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1.发明申请PROCESS FOR THE PREPARATION OF (POLY) AMINOALKYLAMINOACETAMIDE DERIVATIVES OF EPIPODOPHYLLOTOXIN USEFUL FOR THEIR APPLICATIONS IN THERAPEUTICS AS ANTICANCER AGENT 有权制备用于抗生素治疗药物的应用的EPIPODOPHYLLOTOXIN的（多）氨基氨基甲酰胺衍生物的方法公开(公告)号：US20120022273A1
公开(公告)日：2012-01-26
申请号：US12733864
申请日：2008-09-23
IPC分类号： C07D493/04 , C07C269/06 , C07C271/22
CPC分类号： C07C227/20 , C07C271/22 , C07D493/04 , Y02P20/55
摘要： The present invention relates to a new process for the preparation of (poly)aminoalkylaminoacetamide derivatives of epipodophyllotoxin and salts thereof, characterised in that it comprises a step of peptide coupling of 4-amino-4′-demethylepipodophyllotoxin with an amine-containing reactant having protecting groups.
摘要翻译： 本发明涉及一种制备表鬼臼毒素的（多）氨基烷基氨基乙酰胺衍生物及其盐的新方法，其特征在于其包括4-氨基-4'-脱甲基表鬼臼毒素与含胺反应物的肽偶联的步骤，其具有保护作用 团体
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2.发明授权公开(公告)号：US07932406B2
公开(公告)日：2011-04-26
申请号：US11988942
申请日：2006-07-19
IPC分类号： C07D317/70
CPC分类号： C07D493/04
摘要： The invention relates to a method for synthesizing 4.beta.-amino-4′-demethyl-4-desoxypodophyllotoxin of formula (1), characterized by comprising the following successive steps: a) reacting, in a pure weak acid or in a mixture consisting of acid, water and of organic solvent, without another solvent, at a temperature higher than the ambient temperature, thiourea with 4.beta.-halogenoacetamido-4′-demethyl-4-desoxypodophyllotoxin, and; b) recovering the 4.beta.-amino-4′-demethyl-4-desoxypodophyllotoxin.
摘要翻译： 本发明涉及一种合成式（1）的β-氨基-4'-脱甲基-4-脱氧鬼臼毒素的方法，其特征在于包括以下连续步骤：a）在纯的弱酸或混合物 由酸，水和有机溶剂组成，没有另一种溶剂，在高于环境温度的温度下，硫脲与4.β-卤代乙酰胺基-4'-去甲基-4-脱氧鬼臼毒素，和 b）回收4.β-氨基-4'-去甲基-4-脱氧鬼臼毒素。
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3.发明授权公开(公告)号：US08193379B2
公开(公告)日：2012-06-05
申请号：US12894684
申请日：2010-09-30
IPC分类号： C07D317/70
CPC分类号： C07D493/04
摘要： The invention relates to a method for synthesizing 4β-amino-4′-demethyl-4-desoxypodophyllotoxin of formula (1), characterized by comprising the following successive steps: a) reacting, in a pure weak acid or in a mixture consisting of acid, water and of organic solvent, without another solvent, at a temperature higher than the ambient temperature, thiourea with 4β-halogenoacetamido-4′-demethyl-4-desoxypodophyllotoxin, and; b) recovering the 4β-amino-4′-demethyl-4-desoxypodophyllotoxin.
摘要翻译： 本发明涉及一种合成式（1）的4'-二氨基-4'-脱甲基-4-脱氧鬼臼毒素的方法，其特征在于包括以下连续步骤：a）在纯的弱酸或由 酸，水和有机溶剂，没有另一种溶剂，在高于环境温度的温度下，硫脲与4'-卤代乙酰氨基-4'-去甲基-4-脱氧鬼臼毒素，和 b）回收4'-二 - 氨基-4'-去甲基-4-脱氧鬼臼毒素。
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4.发明授权Process for the synthesis of anticancer (poly) aminoalkylaminoacetamide derivatives of epipodophyllotoxin 有权合成表鬼臼毒素的抗癌（poly）氨基烷基氨基乙酰胺衍生物的方法公开(公告)号：US08148552B2
公开(公告)日：2012-04-03
申请号：US12733862
申请日：2008-09-23
IPC分类号： C07D307/77
CPC分类号： C07D493/04
摘要： The present invention describes a new process for the preparation of (poly)aminoalkylaminoacetamide compounds of epipodophyllotoxin useful for their applications in therapeutics as anticancer agents. This process comprises a step of condensation of a primary-amine-containing reactant, whose amine functions are not protected, with β-chloroacetamido-4′-epipodophyllotoxin in a polar aprotic organic solvent.
摘要翻译： 本发明描述了一种制备用于治疗作为抗癌剂的表鬼臼毒素的（多）氨基烷基氨基乙酰胺化合物的新方法。 该方法包括将其胺官能团未被保护的伯胺反应物与极性非质子有机溶剂中的β-氯代乙酰胺基-4'-表鬼臼毒素缩合的步骤。
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5.发明授权Process for the preparation of (poly) aminoalkylaminoacetamide derivatives of epipodophyllotoxin useful for their applications in therapeutics as anticancer agent 有权用于制备用于治疗作为抗癌剂的表鬼臼毒素的（多）氨基烷基氨基乙酰胺衍生物的方法公开(公告)号：US08664409B2
公开(公告)日：2014-03-04
申请号：US12733864
申请日：2008-09-23
IPC分类号： C07D307/77
CPC分类号： C07C227/20 , C07C271/22 , C07D493/04 , Y02P20/55
摘要： The present invention relates to a new process for the preparation of (poly)aminoalkylaminoacetamide derivatives of epipodophyllotoxin and salts thereof, characterized in that it comprises a step of peptide coupling of 4-amino-4′-demethylepipodophyllotoxin with an amine-containing reactant having protecting groups.
摘要翻译： 本发明涉及一种制备表鬼臼毒素的（多）氨基烷基氨基乙酰胺衍生物及其盐的新方法，其特征在于其包括4-氨基-4'-脱甲基表鬼臼毒素与含胺反应物的肽偶联的步骤，其具有保护作用 团体
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6.发明申请公开(公告)号：US20110021791A1
公开(公告)日：2011-01-27
申请号：US12894684
申请日：2010-09-30
IPC分类号： C07D407/10
CPC分类号： C07D493/04
摘要： The invention relates to a method for synthesizing 4β-amino-4′-demethyl-4-desoxypodophyllotoxin of formula (1), characterized by comprising the following successive steps: a) reacting, in a pure weak acid or in a mixture consisting of acid, water and of organic solvent, without another solvent, at a temperature higher than the ambient temperature, thiourea with 4β-halogenoacetamido-4′-demethyl-4-desoxypodophyllotoxin, and; b) recovering the 4β-amino-4′-demethyl-4-desoxypodophyllotoxin.
摘要翻译： 本发明涉及一种合成式（1）的4'-二氨基-4'-脱甲基-4-脱氧鬼臼毒素的方法，其特征在于包括以下连续步骤：a）在纯的弱酸或由 酸，水和有机溶剂，没有另一种溶剂，在高于环境温度的温度下，硫脲与4'-卤代乙酰氨基-4'-去甲基-4-脱氧鬼臼毒素，和 b）回收4'-二 - 氨基-4'-去甲基-4-脱氧鬼臼毒素。
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7.发明申请Process for the Synthesis of Anticancer (Poly) Aminoalkylaminoacetamide Derivatives of Epipodophyllotoxin 有权用于合成表鬼臼毒素的抗癌（Poly）氨基烷基氨基乙酰胺衍生物的方法公开(公告)号：US20100280263A1
公开(公告)日：2010-11-04
申请号：US12733862
申请日：2008-09-23
IPC分类号： C07D493/04
CPC分类号： C07D493/04
摘要： The present invention describes a new process for the preparation of (poly)aminoalkylaminoacetamide compounds of epipodophyllotoxin useful for their applications in therapeutics as anticancer agents. This process comprises a step of condensation of a primary-amine-containing reactant, whose amine functions are not protected, with β-chloroacetamido-4′-epipodophyllotoxin in a polar aprotic organic solvent.
摘要翻译： 本发明描述了一种制备用于治疗作为抗癌剂的表鬼臼毒素的（多）氨基烷基氨基乙酰胺化合物的新方法。 该方法包括将其胺官能团未被保护的伯胺反应物与极性非质子有机溶剂中的β-氯代乙酰胺基-4'-表鬼臼毒素缩合的步骤。
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8.发明申请Method for preparing 4beta-amino-4'-demethyl-4-desoxypodophyllotoxin 有权制备4beta-amino-4'-去甲基-4-脱氧鬼臼毒素的方法公开(公告)号：US20090137826A1
公开(公告)日：2009-05-28
申请号：US11988942
申请日：2006-07-19
IPC分类号： C07D317/70
CPC分类号： C07D493/04
摘要： The invention relates to a method for synthesizing 4β-amino-4′-demethyl-4-desoxypodophyllotoxin of formula (1), characterized by comprising the following successive steps: a) reacting, in a pure weak acid or in a mixture consisting of acid, water and of organic solvent, without another solvent, at a temperature higher than the ambient temperature, thiourea with 4β-halogenoacetamido-4′-demethyl-4-desoxypodophyllotoxin, and; b) recovering the 4β-amino-4′-demethyl-4-desoxypodophyllotoxin.
摘要翻译： 本发明涉及一种合成式（1）的4,4'-氨基-4'-脱甲基-4-脱氧鬼臼毒素的方法，其特征在于包括以下连续步骤：a）在纯的弱酸或由酸组成的混合物中反应 ，水和有机溶剂，没有另一种溶剂，在高于环境温度的温度下，硫脲与4beta-卤代乙酰氨基-4'-去甲基-4-脱氧鬼臼毒素，和; b）回收4beta-amino-4'-去甲基-4-脱氧鬼臼毒素。
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