507/06;C07D507/08;(IPC1-7):C07D265/34 |
主分类号 |
C07D205/08 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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