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公开(公告)号：US08283487B2
公开(公告)日：2012-10-09
申请号：US12626682
申请日：2009-11-26
IPC分类号： C07C271/16
CPC分类号： C07C269/04 , C07C201/12 , C07C269/08 , C07C2601/14 , C07C205/43 , C07C271/22
摘要： Gabapentin enacarbil was prepared and purified from intermediates such as 1-haloalkyl carbamate or carbonate and diacid acetal skeleton. For example, a 1-haloalkyl carbonate or carbamate was prepared by combining a C1 to C10 alcohol or C1 to C10 primary amine, a solvent selected from the group consisting of: acetonitrile, C3 to C7 ketone, C5 to C10 ether, C2 to C7 ester, C5 to C10 hydrocarbon and a combination thereof; a 1-haloalkyl haloformate of the following formula: wherein each X is independently selected from Br, I, or Cl; R1 is alkyl or H; and a C6 to C21 tertiary amine.
摘要翻译： 从中间体如氨基甲酸1-卤代烷基酯或碳酸酯和二酸缩醛骨架制备和纯化加巴喷丁恩卡巴尔。 例如，通过将C1至C10醇或C1至C10伯胺，选自乙腈，C3至C7酮，C5至C10醚，C2至C7的溶剂组合，制备碳酸1-卤代烷基酯或氨基甲酸酯 酯，C5至C10烃及其组合; 下式的1-卤代烷基卤代甲酸酯：其中每个X独立地选自Br，I或Cl; R1是烷基或H; 和C 6至C 21叔胺。
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公开(公告)号：US20100160665A1
公开(公告)日：2010-06-24
申请号：US12626682
申请日：2009-11-26
IPC分类号： C07C269/06 , C07C269/04 , C07C68/00
CPC分类号： C07C269/04 , C07C201/12 , C07C269/08 , C07C2601/14 , C07C205/43 , C07C271/22
摘要： Gabapentin enacarbil was prepared and purified from intermediates such as 1-haloalkyl carbamate or carbonate and diacid acetal skeleton. For example, a 1-haloalkyl carbonate or carbamate was prepared by combining a C1 to C10 alcohol or C1 to C10 primary amine, a solvent selected from the group consisting of: acetonitrile, C3 to C7 ketone, C5 to C10 ether, C2 to C7 ester, C5 to C10 hydrocarbon and a combination thereof; a 1-haloalkyl haloformate of the following formula: wherein each X is independently selected from Br, I, or Cl; R1 is alkyl or H; and a C6 to C21 tertiary amine.
摘要翻译： 从中间体如氨基甲酸1-卤代烷基酯或碳酸酯和二酸缩醛骨架制备和纯化加巴喷丁恩卡巴尔。 例如，通过将C1至C10醇或C1至C10伯胺，选自乙腈，C3至C7酮，C5至C10醚，C2至C7的溶剂组合，制备碳酸1-卤代烷基酯或氨基甲酸酯 酯，C5至C10烃及其组合; 下式的1-卤代烷基卤代甲酸酯：其中每个X独立地选自Br，I或Cl; R1是烷基或H; 和C 6至C 21叔胺。
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公开(公告)号：US08063250B2
公开(公告)日：2011-11-22
申请号：US12313961
申请日：2008-11-26
IPC分类号： C07C213/00
CPC分类号： C07C215/64 , C07C57/15 , C07C2601/14
摘要： Provided are crystalline forms of O-desmethylvenlafaxine fumarate, methods for their preparation, and pharmaceutical compositions thereof.
摘要翻译： 提供了O-去甲基文拉法辛富马酸盐的结晶形式，其制备方法及其药物组合物。
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44.发明授权Purification of rosuvatatin intermediate by thin film evaporation and chemical method 失效通过薄膜蒸发和化学方法纯化罗素伐他汀中间体公开(公告)号：US07884226B2
公开(公告)日：2011-02-08
申请号：US12218403
申请日：2008-07-14
申请人： Tamar Nidam , Omer Malachi , Irena Veinberg , Valerie Niddam-Hildesheim , Vinod Kumar Kansal , Harish Ranjan , Appu Ekambaram Ponnuswamy , Sunil Rokad , Surat Kiran , Debashish Das
发明人： Tamar Nidam , Omer Malachi , Irena Veinberg , Valerie Niddam-Hildesheim , Vinod Kumar Kansal , Harish Ranjan , Appu Ekambaram Ponnuswamy , Sunil Rokad , Surat Kiran , Debashish Das
IPC分类号： C07F9/02
CPC分类号： C07C69/675 , C07B2200/07 , C07D239/42 , C07F9/4006 , C07F9/4053
摘要： Provided are processes for the purification of a pure rosuvastatin intermediate by thin film evaporation and chemical method, and conversion of the intermediate to rosuvastatin or salts thereof.
摘要翻译： 提供了通过薄膜蒸发和化学方法纯化瑞舒伐他汀中间体的方法，以及将中间体转化为瑞舒伐他汀或其盐。
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公开(公告)号：US20090069601A1
公开(公告)日：2009-03-12
申请号：US12001070
申请日：2007-12-06
IPC分类号： C07C209/00
CPC分类号： C07C215/64 , C07C213/02 , C07C213/08 , C07C235/34 , C07C2601/14
摘要： The present invention describes processes for the preparation of O-desmethylvenlafaxine and tridesmethylvenlafaxine, which may be used as an intermediate in preparing O-desmethylvenlafaxine.
摘要翻译： 本发明描述了用于制备O-去甲基文拉法辛和三甲基文拉法辛的方法，其可以用作制备O-去甲基文拉法辛的中间体。
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公开(公告)号：US20070021417A1
公开(公告)日：2007-01-25
申请号：US11361457
申请日：2006-02-23
申请人： Serguei Fine , Tamar Nidam , Viviana Braude
发明人： Serguei Fine , Tamar Nidam , Viviana Braude
IPC分类号： A61K31/5377 , C07D413/02
CPC分类号： C07D263/20 , A61K31/5377 , C07D413/10 , C07D413/14
摘要： The present invention provides improved methods of converting R-N-(4-morpholiyl-3-fluorophenyl)-2-oxo-5-oxazolidinyl-methyl azide (III) to the intermediate S-N-(4-morpholinyl-3-fluorophenyl)-2-oxo-5-oxazolidinyl-methyl amine (II) that involve the production of fewer by-products than previous methods. The amine (II) may then be converted into linezolid (I) of high chemical purity with respect to the inactive R-enantiomer and bis-linezolid (IV), and is in high yield, without the need for tedious, complicated purification steps, such as chromatography.
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公开(公告)号：US07622588B2
公开(公告)日：2009-11-24
申请号：US11083485
申请日：2005-03-18
申请人： Claude Singer , Anita Liberman , Irena Veinberg , Nina Finkelstein , Tamar Nidam
发明人： Claude Singer , Anita Liberman , Irena Veinberg , Nina Finkelstein , Tamar Nidam
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The present invention provides a method for preparing a substantially pure lansoprazole containing less than about 0.2% (wt/wt) impurities including sulfone/sulfide derivatives. The present invention also provides a process for recrystallizing lansoprazole to obtain a lansoprazole containing less than about 0.1% (wt/wt) water.
摘要翻译： 本发明提供一种制备基本上纯的兰索拉唑的方法，该兰索拉唑含有少于约0.2％（重量/重量）的杂质，包括砜/硫化物衍生物。 本发明还提供了使兰索拉唑重结晶以获得含有少于约0.1％（wt / wt）水的兰索拉唑的方法。
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48.发明申请Processes for optical resolution of 1-phenyl-1,2,3,4-tetrahydroisoquinoline 审中-公开1-苯基-1,2,3,4-四氢异喹啉的光学拆分方法公开(公告)号：US20080091023A1
公开(公告)日：2008-04-17
申请号：US11890289
申请日：2007-08-03
申请人： Nurit Perlman , Tamar Nidam
发明人： Nurit Perlman , Tamar Nidam
IPC分类号： C07D217/02 , C07D401/14
CPC分类号： C07D453/02 , C07D217/02
摘要： Optically pure 1(S)-phenyl-1,2,3,4-tetrahydroisoquinoline tartrate is prepared. The 1(S)-phenyl-1,2,3,4-tetrahydroisoquinoline tartrate is particularly useful for preparing solifenacin succinate.
摘要翻译： 制备光学纯的1（S） - 苯基-1,2,3,4-四氢异喹啉酒石酸盐。 1（S） - 苯基-1,2,3,4-四氢异喹啉酒石酸盐特别适用于制备琥珀酸索非那新。
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49.发明申请Isolated bis-linezolid, preparation thereof, and its use as a reference standard 审中-公开分离的双利奈唑胺，其制备及其用途作为参考标准公开(公告)号：US20060252932A1
公开(公告)日：2006-11-09
申请号：US11361509
申请日：2006-02-24
申请人： Tamar Nidam , Viviana Braude , Miri Adler , Revital Ramaty
发明人： Tamar Nidam , Viviana Braude , Miri Adler , Revital Ramaty
IPC分类号： C07D413/14
CPC分类号： C07D263/20 , A61K31/5377 , C07D413/10 , C07D413/14
摘要： The present invention provides an isolated linezolid (1) impurity, bis-linezolid (4), preparation thereof and its use as a reference standard.
摘要翻译： 本发明提供了一种分离的利奈唑胺（1）杂质，双利奈唑胺（4），其制备方法及其用途作为参考标准。
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公开(公告)号：US20050165061A1
公开(公告)日：2005-07-28
申请号：US11084269
申请日：2005-03-18
申请人： Claude Singer , Anita Liberman , Irena Veinberg , Nina Finkelstein , Tamar Nidam
发明人： Claude Singer , Anita Liberman , Irena Veinberg , Nina Finkelstein , Tamar Nidam
IPC分类号： C07D401/12 , A61K31/4439 , C07D43/02
CPC分类号： C07D401/12
摘要： The present invention provides a method for preparing a substantially pure lansoprazole containing less than about 0.2% (wt/wt) impurities including sulfone/sulfide derivatives. The present invention also provides a process for recrystallizing lansoprazole to obtain a lansoprazole containing less than about 0.1% (wt/wt) water.
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