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

申请人： BIOCHEMIE Gesellschaft m.b.H.

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。