Process for the preparation of beta-lactam derivatives, the novel derivatives so obtainable and pharmaceutical compositions containing them
申请人:Technobiotic Ltd.
公开号:EP0005889A1
公开(公告)日:1979-12-12
The invention relates to a process for the preparation of β-lactam derivatives having a substituted hydroxymethyl group at the carbon atom a to the lactam carbonyl group, to the novel antibacterially-active derivatives so-obtainable and to pharmaceutical compositions containing these.
The process comprises reacting under specified conditions an α-halo-β-lactam starting material with activated zinc in the presence of an appropriate aldehyde or ketone and hydrolysing the resulting zinc complex.
The novel β-lactam derivatives are of the general formula I
(with the meaning of R, R1-R4, Y and Z as given in the specification) and include the pharmaceutically acceptable salts thereof.
本发明涉及一种β-内酰胺衍生物的制备工艺,该衍生物在与内酰胺羰基相连的碳原子上具有被取代的羟甲基;本发明还涉及可获得的新型抗菌活性衍生物以及含有这些衍生物的药物组合物。
该工艺包括在特定条件下,在适当的醛或酮存在下,使 α-卤代-β-内酰胺起始原料与活性锌反应,并水解生成的锌络合物。
新型 β-内酰胺衍生物的通式为 I
(R、R1-R4、Y 和 Z 的含义见说明书),并包括其药学上可接受的盐。
US4272439A
申请人:——
公开号:US4272439A
公开(公告)日:1981-06-09
US4283531A
申请人:——
公开号:US4283531A
公开(公告)日:1981-08-11
Bernasconi, C.; Cottier, L.; Descotes, G., Journal of Heterocyclic Chemistry, 1980, vol. 17, p. 45 - 48