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1.发明授权Method for the preparation of cinacalcet and intermediates and impurities thereof 有权西那卡塞及其中间体及其杂质的制备方法公开(公告)号：US08969623B2
公开(公告)日：2015-03-03
申请号：US14052116
申请日：2013-10-11
发明人： Vijayavitthal Thippannachar Mathad , Navnath Chintaman Niphade , Gorakshanath Balasaheb Shinde , Sharad Subhash Ippar , Shrikant Prataprao Deshmukh , Raghavendra Kumar Panchangam
IPC分类号： C07C209/00 , C07C209/62 , C07C209/86 , C07C211/08 , C07C249/02 , C07C251/30 , C07C211/30 , C07C251/16 , C07C251/24 , C07C251/06
CPC分类号： C07C209/62 , C07B2200/07 , C07B2200/13 , C07C211/30 , C07C249/02 , C07C251/06 , C07C251/16 , C07C251/24 , C07C251/30
摘要： A method for the preparation of Cinacalcet is disclosed comprising treating (R)-1-naphthyl ethylamine with an aromatic aldehyde to form (1R)-1-(2-naphthyl)-N-(aryl methylene)ethanamine derivative of Formula (IV), which is further treated with 1-(3-halopropyl)-3-(trifluoromethyl)benzene of Formula (V) to obtain an iminium salt of Formula (VI), followed by hydrolysis to obtain Cinacalcet free base.
摘要翻译： 公开了制备西那卡塞的方法，其包括用芳族醛处理（R）-1-萘基乙胺以形成式（IV）的（1R）-1-（2-萘基）-N-（芳基亚甲基）乙胺衍生物 ，其进一步用式（V）的1-（3-卤代丙基）-3-（三氟甲基）苯处理，得到式（VI）的亚铵盐，随后水解得到西那卡塞游离碱。
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2.发明申请Method For The Preparation Of Cinacalcet And Intermediates And Impurities Thereof 审中-公开西那卡塞及其中间体及其杂质的制备方法公开(公告)号：US20150152040A1
公开(公告)日：2015-06-04
申请号：US14600258
申请日：2015-01-20
发明人： Vijayavitthal Thippannachar Mathad , Navnath Chintaman Niphade , Gorakshanath Balasaheb Shinde , Sharad Subhash Ippar , Shrikant Prataprao Deshmukh , Raghavendra Kumar Panchangam
IPC分类号： C07C209/62 , C07C249/02 , C07C251/24
CPC分类号： C07C209/62 , C07B2200/07 , C07B2200/13 , C07C211/30 , C07C249/02 , C07C251/06 , C07C251/16 , C07C251/24 , C07C251/30
摘要： A method for the preparation of Cinacalcet is disclosed comprising treating (R)-1-naphthyl ethylamine with an aromatic aldehyde to form (1R)-1-(2-naphthyl)-N-(aryl methylene)ethanamine derivative of Formula (IV), which is further treated with 1-(3-halopropyl)-3-(trifluoromethyl)benzene of Formula (V) to obtain an iminium salt of Formula (VI), followed by hydrolysis to obtain Cinacalcet free base.
摘要翻译： 公开了制备西那卡塞的方法，其包括用芳族醛处理（R）-1-萘基乙胺以形成式（IV）的（1R）-1-（2-萘基）-N-（芳基亚甲基）乙胺衍生物 ，其进一步用式（V）的1-（3-卤代丙基）-3-（三氟甲基）苯处理，得到式（VI）的亚铵盐，随后水解得到西那卡塞游离碱。
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3.发明申请Method For The Preparation Of Cinacalcet And Intermediates And Impurities Thereof 有权西那卡塞及其中间体及其杂质的制备方法公开(公告)号：US20140081048A1
公开(公告)日：2014-03-20
申请号：US14052116
申请日：2013-10-11
发明人： Vijayavitthal Thippannachar Mathad , Navnath Chintaman Niphade , Gorakshanath Balasaheb Shinde , Sharad Subhash Ippar , Shrikant Prataprao Deshmukh , Raghavendra Kumar Panchangam
IPC分类号： C07C209/62 , C07C249/02 , C07C251/06
CPC分类号： C07C209/62 , C07B2200/07 , C07B2200/13 , C07C211/30 , C07C249/02 , C07C251/06 , C07C251/16 , C07C251/24 , C07C251/30
摘要： A method for the preparation of Cinacalcet is disclosed comprising treating (R)-1-naphthyl ethylamine with an aromatic aldehyde to form (1R)-1-(2-naphthyl)-N-(aryl methylene)ethanamine derivative of Formula (IV), which is further treated with 1-(3-halopropyl)-3-(trifluoromethyl)benzene of Formula (V) to obtain an iminium salt of Formula (VI), followed by hydrolysis to obtain Cinacalcet free base.
摘要翻译： 公开了制备西那卡塞的方法，其包括用芳族醛处理（R）-1-萘基乙胺以形成式（IV）的（1R）-1-（2-萘基）-N-（芳基亚甲基）乙胺衍生物 ，其进一步用式（V）的1-（3-卤代丙基）-3-（三氟甲基）苯处理，得到式（VI）的亚铵盐，随后水解得到西那卡塞游离碱。
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