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1. 发明授权

KR100425881B1 신규한 몰피난 유도체 失效
标题翻译： 신규한몰피난유도체
公开(公告)号：KR100425881B1
公开(公告)日：2004-04-03
申请号：KR1020010013173
申请日：2001-03-14
申请人： 김형춘 , 고광호 , 최신건 , 주왕기 , 신은주 , 이필호
发明人： 김형춘 , 주왕기 , 이필호 , 고광호 , 최신건 , 신은주
IPC分类号： C07D221/28
摘要： PURPOSE: Provided is a method for manufacturing a morphinan derivative which is very effective in preventing cramps and protecting nerves by changing groups at C3 and C17 of morphinan. CONSTITUTION: The method for manufacturing a morphinan derivative of the formula (1) comprises the next steps of: i) methylating dextrometrophan hydrobromide to obtain dextrophan of the formula (3); ii) reacting dextrophan with cyclopropylmethyl bromide or aryl bromide in the presence of hydride sodium to manufacture 3-cyclopropylmethoxy-17-methylmorphinan and 3-aryloxy-17-methylmorphinan; and iii) reacting 3-aryloxy-17-methylmorphinan with 1-chloroethyl chloroformate to obtain 3-aryloxymorphinan of the formula (5). In the formula, R is cyclopropylmethyl or aryl group. R' is a methyl group when R is a cyclopropylmethyl group and is hydrogen when R is an aryl group.
摘要翻译：目的：提供一种吗啡喃衍生物的制备方法，它通过改变吗啡喃的C3和C17基团而在预防痉挛和保护神经方面非常有效。构成：制备式（1）的吗啡喃衍生物的方法包括以下步骤：i）甲基化右啡索酸氢溴酸以获得式（3）的右啡肽; ii）在氢化钠存在下，将右旋氯丙烷与环丙基甲基溴或芳基溴化物反应，制备3-环丙基甲氧基-17-甲基吗啡喃和3-芳氧基-17-甲基吗啡喃; 和iii）使3-芳氧基-17-甲基吗啡喃与氯甲酸1-氯乙酯反应，得到式（5）的3-芳氧基吗啡喃。在该式中，R是环丙基甲基或芳基。当R是环丙基甲基时，R'是甲基，而当R是芳基时，R'是氢。

2. 发明公开

KR1020010044661A 신규한 몰피난 유도체 失效
标题翻译：制造新奇莫衍生物的方法
公开(公告)号：KR1020010044661A
公开(公告)日：2001-06-05
申请号：KR1020010013173
申请日：2001-03-14
申请人： 김형춘 , 고광호 , 최신건 , 주왕기 , 신은주 , 이필호
发明人： 김형춘 , 주왕기 , 이필호 , 고광호 , 최신건 , 신은주
IPC分类号： C07D221/28
摘要： PURPOSE: Provided is a method for manufacturing a morphinan derivative which is very effective in preventing cramps and protecting nerves by changing groups at C3 and C17 of morphinan. CONSTITUTION: The method for manufacturing a morphinan derivative of the formula (1) comprises the next steps of: i) methylating dextrometrophan hydrobromide to obtain dextrophan of the formula (3); ii) reacting dextrophan with cyclopropylmethyl bromide or aryl bromide in the presence of hydride sodium to manufacture 3-cyclopropylmethoxy-17-methylmorphinan and 3-aryloxy-17-methylmorphinan; and iii) reacting 3-aryloxy-17-methylmorphinan with 1-chloroethyl chloroformate to obtain 3-aryloxymorphinan of the formula (5). In the formula, R is cyclopropylmethyl or aryl group. R' is a methyl group when R is a cyclopropylmethyl group and is hydrogen when R is an aryl group.
摘要翻译：目的：提供吗啡喃衍生物的制备方法，其通过改变吗啡喃的C3和C17的基团非常有效地预防痉挛和保护神经。构成：制备式（1）的吗啡喃衍生物的方法包括以下步骤：i）甲基化右美沙芬氢溴酸盐，得到式（3）的右旋糖酐; ii）在氢化钠存在下使右旋丙醚与环丙基甲基溴或芳基溴反应，制备3-环丙基甲氧基-17-甲基吗啡喃和3-芳氧基-17-甲基吗啡喃; 和iii）使3-芳氧基-17-甲基吗啡喃与氯甲酸1-氯乙酯反应，得到式（5）的3-芳氧基吗啡喃。在该式中，R是环丙基甲基或芳基。当R为环丙基甲基时，R'为甲基，当R为芳基时，R'为氢。

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