| 发明名称 |
PROCESS FOR PREPARING 1-OXIDE OF 7BETA-PHENOXY-ACETAMIDO-3-METHYL-3-CEPHEM-4-CARBOXYLIC ACID -METHOXYMETHYL-ESTER |
| 摘要 |
1409992 Process for preparing cephalexin; penam- and cephem-derived methoxymethyl esters BRISTOL-MYERS CO 7 Feb 1974 [8 Feb 1973] 05682/74 Heading C2C A process for preparing cephalexin comprises (a) reacting methoxymethyl 3-methyl-7-#-phenoxy acetamidoceph-3-em-4-carboxylate (I) with a halogenating agent (e.g. PCl 5 ) and acid acceptor in an inert, water-immiscible solvent at - 10‹ to - 60‹ C.; (b) reacting the I-imidochloride with a (<C 7 ) aliphatic alcohol at -20‹ to - 70‹ C.; (c) reacting the I-imido/alkyl ether with D-(-)-PhCH(NH 2 ,HCl)COCl at below - 30‹ C.; (d) hydrolysing the thus-formed complex; and (c) basifying the cephalexin-hydrochloride obtained. (I) is prepared by reacting penicillin-V sulphoxide with ClCH 2 OMe and acid acceptor to give methoxymethyl 6-phenoxyacetamidopenicillanate sulphoxide (II) and subjecting the latter to conventional ring expansion. The invention comprises also, (I) and (II), per se. Therapeutic compositions comprise cephaloxin prepared by the above process, and an inert pharmaceutically acceptable carrier. |
| 申请公布号 |
HU173425(B) |
申请公布日期 |
1979.05.28 |
| 申请号 |
HU1974BI00517 |
申请日期 |
1974.02.07 |
| 申请人 |
BRISTOL-MYERS CO,US |
发明人 |
SAPINO,CHESTER JUN,US;RUGGERI,MARIANO V.,US |
| 分类号 |
C07D499/32;C07D499/00;C07D499/08;C07D499/60;C07D501/10;C07D501/22 |
主分类号 |
C07D499/32 |
| 代理机构 |
|
代理人 |
|
| 主权项 |
|
| 地址 |
|
