申请人:Fujisawa Pharmaceutical Co., Ltd.
公开号:US03993646A1
公开(公告)日:1976-11-23
A process for producing a 2-cephem or 3-cephem derivative compound of the formula: ##SPC1## Wherein R.sub.1 represents a substituted or unsubstituted amino radical and R.sub.4 represents hydrogen or a radical selected from the group consisting of carboxy, protected carboxy, ester, acid amide, acid anhydride, acid halide, acid azide and carboxy salt, and the dotted line indicates the alternate bond structure providing 3-cephem or 2-cephem, which comprises: Reacting a halogenated derivative selected from the group consisting of a halogenated penam derivative having the formula: ##SPC2## A halogenated cepham derivative of the formula: ##SPC3## Wherein X represents a halogen atom, R.sub.3 represents a radical selected from the group consisting of carboxy, protected carboxy, ester, acid amide, acid anhydride, acid halide, acid azide and carboxy salt, and R.sub.1 is as defined above, or mixtures thereof with a dehydrohalogenoic acid reagent.
一种用于生产式I所示的2-头孢烯或3-头孢烯衍生物化合物的方法:
##SPC1##
其中R1表示取代或未取代的氨基基团,R4表示氢或选自羧基、保护的羧基、酯、酰胺、酸酐、酸卤化物、酸叠氮化物和羧酸盐的基团,虚线表示提供3-头孢烯或2-头孢烯的交替键结构,该方法包括:
使选自以下组的卤化衍生物与脱卤化氢酸试剂反应:
具有式II的卤化青霉烷衍生物:
##SPC2##
具有式III的卤化头霉烷衍生物:
##SPC3##
其中X表示卤素原子,R3表示选自羧基、保护的羧基、酯、酰胺、酸酐、酸卤化物、酸叠氮化物和羧酸盐的基团,R1如上定义,或它们的混合物。