发明名称 |
{66 {HU 2,3{B -1,4 Morpholine-2-carboxylic acid derivatives as antibacterial agents |
摘要 |
There is described the stereoselective total synthesis of novel DELTA 2,3-1,4-morpholine-2-carboxylic acids possessing a fused beta -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> I wherein Z is halo, hydroxyl, etherified hydroxyl or hydroxyl esterified with a carboxylic acid residue or a sulfonic acid residue and X is amino, azido or acylamino. Also included in the invention are compounds of formula I 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 of formula I. The compounds of formula I are potent antibacterial agents or are of use as intermediates in the preparation of such antibacterial agents.
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申请公布号 |
US4112230(A) |
申请公布日期 |
1978.09.05 |
申请号 |
US19770759710 |
申请日期 |
1977.01.17 |
申请人 |
BRISTOL-MYERS COMPANY |
发明人 |
MENARD, MARCEL;LIM, GARY M. F.;CONWAY, TERRY T. |
分类号 |
C07D507/04;A61K31/535;A61P31/04;C07C59/66;C07D205/085;C07D309/12;C07D317/28;C07D498/04;C07D498/14;C07D507/06;C07D507/08;(IPC1-7):C07D265/36;C07D498/02;A01N9/00;A01N9/22 |
主分类号 |
C07D507/04 |
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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