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公开(公告)号：EP0973779B1
公开(公告)日：2003-07-02
申请号：EP98921425.9
申请日：1998-04-02
IPC分类号： C07D501/22
CPC分类号： C07D501/00
摘要： Cefdinir in the form of a salt with dicyclohexylamine, a process for its production and its use in the purification of impure cefdinir.
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公开(公告)号：EP0757691B1
公开(公告)日：2003-07-02
申请号：EP95917948.2
申请日：1995-04-24
IPC分类号： C07D501/18 , C07D501/62
CPC分类号： C07K5/06139 , C07D501/00 , Y02P20/55
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公开(公告)号：EP1173444A1
公开(公告)日：2002-01-23
申请号：EP00943708.8
申请日：2000-05-03
IPC分类号： C07D501/04 , C07D501/12 , C07D501/34
CPC分类号： C07D501/00
摘要： The novel intermediate compound crystalline 7-[2-(2-fomylaminothiazol-4-yl)-2 -(Z)-(methoxyimino)acetamido]-3-methoxymethyl-3-cephem-4-carboxylic acid-1 -(isopropoxy/crystallization of cefpodoxime proxetil. The crystallization process comprises dissolving or suspending the intermediate in the presence of a nitrile or a ketone or mixtures thereof; at a ratio of 1 gm of the intermediate to 2-15 ml nitrile; or at a ratio of 1 gm of the intermediate to 3-15 ml ketone; in the presence of 5-80 ml water; and thereafter isolating the intermediate in crystalline form and converting the intermediate by splitting off the formyl group from the amino group attached to the thiazolyl group, to obtain the desired product cefpodoxime proxetil, in the form of a diastereoisomeric mixture in a ratio of B/(A+B) of 0.5 to 0.6.
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公开(公告)号：EP1133298A1
公开(公告)日：2001-09-19
申请号：EP99959327.0
申请日：1999-11-24
IPC分类号： A61K31/546 , A61K9/14 , A61K9/20 , A61K9/36 , A61P31/04
CPC分类号： A61K9/143 , A61K9/146 , A61K9/2009 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K31/545
摘要： Cefuroxime axetil in a non-gelatinous form on contact with an aqueous liquid, e.g. in the form of a solid solution in a polymer or in the form of a solid dispersion on a carrier, e.g. useful for the production of pharmaceutical compositions comprising cefuroxime axetil as an active ingredient and the use of cefuroxime axetil in the manufacture of an oral dosage form which does not exhibit an adverse food effect.
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5.发明公开
公开(公告)号：EP0976755A1
公开(公告)日：2000-02-02
申请号：EP99120572.5
申请日：1991-01-21
发明人： Diago, José , Ludescher, Johannes
IPC分类号： C07D499/12 , C07D501/06
CPC分类号： C07D501/00 , C07D499/00
摘要： A process for the production of an 6-alpha-aminoacyl-penicillin or 7-alpha-aminoacyl-desacetoxy-cephalosporin comprising the steps
(i) producing a mixed carboxylic acid anhydride by reaction of an N-substituted vinyl alpha-amino acid with an appropriate acylating agent in a methyl-(C 2-4 )alkyl ketone, di-(C 2-4 )alkyl ketone, (C 1-3 ) alkanoic acid butyl ester or an aromatic hydrocarbon as a solvent,
(ii) reacting the mixed carboxylic acid anhydride obtained in step (i) with a solution or a suspension of 6-APA or derivative thereof in non-halogenated solvent, and
(iii) isolating a 6-alpha-aminoacyl-penicillin or a 7-alpha-aminoacyl-desacetoxycephalosporin obtained by adding water to the reaction mixture obtained in step (ii) to form a two-phase system and isolating a 6-alpha-aminacyl penicillin or 7-alpha-aminoacyl-desacetoxy-cephalosporin obtained by separating the aqueous phase from the organic phase.摘要翻译： 制备6-α-氨基酰基 - 青霉素或7-α-氨酰基 - 脱乙酰氧基 - 头孢菌素的方法，包括以下步骤：（i）通过N-取代的乙烯基α-氨基酸与 甲基 - （C2-4）烷基酮，二（C2-4）烷基酮，（C1-3）链烷酸丁酯或芳烃作为溶剂的合适的酰化剂，（ii）使混合的羧酸 步骤（i）中获得的酐与6-APA或其衍生物在非卤化溶剂中的溶液或悬浮液，和（iii）分离得到的6-α-氨基酰基青霉素或7-α-氨基酰基 - 脱乙酰氧基头孢菌素 向步骤（ii）中获得的反应混合物中加入水以形成两相体系并分离通过从有机相中分离水相而获得的6-α-氨基酰基青霉素或7-α-氨基酰基 - 脱乙酰氧基 - 头孢菌素。
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公开(公告)号：EP0908461A1
公开(公告)日：1999-04-14
申请号：EP98124140.9
申请日：1994-10-21
发明人： Danklmaier, Johann
IPC分类号： C07D501/04 , C07D501/18
CPC分类号： C07D501/00
摘要： A process for etherifying the hydroxymethyl group in position 3 of a cephalosporin by reaction of a 3-hydroxymethyl cephalosporin with an dioxycarbenium-tetrafluoroborate.
摘要翻译： 通过使3-羟甲基头孢菌素与四氟硼酸二氧碳鎓反应来醚化头孢菌素3位羟甲基的方法。
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公开(公告)号：EP0799232A1
公开(公告)日：1997-10-08
申请号：EP95942724.0
申请日：1995-12-22
CPC分类号： C07D501/00
摘要： A process for the production of cefotaxime in acetone/water and its use in the production of a sodium salt of cefotaxime and a crystalline sodium salt of cefotaxime in form of rounded agglomerates and in form of needles.
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公开(公告)号：EP0658558A1
公开(公告)日：1995-06-21
申请号：EP94118048.1
申请日：1994-11-15
IPC分类号： C07D501/24 , A61K31/545
CPC分类号： C07D501/00
摘要： Process of depleting 7-amino-3-[(E)-2-(4-methyl-5-thiazolyl)vinyl]-3-cephem-4-carboxylic acid in Z/E mixtures of 7-amino-3-[2-(4-methyl-5-thiazolyl)vinyl]-3-cephem-4-carboxylic acid
a) by subjecting an amine salt of a Z/E mixture of 7-amino-3-[2-(4-methyl-5-thiazolyl)vinyl]-3-cephem-4-carboxylic acid to crystallization and converting this amine salt into 7-amino-3-[2-(4-methyl-5-thiazolyl)vinyl]-3-cephem-4-carboxylic acid, or
b) by subjecting the Z/E mixture to chromatography.摘要翻译： 将7-氨基-3- [2-（4-甲基-5-噻唑基）乙烯基] -3-头孢烯-4-羧酸在7-氨基-3- [2 - （4-甲基-5-噻唑基）乙烯基] -3-头孢烯-4-羧酸a）通过将7-氨基-3- [2-（4-甲基-5 - - 噻唑基）乙烯基] -3-头孢烯-4-羧酸结晶并将该胺盐转化为7-氨基-3- [2-（4-甲基-5-噻唑基）乙烯基] -3-头孢烯-4-羧酸 酸，或b）通过使Z / E混合物进行色谱分离。 ZO
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公开(公告)号：EP0612750A2
公开(公告)日：1994-08-31
申请号：EP94105662.4
申请日：1985-11-21
IPC分类号： C07D501/18 , C07F7/18 , C07D501/06
CPC分类号： C07D501/04 , C07D501/00 , C07D501/02 , C07D501/18 , C07F7/18
摘要： 7-Trimethylamino-3-jodomethylcephem(3)-4-carbonsäuretrimethylsilylester, dessen Verwendung als Zwischenprodukt zur Herstellung von Cephalosporinderivaten und ein Verfahren zur Herstellung von Cephalosporinderivaten unter Verwendung dieses Zwischenproduktes.
摘要翻译： 7-三甲基-3- jodomethylcephem（3）-4-carbonsäuretrimethylsilylester，其作为中间体使用为头孢菌素衍生物的制备方法以及使用该中间体的头孢菌素衍生物的制备方法。
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10.发明授权Cephalosporinzwischenprodukte, Verfahren zu ihrer Herstellung und ihre Verwendung 失效Cephalosporinzwischenprodukte，其制备方法及其用途。
公开(公告)号：EP0312844B1
公开(公告)日：1994-06-22
申请号：EP88116570.8
申请日：1985-04-04
发明人： Ascher, Gerd , Sturm, Herbert , Thaler, Heinrich , Veit, Werner
IPC分类号： C07D417/12
CPC分类号： C07D277/587 , C07D277/74 , C07D501/00 , Y02P20/55
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