发明名称 |
Process for the rearrangement of penicillins to cephalosporins and intermediate compounds thereof |
摘要 |
Penicillin sulfoxides are converted to 3-halo-3-methyl-cepham-4-carboxylic acid esters and amides or the corresponding cephem derivatives by heating the penicillin sulfoxide precursor in a polyhaloalkane solvent to a temperature between 50 DEG to about 150 DEG C. in the presence of an equimolar amount of a neutral or basic catalyst, respectively. The catalysts employed are bases such as pyridine, picoline, lutidine, quinoline, isoquinoline, dimethylaniline or a quaternary ammonium salt. The 3-halo-cepham intermediates produced with a quaternary ammonium catalyst are dehydrohalogenated to afford known cephem derivatives or converted to the free 4-carboxylic acid and the alkali metal, alkaline earth metal or ammonium salts thereof to afford novel antibacterial agents.
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申请公布号 |
US4010156(A) |
申请公布日期 |
1977.03.01 |
申请号 |
US19750602623 |
申请日期 |
1975.08.07 |
申请人 |
AMERICAN HOME PRODUCTS CORPORATION |
发明人 |
NUDELMAN, ABRAHAM;MCCAULLY, RONALD J. |
分类号 |
C07D213/20;C07D215/10;C07D501/10;(IPC1-7):C07D501/10 |
主分类号 |
C07D213/20 |
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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