发明名称 |
METHOD OF PRODUCING 3-HYDROXY-3-METHYL-7-AMINOCEFAM COMPOUNDS |
摘要 |
<p>1289392 3 - Hydroxy - 3 - methyl - 7 - aminocepham - 4 - carboxyl derivatives ; cephalo- Sporins ELI LILLY & CO 4 Dec 1970 [24 Feb 1970 (2)] 57731/70 Heading C2A Novel 3 - hydroxy - 3 - methyl - 7 - aminocepham - 4 - carboxyl compounds of general formula wherein R is H, H 2 #, or an amino-protecting group and R<SP>1</SP> is H, an ester group, a salt-forming cation or an anionic charge when R is H 2 #, are prepared by heating a penicillin sulphoxide acid or ester in the presence of sulphuric acid, sulphamic acid, or a soluble salt or ester thereof to about 80‹ C. to about 150‹ C. in a reaction mixture containing at least about 10% by volume of a tertiary carboxamide to yield the acid or ester product, which may then be converted to the desired salts or zwitterions. Known #<SP>3</SP>-cephem-cephalosporins can be prepared from the novel compounds, e.g. 3-methyl- 7 - (2<SP>1</SP> - phenoxy - acetamido) - 3 - cephem - 4- carboxylate is prepared by treating 4<SP>11</SP>-nitrobenzyl 3 - hydroxy - 3 - methyl - 7 - (2<SP>1</SP>- phenoxy - acetamido) - cepham - 4 - carboxylate with acetic anhydride and N,N-dimethylacetamide to yield 4<SP>11</SP>-nitrobenzyl-3-methyl-7-(2<SP>1</SP>- phenoxy - acetamido) - 3 - cephem - 4 - carboxylate and removing the ester group by known hydrogenation methods.</p> |
申请公布号 |
CS193010(B2) |
申请公布日期 |
1979.09.17 |
申请号 |
CS19700008263 |
申请日期 |
1970.12.08 |
申请人 |
GUTOWSKI,GERALD E.,US;FOSTER,BENNIE J.,US;HATFIELD,LOWELL DE LOSS,US |
发明人 |
GUTOWSKI,GERALD E.,US;FOSTER,BENNIE J.,US;HATFIELD,LOWELL DE LOSS,US |
分类号 |
A61K;A61K31/545;B01J21/00;B01J31/00;C07B61/00;C07D;C07D501/00;C07D501/10;C07D501/14;C07D501/24;(IPC1-7):C07D501/10 |
主分类号 |
A61K |
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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