一种适合工业化生产的溴甲纳曲酮的制备方法

A Synthetic Process of Methylnaltrexone Bromide for Industrial Production

以盐酸纳曲酮为原料,先用乙酸酐保护其酚羟基,再和溴甲烷进行N-甲基化反应,所得反应物再用氢溴酸水解得到溴甲纳曲酮,总收率35%,HPLC纯度大于99.9%,该制备方法操作简单,适合工业化生产。

Methylnaltrexone bromide was synthesized by using naltrexone hydrochloride as starting materials, etherification with acetic anhydride and methylation with methyl iodide, which was subjected to hydrolysis with hydrobromic acid. The overall yield was about 35 % and HPLC purity was more than 99.9 %. The process is simple and suitable for industrial production.