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公开(公告)号：US07507861B2
公开(公告)日：2009-03-24
申请号：US11169995
申请日：2005-06-28
申请人： Eugenio Castelli , Giuseppe Lo Monaco , Silvia Mantovani , Paola Daverio , Paolo Riva , Alessandra Vailati , Stefano Bianchi
发明人： Eugenio Castelli , Giuseppe Lo Monaco , Silvia Mantovani , Paola Daverio , Paolo Riva , Alessandra Vailati , Stefano Bianchi
IPC分类号： C07C213/06
CPC分类号： C07C217/16 , C07B2200/07 , C07C213/06 , C07C213/08 , C07C217/48
摘要： The present invention provides improved processes for the preparation of atomoxetine hydrochloride under reaction conditions that improve reaction yields and facilitate commercial synthesis. In particular, the invention is directed to the synthesis of atomoxetine HCl by adding HCl to a mixture of (R)-(−)-tomoxetine (S)-(+)-mandelate with an organic solvent, with or without a base and water.
摘要翻译： 在提高反应产率和促进商业合成的反应条件下，本发明提供了制备盐酸阿托西汀的改进方法。 特别地，本发明涉及通过向（R） - （ - ） - 托莫西汀（S） - （+） - 扁桃酸酯与有机溶剂，有或没有碱和水的混合物中加入HCl来合成阿托莫西汀HCl 。
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2.发明申请Process for preparing memantine hydrochloride substantially free of impurities 审中-公开基本上不含杂质的美金刚盐酸盐的制备方法公开(公告)号：US20080033054A1
公开(公告)日：2008-02-07
申请号：US11729005
申请日：2007-03-27
IPC分类号： A61K31/13 , A61P25/16 , A61P25/28 , C07C211/38 , G01N30/02
CPC分类号： C07C209/84 , C07C209/50 , C07C233/06 , C07C2603/74 , C07C211/38
摘要： The present invention encompasses processes for preparing Memantine hydrochloride and its derivatives, substantially free of impurities.
摘要翻译： 本发明包括基本上不含杂质的美金刚盐酸盐及其衍生物的制备方法。
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3.发明授权Isolated atomoxetine impurity, processes for the preparation of atomoxetine impurities and their use as reference standards 失效分离的阿托莫西汀杂质，制备阿托莫西汀杂质的方法及其作为参考标准公开(公告)号：US07378553B2
公开(公告)日：2008-05-27
申请号：US11170430
申请日：2005-06-28
IPC分类号： C07C213/06
CPC分类号： C07C217/16 , C07B2200/07 , C07C213/06 , C07C213/08 , C07C217/48
摘要： The present invention provides isolated N-methyl-3-(3-methylphenoxy)-3-phenylpropylamine hydrochloride, and preparation thereof as well as of N-methyl-3-(4-methylphenoxy)-3-phenylpropylamine hydrochloride and of N-methyl-3-phenoxy-3-phenylpropylamine hydrochloride. The invention further provides the use of the above compounds as reference markers and/or reference standards during the synthesis of Atomoxetine. Also provided is a method of limiting the amounts of the impurities 3FT (3-fluorotoluene), 4FT (4-fluorotoluene), and FB (fluorobenzene) in the 2-fluorotoluene starting material used in the synthesis of Atomoxetine Hydrochloride. The purity of the Atomoxetine Hydrochloride product is ensured by determining the amounts of 3FT, 4FT, and FB in the 2-fluorotoluene starting material with the marker 3-ATM HCl.
摘要翻译： 本发明提供了分离的N-甲基-3-（3-甲基苯氧基）-3-苯基丙胺盐酸盐及其制备方法以及N-甲基-3-（4-甲基苯氧基）-3-苯基丙胺盐酸盐和N-甲基 -3-苯氧基-3-苯基丙胺盐酸盐。 本发明还提供了在阿莫西汀合成期间上述化合物作为参考标记和/或参考标准物的用途。 还提供了限制用于合成阿托莫西汀盐酸盐的2-氟甲苯原料中杂质3FT（3-氟甲苯），4FT（4-氟甲苯）和FB（氟苯）的量的方法。 通过用标记3-ATM HCl测定2-氟甲苯原料中的3FT，4FT和FB的量来确保盐酸阿莫西汀产品的纯度。
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公开(公告)号：US07355078B2
公开(公告)日：2008-04-08
申请号：US11170429
申请日：2005-06-28
申请人： Eugenio Castelli , Giuseppe Lo Monaco , Silvia Mantovani , Paola Daverio , Paolo Riva , Alessandra Vailati , Stefano Bianchi
发明人： Eugenio Castelli , Giuseppe Lo Monaco , Silvia Mantovani , Paola Daverio , Paolo Riva , Alessandra Vailati , Stefano Bianchi
IPC分类号： C07C213/08
CPC分类号： C07C217/16 , C07B2200/07 , C07C213/06 , C07C213/08 , C07C217/48
摘要： Provided are processes for preparing tomoxetine comprising reacting N-methyl-3-hydroxy-3-phenylpropylamine with dimethylsulfoxide (DMSO) and 2-fluorotoluene in the presence of an alkali base to form tomoxetine. Also provided is the conversion of said tomoxetine into atomoxetine or a pharmaceutically acceptable salt thereof.
摘要翻译： 提供了制备托莫西汀的方法，其包括在碱碱存在下使N-甲基-3-羟基-3-苯基丙胺与二甲基亚砜（DMSO）和2-氟甲苯反应，形成托莫西汀。 还提供了所述托莫西汀转化为阿托西汀或其药学上可接受的盐。
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公开(公告)号：US20060009489A1
公开(公告)日：2006-01-12
申请号：US11169995
申请日：2005-06-28
申请人： Eugenio Castelli , Giuseppe Lo Monaco , Silvia Mantovani , Paola Daverio , Paolo Riva , Alessandra Vailati , Stefano Bianchi
发明人： Eugenio Castelli , Giuseppe Lo Monaco , Silvia Mantovani , Paola Daverio , Paolo Riva , Alessandra Vailati , Stefano Bianchi
IPC分类号： A61K31/47
CPC分类号： C07C217/16 , C07B2200/07 , C07C213/06 , C07C213/08 , C07C217/48
摘要： The present invention provides improved processes for the preparation of atomoxetine hydrochloride under reaction conditions that improve reaction yields and facilitate commercial synthesis. In particular, the invention is directed to the synthesis of atomoxetine HCl by adding HCl to a mixture of (R)-(−)-tomoxetine (S)-(+)-mandelate with an organic solvent, with or without a base and water.
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公开(公告)号：US20080214846A1
公开(公告)日：2008-09-04
申请号：US12151530
申请日：2008-05-06
IPC分类号： C07D307/78
CPC分类号： C07D405/06 , C07D207/09 , C07D207/48 , C07D307/79
摘要： Provided are darifenacin hydrobromide free of oxidized darifenacin, and processes for the preparation thereof.
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公开(公告)号：US07317127B2
公开(公告)日：2008-01-08
申请号：US11170379
申请日：2005-06-28
申请人： Eugenio Castelli , Giuseppe Lo Monaco , Silvia Mantovani , Paola Daverio , Paolo Riva , Alessandra Vailati , Stefano Bianchi
发明人： Eugenio Castelli , Giuseppe Lo Monaco , Silvia Mantovani , Paola Daverio , Paolo Riva , Alessandra Vailati , Stefano Bianchi
IPC分类号： C07C209/88 , A61K31/135 , C07B57/00
CPC分类号： C07C217/16 , C07B2200/07 , C07C213/06 , C07C213/08 , C07C217/48
摘要： The present invention provides a process for the optical resolution of racemic tomoxetine under reaction conditions that improve reaction yields and optical purity. The invention also provides an epimerization process for the (S)-(+) enantiomer. The invention further provides the conversion of the enantiomer obtained from the optical resolution into atomoxetine or a pharmaceutically acceptable salt thereof.
摘要翻译： 本发明提供了在提高反应产率和光学纯度的反应条件下旋光拆分外消旋的托莫西汀的方法。 本发明还提供了（S） - （+）对映体的差向异构化方法。 本发明还提供了从光学拆分得到的对映异构体转化成阿托莫西汀或其药学上可接受的盐。
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公开(公告)号：US20080269504A1
公开(公告)日：2008-10-30
申请号：US12217252
申请日：2008-07-01
IPC分类号： C07D405/10
CPC分类号： C07D405/06 , C07D207/09 , C07D207/48 , C07D307/79
摘要： Provided are darifenacin hydrobromide free of oxidized darifenacin, and processes for the preparation thereof.
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9.发明申请Pure darifenacin hydrobromide substantially free of oxidized darifenacin and salts thereof and processes for the preparation thereof 审中-公开基本上不含氧化的达西那新及其盐的纯达赖芬那新氢溴酸盐及其制备方法公开(公告)号：US20080216562A1
公开(公告)日：2008-09-11
申请号：US12151535
申请日：2008-05-06
IPC分类号： G01N30/02
CPC分类号： C07D405/06 , C07D207/09 , C07D207/48 , C07D307/79
摘要： Provided are darifenacin hydrobromide free of oxidized darifenacin, and processes for the preparation thereof.
摘要翻译： 提供不含氧化的达瑞芬酸的达立芬那酸氢溴酸盐及其制备方法。
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10.发明申请Isolated atomoxetine impurity, processes for the preparation of atomoxetine impurities and their use as reference standards 失效分离的阿托莫西汀杂质，制备阿托莫西汀杂质的方法及其作为参考标准公开(公告)号：US20060009532A1
公开(公告)日：2006-01-12
申请号：US11170430
申请日：2005-06-28
IPC分类号： A61K31/135
CPC分类号： C07C217/16 , C07B2200/07 , C07C213/06 , C07C213/08 , C07C217/48
摘要： The present invention provides isolated N-methyl-3-(3-methylphenoxy)-3-phenylpropylamine hydrochloride, and preparation thereof as well as of N-methyl-3-(4-methylphenoxy)-3-phenylpropylamine hydrochloride and of N-methyl-3-phenoxy-3-phenylpropylamine hydrochloride. The invention further provides the use of the above compounds as reference markers and/or reference standards during the synthesis of Atomoxetine. Also provided is a method of limiting the amounts of the impurities 3FT (3-fluorotoluene), 4FT (4-fluorotoluene), and FB (fluorobenzene) in the 2-fluorotoluene starting material used in the synthesis of Atomoxetine Hydrochloride. The purity of the Atomoxetine Hydrochloride product is ensured by determining the amounts of 3FT, 4FT, and FB in the 2-fluorotoluene starting material with the marker 3-ATM HCl.
摘要翻译： 本发明提供了分离的N-甲基-3-（3-甲基苯氧基）-3-苯基丙胺盐酸盐及其制备方法以及N-甲基-3-（4-甲基苯氧基）-3-苯基丙胺盐酸盐和N-甲基 -3-苯氧基-3-苯基丙胺盐酸盐。 本发明还提供了在阿莫西汀合成期间上述化合物作为参考标记和/或参考标准物的用途。 还提供了限制用于合成阿托莫西汀盐酸盐的2-氟甲苯原料中杂质3FT（3-氟甲苯），4FT（4-氟甲苯）和FB（氟苯）的量的方法。 通过用标记3-ATM HCl测定2-氟甲苯原料中的3FT，4FT和FB的量来确保盐酸阿莫西汀产品的纯度。
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