溴甲纳曲酮的合成

Synthesis of Methylnaltrexone Bromide

溴甲纳曲酮可经过两步化学反应而获得,以盐酸纳曲酮为起始原料,经过氨水游离成游离纳曲酮碱,再与溴甲烷反应制备季N-烷基吗啡喃生物碱盐的粗品,粗品经过特殊精制手段达到除去常规精制方法难以除去的杂质,两个反应操作均较简易,本文献的特色点是反应路线比较简单,合成制备季N-烷基吗啡喃生物碱盐方法新颖,避开专利中的常规制备方法。除此之外,通过该粗品精致方案,能获得更少杂质的主产品,解决杂质限度难以低于千分之一的难题。

The methylnaltrexone bromide can be gotten from a two step chemical reaction naltrexone hydrochloride as the starting material was disposed to ammonia water to produced naltrexone,followed by reaction with methyl bromide to prepare quaternary N-alkyl morphine nan alkaloid salt＇s crude products.Special refining methods were applied to remove impurities in crude products which conventional methods can not be completed.Novel and simple are the most important characteristics of the reaction route to synthesis quaternary N-alkyl morphinenan alkaloid salt.The two steps are easy to operation and by which the conventional preparation methods in patent can be avoided.In addition,by the special refining methods products with less impurities can be obtained so that the difficulty which limit of impurities less than one thousandth is solved.