申请人:GERDES Klaus
公开号:US20090326219A1
公开(公告)日:2009-12-31
A process for the production of extremely pure galanthamine or extremely pure galanthamine derivatives, a start is made from racemic bromine narwedine, which is debrominated under palladium catalysis. In this case, the working-up of the reaction mixture, which is carried out in the presence of oxygen or peroxides so that the palladium catalyst in an insoluble form is converted into an easily separable form, is essential. The further reaction is carried out by reduction of enantiomer-pure narwedine to form enantiomer-pure galanthamine, whereby it is then alkylated or dealkylated so that a corresponding substitution on the ring-nitrogen atom is achieved. By further purification, such as recrystallization, residual portions of palladium of below 5 ppm are achieved, so that direct use as a pharmaceutical raw material is made possible.
一种生产极纯的风信子碱或其衍生物的方法,首先从外消旋溴化纳尔维丁开始,通过钯催化去溴化。在这种情况下,反应混合物的处理必须在氧气或过氧化物的存在下进行,以便将钯催化剂转化为易于分离的不溶形式。进一步的反应是将对映纯的纳尔维丁还原成对映纯的风信子碱,然后通过烷基化或去烷基化使环氮原子上发生相应的取代。通过进一步的纯化,如重结晶,可以实现钯的残留量低于5 ppm,从而使其可以直接用作药用原料。