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1.发明授权PREPARATION METHOD OF RIVASTIGMINE, ITS INTERMEDIATES AND PREPARATION METHOD OF THE INTERMEDIATES 有权利福平的制备方法及其中间体和中间体的制备方法
公开(公告)号：EP2233465B1
公开(公告)日：2017-06-28
申请号：EP08700628.4
申请日：2008-01-10
发明人： ZHANG, Fuli , HU, Meng , XIE, Meihua , LAI, Anping , SUN, Rentong , CHEN, Daoxin , BAO, Rusheng , BAI, Hua
IPC分类号： C07C217/58 , C07C271/44
CPC分类号： C07C217/58 , C07B2200/07 , C07C215/50 , C07C271/44
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2.发明公开
公开(公告)号：EP2711354A1
公开(公告)日：2014-03-26
申请号：EP12785792.8
申请日：2012-05-16
发明人： ZHANG, Fuli , YANG, Zhezhou , YANG, Chunbo , CHEN, Daoxin , YANG, Zhiqing , SUN, Rentong , BAI, Hua
IPC分类号： C07C211/27 , C07C269/06 , C07C271/44 , A61K31/27 , A61P25/28
CPC分类号： C07C271/44 , C07B2200/07 , C07C215/66 , C07C217/58 , C07C269/04 , C07C269/06 , C07C309/04
摘要： The present invention provides the preparation method for (S)-3-(1-(dimethylamino)ethyl)phenyl ethyl(methyl)carbamate (formula X compound), the preparation methods for its intermediates (S)-1-(3-methoxyphenyl)-N,N-dimethyl-N-((S)-1-phenylethyl)ethanaminium(formula VI compound), (S)-1-(3-hydroxyphenyl)-N,N-dimethyl-N-((S)-1-phenylethyl)ethanaminium(formula VIII compound) and (S)-1-(3-(ethyl(methyl)carbamoyloxy)phenyl)-N,N-dimethyl-N-((S)-1-phenylethyl)ethanaminium (formula IX compound), as well as the method for using above mentioned formula IX compound to prepare rivastigmine which can be used for the treatment of Alzheimer's disease. The preparation method for rivastigmine has a reasonable synthetic design with convenient source of raw materials and high total yield, and the product resulted has high chemical and optical purity, which makes it easy for large-scale. industrial production.
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3.发明授权PREPARATION METHOD FOR RIVASTIGMINE, INTERMEDIATES THEREOF, AND PREPARATION METHOD FOR SAID INTERMEDIATES 有权利伐斯汀的制备方法，其中间体以及用于所述中间体的制备方法
公开(公告)号：EP2711354B1
公开(公告)日：2018-02-21
申请号：EP12785792.8
申请日：2012-05-16
发明人： ZHANG, Fuli , YANG, Zhezhou , YANG, Chunbo , CHEN, Daoxin , YANG, Zhiqing , SUN, Rentong , BAI, Hua
IPC分类号： C07C211/27 , C07C269/06 , C07C271/44 , A61K31/27 , A61P25/28
CPC分类号： C07C271/44 , C07B2200/07 , C07C215/66 , C07C217/58 , C07C269/04 , C07C269/06 , C07C309/04
摘要： The present invention provides the preparation method for (S)-3-(1-(dimethylamino)ethyl)phenyl ethyl(methyl)carbamate (formula X compound), the preparation methods for its intermediates (S)-1-(3-methoxyphenyl)-N,N-dimethyl-N-((S)-1-phenylethyl)ethanaminium(formula VI compound), (S)-1-(3-hydroxyphenyl)-N,N-dimethyl-N-((S)-1-phenylethyl)ethanaminium(formula VIII compound) and (S)-1-(3-(ethyl(methyl)carbamoyloxy)phenyl)-N,N-dimethyl-N-((S)-1-phenylethyl)ethanaminium (formula IX compound), as well as the method for using above mentioned formula IX compound to prepare rivastigmine which can be used for the treatment of Alzheimer's disease. The preparation method for rivastigmine has a reasonable synthetic design with convenient source of raw materials and high total yield, and the product resulted has high chemical and optical purity, which makes it easy for large-scale. industrial production.
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4.发明公开PREPARATION METHOD OF RIVASTIGMINE, ITS INTERMEDIATES AND PREPARATION METHOD OF THE INTERMEDIATES 有权用于生产利斯的明及其中间体和工艺中间体的制备方法
公开(公告)号：EP2233465A1
公开(公告)日：2010-09-29
申请号：EP08700628.4
申请日：2008-01-10
发明人： ZHANG, Fuli , HU, Meng , XIE, Meihua , LAI, Anping , SUN, Rentong , CHEN, Daoxin , BAO, Rusheng , BAI, Hua
IPC分类号： C07C211/27 , C07C69/06 , C07C271/44 , A61K31/27 , A61P25/28
CPC分类号： C07C217/58 , C07B2200/07 , C07C215/50 , C07C271/44
摘要： The present invention provides N-methylethylcarbamino-3-[(S)-1-(methyl-[(S)-1-phenylethyl] amino) ethyl] phenyl ester represented by formula (II) and its preparation method. The present invention also provides (S)-1-(3-methoxyphenyl)-N-methyl-N-[(S)-1-phenylethyl] ethylamine and 3-[(S)-1-(methyl-[(S)-1-phenylethyl] amino) ethyl] phenol as intermediates of the compound represented by formula (II), and the use of the compound represented by formula (II) for preparing rivastigmine used for treating Alzheimer disease.
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