摘要
为了有效控制盐酸纳曲酮的质量,该研究合成了 7个有关物质:17-(1-丁烯基)-4,5-环氧-3,14-二羟基吗啡烷-6-酮(有关物质C)、双纳曲酮(有关物质D)、3-环丙甲氧基-17-(环丙甲基)-4,5-环氧-14-羟基吗啡烷-6-酮(有关物质E)、17-正丁基-4,5-环氧-3,14-二羟基吗啡烷-6-酮(有关物质H)、17-(环丙甲基)-3-甲氧基-4,5-环氧-14-羟基吗啡烷-6-酮(有关物质J)、17-(环丙甲基)-4,5-环氧-3,14-二羟基吗啡-7-烯-6-酮(有关物质K)、纳曲酮氮氧化物(有关物质L).其中,有关物质K、L未收录进《欧洲药典》10.0中,有关物质C、D、H的合成路线未见文献报道.上述有关物质结构均经 MS、1HNMR、13C NMR确证.
Abstract
In order to effectively control the quality of naltrexone hydrochloride,seven related substances were synthesized in this study:17-(1-butenyl)-4,5-epoxy-3,14-dihydroxymorphine-6-one(related substance C),bis-naltrexone(related substance D),3-cyclopropylmethoxy-17-(cyclopropylmethyl)-4,5-epoxy-14-hydroxymorphine-6-one(related substance E),17-n-butyl-4,5-epoxy-3,14-dihydroxymorphine-6-one(related substance H),17-(cyclopropylmethyl)-3-methoxyl-4,5-epoxy-14-hydroxymorphine-6-one(related substance J),17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphin-7-ene-6-one(related substance K),naltrexone nitrogen oxide(related substance L).The related substances K and L were not included in European pharmacopoeia 10.0.The synthetic routes of substances C,D and H had not been reported.The structures of these compounds were confirmed by MS,1H NMR and 13C NMR.
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