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1. 发明申请

WO2005004805A3 THERMALLY STABLE CRYSTALLINE EPIRUBICIN HYDROCHLORIDE AND METHOD OF MAKING THE SAME 审中-公开
标题翻译：热稳定的环丙沙星盐酸盐及其制备方法
公开(公告)号：WO2005004805A3
公开(公告)日：2006-06-22
申请号：PCT/US2004020679
申请日：2004-06-25
申请人： SOLUX CORP , ZABUDKIN ALEXANDER , MATVIENKO VICTOR , MATVYEYEV ALEXEY , ITKIN ALEKSANDR
发明人： ZABUDKIN ALEXANDER , MATVIENKO VICTOR , MATVYEYEV ALEXEY , ITKIN ALEKSANDR
IPC分类号： C07H15/24 , A61K20060101 , A61K31/704
CPC分类号： C07H15/24
摘要： A crystalline form of epirubicin hydrochloride, named herein as "type II" crystalline epirubicin hydrochloride, has excellent thermal stability. Type II crystalline epirubicin hydrochloride has a powder X-ray diffraction pattern having average values of diffraction angle (2?) and relative intensity P(%) as presented in the following table (I).
摘要翻译：盐酸表柔比星的结晶形式，在本文中称为“II型”结晶表柔比星盐酸盐，具有优异的热稳定性。 II型结晶表柔比星盐酸盐具有如下表（I）所示的具有衍射角（2θ）和相对强度P（％）的平均值的粉末X射线衍射图。

2. 发明申请

WO2007070820A3 METHOD FOR PREPARING 4-DEMETHYLDAUNORUBICIN 审中-公开
标题翻译：制备4-去甲基多柔比星的方法
公开(公告)号：WO2007070820A3
公开(公告)日：2008-03-27
申请号：PCT/US2006061978
申请日：2006-12-13
申请人： SOLUX CORP , ZABUDKIN ALEXANDER , MATVIENKO VICTOR , MATVEEV ALEXEY , ITKIN ALEKSANDR
发明人： ZABUDKIN ALEXANDER , MATVIENKO VICTOR , MATVEEV ALEXEY , ITKIN ALEKSANDR
IPC分类号： C07H15/24 , A01N43/04 , A61K31/70
CPC分类号： C07H15/24
摘要： A method of preparing the anthracyclin carminomycin using a starting material comprising daunorubicin. The method comprises reacting daunorubicin or N-protected daunorubicin with soft Lewis acids for the demethylation of the 4-methoxy group, resulting in a reaction mass. The reaction mass is treated with an aqueous solution of a strong organic acid or a mineral acid. After decomposition of the resulting carminomycin and Lewis acids reactive complex, the reaction mass is extracted using a water insoluble organic solvent. As a result, carminomycin is extracted as a base.
摘要翻译：使用包含柔红霉素的起始材料制备蒽环霉素卡明霉素的方法。该方法包括将柔红霉素或N-保护的柔红霉素与软路易斯酸反应，以使4-甲氧基脱甲基，得到反应物质。反应物质用强有机酸或无机酸的水溶液处理。所得的卡培霉素和路易斯酸反应性络合物分解后，使用水不溶性有机溶剂提取反应物质。结果，将卡培霉素提取为碱。

3. 发明申请

WO2007076345A2 SYNTHESIS OF EPIRUBICIN FROM 13-DIHYDRODAUNORUBICINE 审中-公开
标题翻译：来自13-二氢异喹啉的EPIRUBICIN的合成
公开(公告)号：WO2007076345A2
公开(公告)日：2007-07-05
申请号：PCT/US2006062286
申请日：2006-12-19
申请人： SOLUX CORP , ZABUDKIN ALEXANDER , MATVIENKO VICTOR , MATVEEV ALEXEY , ITKIN ALEKSANDR
发明人： ZABUDKIN ALEXANDER , MATVIENKO VICTOR , MATVEEV ALEXEY , ITKIN ALEKSANDR
IPC分类号： A61K31/704 , C07H15/24
CPC分类号： C07H1/00 , C07H15/24 , C07H15/252
摘要： A method of preparing an anthracyclin such as epirubicin from a starting material comprising 13-dihydrodaunorubicine (13-daunorubicinol). The method comprises producing N-Trifluoroacetyl-13-daunorubicinol from 13-daunorubicinol by acylation. The N-Trifluoroacetyl-13-daunorubicinol is reacted with an aprotic solvent and an acylating agent to produce an intermediate sulfoxy salt which is treated with a strong base to produce 4'-keto-N-Trifluoroacetyldaunorubicin. The 4'-keto-N-Trifluoroacetyldaunorubicin is reacted with a reducing agent, such as borohydride of an alkaline metal, to produce N-Trifluoroacetyl-4'-epi-daunorubicin. The N-Trifluoroacetyl-4`-epi-daunorubicin is hydrolyzed in a basic solution to produce an intermediate compound. The intermediate compound is reacted with a halogenizing agent to produce a 14-Hal-derivative. The 14-Hal derivative is hydrolized in the presence of a formate of an alkaline metal to produce the desired final compound.
摘要翻译：从包含13-二氢阿柔比星（13-柔红霉素）的原料制备蒽环类似表柔比星的方法。该方法包括通过酰化由13-柔红霉素生产N-三氟乙酰基-13-柔红霉素。将N-三氟乙酰基-13-柔红霉素与非质子传递溶剂和酰化剂反应，生成中间体磺酰氧基盐，用强碱处理产生4'-酮 - 三氟乙酰基柔红霉素。 4'-酮-N-三氟乙酰基柔红霉素与还原剂如碱金属的硼氢化物反应，生成N-三氟乙酰基-4'-表柔比星。将N-三氟乙酰基-4'-表柔比星在碱性溶液中水解以产生中间体化合物。使中间体化合物与卤化剂反应生成14-Hal衍生物。将14-Hal衍生物在碱金属甲酸盐存在下水解，得到所需的最终化合物。

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