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。