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1. 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。

2. 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。

3. 发明申请

WO2005004805A2 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：WO2005004805A2
公开(公告)日：2005-01-20
申请号：PCT/US2004/020679
申请日：2004-06-25
申请人： SOLUX CORPORATION , ZABUDKIN, Alexander , MATVIENKO, Victor , MATVYEYEV, Alexey , ITKIN, Aleksandr
发明人： ZABUDKIN, Alexander , MATVIENKO, Victor , MATVYEYEV, Alexey , ITKIN, Aleksandr
IPC分类号： A61K
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 (2θ) 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。

4. 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。

5. 发明申请

WO2010039159A1 THERMALLY STABLE CRYSTALLINE EPIRUBICIN HYDROCHLORIDE 审中-公开
标题翻译：热稳定结晶EPIRUBICIN HYDROCHLORIDE
公开(公告)号：WO2010039159A1
公开(公告)日：2010-04-08
申请号：PCT/US2008/086102
申请日：2008-12-09
申请人： SOLUX CORPORATION , 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
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 theta) and relative intensity P(%) as presented in the Table of Fig. 1.
摘要翻译：盐酸表柔比星的结晶形式称为“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图1的表所示的具有衍射角（2θ）和相对强度P（％）的平均值的粉末X射线衍射图。 1。

6. 发明申请

WO2006096665A1 EPIMERIZATION OF 4'-C BOND AND MODIFICATION OF 14-CH3-(CO)-FRAGMENT IN ANTHRACYCLIN ANTIBIOTICS 审中-公开
标题翻译： 4'-C BOND的化学和14-CH3-（CO）-FRAGMENT在ANTHRACYCLIN抗生素中的修饰
公开(公告)号：WO2006096665A1
公开(公告)日：2006-09-14
申请号：PCT/US2006/007987
申请日：2006-03-06
申请人： SOLUX CORPORATION , MATVIENKO, Victor , MATVYEYEV, Alexey , ZABUDKIN, Alexander , ITKIN, Aleksandr
发明人： MATVIENKO, Victor , MATVYEYEV, Alexey , ZABUDKIN, Alexander , ITKIN, Aleksandr
IPC分类号： A61K31/65 , C07H15/252
CPC分类号： C07H15/252
摘要： A method of synthesizing Rl, R2-substituted-4' (ax. or eq.)-OH anthracyclines and their corresponding salts of Formula (1) from daunorubicin or N-Trifluoroacetyl-4- Rl - derivatives of daunorubicin, wherein Rl is defined as H, OH, and 4'-HO is defined as ax[ial]. The method includes producing N-Trifluoroacetyl daunorubicin and treating the N- Trifluoroacetyldaunorubicin or N-Trifluoroacetyl-4-R 1 -derivatives of daunorubicin, wherein R 1 is defined as H, OH, with dimethylsulfoxide activated by different acylating agents. The attained intermediate product is then treated with a strong base (ex. tertiary amines) resulting in the 4 -keto-N-Trifluoroacetyl-4-R 1 daunorubicin wherein Ri is defined as H, OH, OMe. The 4-keto-N-Trifluoroacetyl-4-R 1 -daunorubicin is reacted with a reducing agent, a derivative of a borohydride of an alkaline metal MHBL 3 ,to produce N- Trifluoroacetyl-4'-epi-4-R 1 -daunorubicin. The N-Trifluoroacetyl-4'-epi-4-R 1 -daunorubicin undergoes hydrolysis in a basic solution to produce a derivate of an anthoacyclin which is halogenized [by complex halogenidesjto form a 14-Hal-derivative. This result is then hydrolyzed by well-known methods in the presence of a formate of an alkaline metal to form the desired final compound.
摘要翻译：从柔红霉素的柔红霉素或N-三氟乙酰基-4-R1-衍生物合成R1，R2-取代-4'（ax。或eq。）-OH蒽环类化合物及其相应的式（1）盐，其中R1定义因为H，OH和4'-HO被定义为ax [ial]。该方法包括生产N-三氟乙酰柔红霉素并处理柔红霉素的N-三氟乙酰基柔红霉素或N-三氟乙酰基-4-R 1 - 1衍生物，其中R 1定义为H， OH，与不同酰化剂活化的二甲亚砜。然后用强碱（例如叔胺）处理得到的中间产物，得到4-酮-N-三氟乙酰基-4-R 1柔红霉素，其中R 1定义为H，OH，OMe 。使4-酮基-N-三氟乙酰基-4-R 1 - 大霉素与还原剂，碱金属MHBL 3 N的硼氢化物的衍生物反应，生成 N-三氟乙酰基-4'-表-i-4-R 1 -daunorubicin。 N-三氟乙酰基-4'-表 - 4-R 1 - 大霉素在碱性溶液中进行水解以产生蒽环衍生物，其通过复合卤化物卤化形成14-Hal衍生物。然后通过公知的方法在碱金属甲酸盐存在下水解该结果，形成所需的最终化合物。

7. 发明申请

WO2009088618A1 METHOD OF ARALKYLATION OF 4'-HYDROXYL GROUP OF ANTHRACYCLINS 审中-公开
标题翻译： 4'-羟基苯甲酸基团的芳基化方法
公开(公告)号：WO2009088618A1
公开(公告)日：2009-07-16
申请号：PCT/US2008/086088
申请日：2008-12-09
申请人： SOLUX CORPORATION , ZABUDKIN, Alexander , MATVIENKO, Victor , MATVEEV, Alexey , ITKIN, Aleksandr
发明人： ZABUDKIN, Alexander , MATVIENKO, Victor , MATVEEV, Alexey , ITKIN, Aleksandr
IPC分类号： A01N43/04 , A61K31/70 , C07H15/24
CPC分类号： C07H15/252
摘要： A method for the aralkylation of anthracyclins by utilizing an aralkylating agent R 3 -CH 2 X (for example, BnBr) in accordance with the reaction pathway describe by the scheme shown in Fig. 1. The present invention recognizes that 4-R 1 , 3'-N 3 -Daunomycines are suitable substrates for selective 4'-O-benzylation, yielding 4-R 1 , 3'-N 3 -4 '-O-Aralkyl-Daunorubicines (in particular, 4'-O-Bn-Daunomycines). Thus, the present invention provides a pathway for a simple production of 4'-O-aralkylated derivatives of anthracyclines which can be effectively used to produce anthracyclines.
摘要翻译：通过利用图3所示方案描述的根据反应途径的芳烷基化试剂R3-CH2X（例如BnBr）对蒽环进行芳烷基化的方法。本发明认识到4-R1，3'-N3-霉素霉素是选择性4'-O-苄基化的合适底物，得到4-R1，3'-N3-4'-O-芳烷基 - 柔红霉素（特别是，4'-O-Bn-道诺霉素）。因此，本发明提供了可以有效地用于生产蒽环类的简单生产蒽环类的4'-O-芳烷基化衍生物的途径。

8. 发明申请

WO2007076345A3 SYNTHESIS OF EPIRUBICIN FROM 13-DIHYDRODAUNORUBICINE 审中-公开
公开(公告)号：WO2007076345A3
公开(公告)日：2007-07-05
申请号：PCT/US2006/062286
申请日：2006-12-19
申请人： SOLUX CORPORATION , 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
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.

9. 发明申请

WO2007070820A2 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：WO2007070820A2
公开(公告)日：2007-06-21
申请号：PCT/US2006/061978
申请日：2006-12-13
申请人： SOLUX CORPORATION , ZABUDKIN, Alexander , MATVIENKO, Victor , MATVEEV, Alexey , ITKIN, Aleksandr
发明人： ZABUDKIN, Alexander , MATVIENKO, Victor , MATVEEV, Alexey , ITKIN, Aleksandr
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。

10. 发明申请

WO2005021565A1 METHOD OF PREPARING 4-R-SUBSTITUTED 4-DEMETHOXYDAUNORUBICIN 审中-公开
标题翻译：制备4-R取代的4-去甲基多巴胺的方法
公开(公告)号：WO2005021565A1
公开(公告)日：2005-03-10
申请号：PCT/US2004/016739
申请日：2004-05-20
申请人： SOLUX CORPORATION , ZABUDKIN, Alexander , MATVIENKO, Victor , MATVYEYEV, Alexey , ITKIN, Aleksandr
发明人： ZABUDKIN, Alexander , MATVIENKO, Victor , MATVYEYEV, Alexey , ITKIN, Aleksandr
IPC分类号： C07H15/252
CPC分类号： C07H15/252 , C07H1/00
摘要： A method of synthesizing 4-R-substituted anthracyclines and their corresponding salts from 4-demethyldaunorubicin includes the steps of treating 4-demethyldaunorubicin with a sulfonylating agent to form 4-demethyl-4-sulfonyl-R 3 -daunorubicin. 4-Demethyl-4-R 3 -sulfonyl-daunorubicin is then subject to a reducing agent in the presence of a transition metal catalyst in a temperature range of about 30 °C to about 100 °C in a polar aprotic solvent in an inert atmosphere. Protected 4-demethoxy-4-R-daunomycin then undergoes hydrolysis in a basic solution to form the 4-R-substituted anthracyclines. The novel method lacks the step of forming a stereospecific glycoside bond between aglycone and aminoglycoside. The method also increases the yield of the final product up to 30 to 40%.
摘要翻译：从4-去甲基柔红霉素合成4-R取代的蒽环类及其相应的盐的方法包括用磺酰化剂处理4-去甲基柔红霉素以形成4-去甲基-4-磺酰基-γ-三柔比星的步骤。然后将4-去甲基-4-R 3 - 磺酰基柔红霉素在过渡金属催化剂存在下，在约30℃至约100℃的温度范围内，在极性非质子溶剂中，在惰性气氛中。然后将受保护的4-脱甲氧基-4R-道宁霉素在碱性溶液中进行水解以形成4-R取代的蒽环类。该新方法缺乏在糖苷配基和氨基糖苷之间形成立体特异性糖苷键的步骤。该方法还可将最终产品的产率提高至30至40％。

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