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溴甲纳曲酮的合成

Synthesis of Methylnaltrexone Bromide
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摘要 盐酸纳曲酮与乙二醇缩合、叔丁基二甲基氯硅烷保护,再与碘甲烷进行N-甲基化反应得(R)-3-[(叔丁基二甲基硅基)氧基]-17-环丙甲基-4,5a-环氧-14-羟基-6-(1,3-二氧戊烷-2-基)-N-甲基吗啡喃碘化物,再经氢溴酸水解、溴离子交换得溴甲纳曲酮,总收率53%,HPL,C纯度大于99%。 Methylnaltrexone bromide was synthesized from naltrexone hydrochloride via condensation with ethylene glycol, etherification with t-butyldimethylchlorosilane and methylation with methyl iodide to give (R)-3-[ (t- butyldimethylsilyl) oxy] - 17-cyclopropylmethyl-4,5 a-epoxy- 14-hydroxy-6- (1,3-dioxolane-2-yl) -N-methylmorphinanium iodide, which was subjected to hydrolysis with hydrobromic acid, ion exchange with bromide anion exchange resin. The overall yield was about 53 % and HPLC purity was more than 99%.
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2015年第1期4-6,共3页 Chinese Journal of Pharmaceuticals
基金 国家十一五"重大新药创制"科技重大专项(2010ZX09401-306-2-14)
关键词 溴甲纳曲酮 便秘 合成 methylnaltrexone bromide constipation synthesis
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