There is provided an improved and convenient process for the synthesis of aporphines, such as apomorphine and apocodeine, by the rearrangement of the corresponding morphine or codeine derivatives. The use of a suitable water scavenger in an acid catalyzed rearrangement of the morphine derivatives unexpectedly results in a reaction temperature convenient for plant operation without sacrificing product. The method of the present invention also alleviates the cumbersome operations that were employed in the prior art to eliminate water from the reaction mixture at the elevated temperatures. This process is adaptable for the general preparation of other aporphines from the corresponding morphine congeners.
提供了一种改进和便利的合成阿泼
吗啡(apomorphine)和阿泼可定(apocodeine)等阿泼啡(aporphines)的方法,该方法通过对应的
吗啡(morphine)或
可待因(codeine)衍
生物的重排来实现。在酸催化的
吗啡衍
生物重排中使用适当的
水清除剂,出乎意料地得到了适合植物操作的反应温度,而不会牺牲产品。本发明方法还减轻了在先前的技术中用于在高温下从反应混合物中消除
水的繁琐操作。该过程适用于从相应的
吗啡同系物中普遍制备其他阿泼啡的方法。