申请人:Beecham Group p.l.c.
公开号:US05064649A1
公开(公告)日:1991-11-12
.beta.-Lactam antibiotics of the formula (Ia) or a pharmaceutically acceptable salt or pharmaceutically acceptable in vivo hydrolysable ester thereof are disclosed: ##STR1## wherein R.sup.1 is hydrogen, methoxy or formamido; R.sup.2 is a acyl group, in particular that of an antibacterially active cephalosporin; CO.sub.2 R.sup.6 is carboxy group or a carboxylate anion; R.sup.4 is a butenolide or butanolide ring, optionally substituted by one or two alkyl, dialkylamino, alkoxy, hydroxy or aryl groups, which may be the same or different, or, wherein two adjacent carbon atoms which are available for substitution define the common bond of an aromatic fused bicyclic system; X is S, SO, SO.sub.2, O or CH.sub.2 ; and the dashed line adjacent to R.sup.4 represents an optional double bond. Processes for the preparation of compounds together with intermediates for use therein are disclosed.
公开了式(Ia)的.beta.-内酰胺类抗生素或其药学上可接受的盐或体内可水解的酯:##STR1## 其中R.sup.1是氢,甲氧基或甲酰胺基;R.sup.2是酰基,特别是一种抗菌活性头孢菌素的酰基;CO.sub.2 R.sup.6是羧基或羧酸根离子;R.sup.4是丁烯内酯或丁醇内酯环,可选地被一个或两个烷基,二烷基氨基,烷氧基,羟基或芳基取代,这些基团可以相同或不同,或者其中两个相邻的可取代碳原子定义为芳香融合双环系统的共轭键;X是S,SO,SO.sub.2,O或CH.sub.2;虚线相邻于R.sup.4表示可选的双键。公开了用于制备化合物的过程以及用于其中的中间体。