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公开(公告)号：US07129378B2
公开(公告)日：2006-10-31
申请号：US10508941
申请日：2003-04-07
IPC分类号： C07C209/62
CPC分类号： C07D291/04 , C07B2200/07 , C07C209/52 , C07C249/02 , C07C303/34 , C07C2601/04 , C07D453/04 , C07C307/02 , C07C211/29 , C07C251/16
摘要： This invention provides a method of preparing amine stereoisomers, which comprises stereoselectively reducing a sulfinylimine that bears on the sulfinyl group a residue of an alcohol, thiol or amine, or reacting a sulfinylimine stereoisomer that bears on the sulfinyl group a residue of an alcohol, thiol or amine with a source of a nucleophile, to afford a sulfinylamine stereoisomer, followed by contacting the sulfinylamine stereoisomer with a reagent suitable for the cleavage of a sulfur-nitrogen bond, to afford an amine stereoisomer. It also provides novel intermediates useful in the method, and the use of certain of the intermediates in the preparation of sulfoxide and sulfinylamine stereoisomers.
摘要翻译： 本发明提供一种制备胺立体异构体的方法，其包括立体选择性还原亚磺酰亚胺，其在亚磺酰基上具有醇，硫醇或胺的残基，或使亚磺酰基上的亚硫酰亚胺立体异构体与醇的残基反应，硫醇 或具有亲核试剂来源的胺，得到亚磺酰胺立体异构体，然后使亚磺酰胺立体异构体与适合于硫 - 氮键切割的试剂接触，得到胺立体异构体。 它还提供了可用于该方法的新型中间体，以及某些中间体在制备亚砜和亚磺酰胺立体异构体中的用途。
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12.发明授权Methods of preparing didesmethylsibutramine and other sibutramine derivatives 有权二甲基西布曲明和其他西布曲明衍生物的制备方法公开(公告)号：US06894189B2
公开(公告)日：2005-05-17
申请号：US10643941
申请日：2003-08-20
IPC分类号： C07C209/60 , C07C211/29 , C07C313/06 , C07C209/62 , C07C211/17 , C07C251/06
CPC分类号： C07C209/60 , C07C313/06 , C07C2601/04 , C07C211/29
摘要： This invention encompasses novel methods of preparing sibutramine and sibutramine derivatives, and stereomerically pure sibutramine derivatives in particular. Examples of sibutramine derivatives include, but are not limited to, sibutramine metabolites such as desmethylsibutramine and didesmethylsibutramine. The invention further encompasses novel compounds useful in the synthesis of sibutramine derivatives.
摘要翻译： 本发明包括制备西布曲明和西布曲明衍生物的新方法，特别是立体异构纯的西布曲明衍生物。 西布曲明衍生物的实例包括但不限于西布曲明代谢物如脱甲基西布曲明和二甲基西布曲明。 本发明还包括可用于合成西布曲明衍生物的新化合物。
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公开(公告)号：US06610887B2
公开(公告)日：2003-08-26
申请号：US10120503
申请日：2002-04-12
IPC分类号： C07C20962
CPC分类号： C07C209/60 , C07C313/06 , C07C2601/04 , C07C211/29
摘要： This invention encompasses novel methods of preparing sibutramine and sibutramine derivatives, and stereomerically pure sibutramine derivatives in particular. Examples of sibutramine derivatives include, but are not limited to, sibutramine metabolites such as desmethylsibutramine and didesmethylsibutramine. The invention further encompasses novel compounds useful in the synthesis of sibutramine derivatives.
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公开(公告)号：US07332610B2
公开(公告)日：2008-02-19
申请号：US11514141
申请日：2006-09-01
IPC分类号： C07D291/04
CPC分类号： C07D291/04 , C07B2200/07 , C07C209/52 , C07C249/02 , C07C303/34 , C07C2601/04 , C07D453/04 , C07C307/02 , C07C211/29 , C07C251/16
摘要： This invention provides intermediates useful in a method of preparing amine stereoisomers. It also provides a method of preparing sulfoxide and sulfinylamine stereoisomers using certain of the intermediates.
摘要翻译： 本发明提供了可用于制备胺立体异构体的方法的中间体。 它还提供了使用某些中间体制备亚砜和亚磺酰胺立体异构体的方法。
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公开(公告)号：US07064214B2
公开(公告)日：2006-06-20
申请号：US10120541
申请日：2002-04-12
申请人： Chris Hugh Senanayake , Zhengxu Han , Dhileepkumar Krishnamurthy , Derek Pflum , Harold Scott Wilkinson
发明人： Chris Hugh Senanayake , Zhengxu Han , Dhileepkumar Krishnamurthy , Derek Pflum , Harold Scott Wilkinson
IPC分类号： C07D213/02 , C07D235/04
CPC分类号： C07D291/04 , C07B2200/07 , C07C303/36 , C07C313/04 , C07C315/00 , C07C317/04 , C07C2602/08 , C07D235/28 , C07D291/08 , C07D401/12 , C07C317/14 , C07C311/03
摘要： This invention encompasses novel methods of preparing sulfinamides and sulfoxides, particularly stereomerically pure sulfinamides and sulfoxides. The invention further encompasses novel compounds from which sulfinamides and sulfoxides can be prepared.
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16.发明授权Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives and intermediates therein 有权制备吡喃葡萄糖基取代的苄基苯衍生物及其中间体的方法公开(公告)号：US07772191B2
公开(公告)日：2010-08-10
申请号：US11416683
申请日：2006-05-03
申请人： Matthias Eckhardt , Frank Himmelsbach , Xiao-jun Wang , Wenjun Tang , Xiufeng Sun , Li Zhang , Dhileepkumar Krishnamurthy , Chris Hugh Senanayake , Zhengxu Han
发明人： Matthias Eckhardt , Frank Himmelsbach , Xiao-jun Wang , Wenjun Tang , Xiufeng Sun , Li Zhang , Dhileepkumar Krishnamurthy , Chris Hugh Senanayake , Zhengxu Han
IPC分类号： A61K31/341 , A61K31/351 , A61K31/7034 , A61K31/7048 , C07H7/04 , C07D309/12 , C07D307/20
CPC分类号： C07D407/12 , C07D309/10 , C07F1/02 , C07F3/02 , C07H15/04 , C07H15/203 , C07H19/01
摘要： The present invention relates to processes for preparing the compounds of general formula I, wherein the groups R1 and R3 are defined according to claim 1. Furthermore this inventions relates to intermediates obtained in these processes.
摘要翻译： 本发明涉及制备通式I化合物的方法，其中基团R1和R3根据权利要求1定义。此外，本发明涉及在这些方法中获得的中间体。
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公开(公告)号：US20080214870A1
公开(公告)日：2008-09-04
申请号：US12032727
申请日：2008-02-18
IPC分类号： C07C251/00
CPC分类号： C07D291/04 , C07B2200/07 , C07C209/52 , C07C249/02 , C07C303/34 , C07C2601/04 , C07D453/04 , C07C307/02 , C07C211/29 , C07C251/16
摘要： This invention provides intermediates useful in a method of preparing amine stereoisomers. It also provides a method of preparing sulfoxide and sulfinylamine stereoisomers using certain of the intermediates.
摘要翻译： 本发明提供了可用于制备胺立体异构体的方法的中间体。 它还提供了使用某些中间体制备亚砜和亚磺酰胺立体异构体的方法。
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公开(公告)号：US07256297B2
公开(公告)日：2007-08-14
申请号：US11340551
申请日：2006-01-27
申请人： Chris Hugh Senanayake , Zhengxu Han , Dhileepkumar Krishnamurthy , Derek Pflum , Harold Scott Wilkinson
发明人： Chris Hugh Senanayake , Zhengxu Han , Dhileepkumar Krishnamurthy , Derek Pflum , Harold Scott Wilkinson
IPC分类号： C07D291/04
CPC分类号： C07D291/04 , C07B2200/07 , C07C303/36 , C07C313/04 , C07C315/00 , C07C317/04 , C07C2602/08 , C07D235/28 , C07D291/08 , C07D401/12 , C07C317/14 , C07C311/03
摘要： This invention encompasses novel methods of preparing sulfinamides and sulfoxides, particularly stereomerically pure sulfinamides and sulfoxides. The invention further encompasses novel compounds from which sulfinamides and sulfoxides can be prepared.
摘要翻译： 本发明包括制备亚磺酰胺和亚砜，特别是立体异构纯的亚磺酰胺和亚砜的新方法。 本发明还包括可以制备亚磺酰胺和亚砜的新化合物。
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公开(公告)号：US20060287539A1
公开(公告)日：2006-12-21
申请号：US11514141
申请日：2006-09-01
IPC分类号： C07D207/30
CPC分类号： C07D291/04 , C07B2200/07 , C07C209/52 , C07C249/02 , C07C303/34 , C07C2601/04 , C07D453/04 , C07C307/02 , C07C211/29 , C07C251/16
摘要： This invention provides intermediates useful in a method of preparing amine stereoisomers. It also provides a method of preparing sulfoxide and sulfinylamine stereoisomers using certain of the intermediates.
摘要翻译： 本发明提供了可用于制备胺立体异构体的方法的中间体。 它还提供了使用某些中间体制备亚砜和亚磺酰胺立体异构体的方法。
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公开(公告)号：US20140135493A1
公开(公告)日：2014-05-15
申请号：US13921145
申请日：2011-12-15
申请人： Daniel Robert Fandrick , Zhi-Hui Lu , Diana Crimhilda Reeves , Jonathan Timothy Reeves , Chris Hugh Senanayake , Jinhua J. Song , Yongda Zhang
发明人： Daniel Robert Fandrick , Zhi-Hui Lu , Diana Crimhilda Reeves , Jonathan Timothy Reeves , Chris Hugh Senanayake , Jinhua J. Song , Yongda Zhang
IPC分类号： C07D413/10 , C07D213/64 , C07C271/48 , C07D265/10
CPC分类号： C07D413/10 , C07C271/48 , C07D213/64 , C07D265/10
摘要： Disclosed is a process for making diastereomeric compound of the formula (I): wherein m, n and R1 to R4 are as defined herein. The process of the invention provides the compound of formula (I) in high yield and substantially free of the corresponding diastereomers. The compounds of formula (I) prepared by the process of the invention are useful for making pharmaceutically active compounds such as 11-β-hydroxysteroid hydrogenase type 1 (11-β-HSD1) inhibitors.
摘要翻译： 公开了制备式（I）的非对映体化合物的方法：其中m，n和R 1至R 4如本文所定义。 本发明的方法以高产率提供式（I）化合物，基本上不含相应的非对映异构体。 通过本发明的方法制备的式（I）化合物可用于制备药学活性化合物，例如11-羟基类固醇类氢化酶1型（11-＆amp; -HSD1）抑制剂。
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