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1.发明授权Process for the preparation of 7-amino syn 3,5-dihydroxy heptanoic acid derivatives, intermediates thereof and methods for their preparation 失效7-氨基顺式3,5-二羟基庚酸衍生物的制备方法，其中间体及其制备方法公开(公告)号：US07504532B2
公开(公告)日：2009-03-17
申请号：US11941347
申请日：2007-11-16
申请人： Reinhold Öhrlein , Gabriele Baisch , Hans Jörg Kirner , Stephan Burkhardt , Martin Studer , Frank Bienewald
发明人： Reinhold Öhrlein , Gabriele Baisch , Hans Jörg Kirner , Stephan Burkhardt , Martin Studer , Frank Bienewald
IPC分类号： C07C229/00 , C07C291/00 , C07C59/10
CPC分类号： C07C69/67 , C07C69/716 , C07C69/732 , C07C69/738 , C07C227/32 , C07C229/22 , C07C235/06 , C07C235/74 , C12P7/62 , Y02P20/55
摘要： Synthesis methods for the preparation of intermediates which are suitable for the preparation of statin derivatives, and especially to synthesis methods for the intermediate of formula (VI) wherein Ra′ and Rc′ are each independently of the other hydrogen or hydroxy-protecting group, or together are a bridging hydroxy-protecting group; and Rb is a carboxy-protecting group.
摘要翻译： 用于制备适于制备他汀类衍生物的中间体的合成方法，特别是其中R a'和R c'各自独立于其它氢或羟基保护基的式（Ⅵ）中间体的合成方法，或 一起是桥接羟基保护基团; 并且Rb是羧基保护基。
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2.发明授权Process for preparation of 7-amino syn 3,5-dihydroxy heptanoic acid derivatives, intermediates thereof and methods for their preparation 失效7-氨基顺式3,5-二羟基庚酸衍生物的制备方法，其中间体及其制备方法公开(公告)号：US07317123B2
公开(公告)日：2008-01-08
申请号：US10482946
申请日：2002-07-02
申请人： Reinhold Öhrlein , Gabriele Baisch , Hans Jörg Kirner , Stephan Burkhardt , Martin Studer , Frank Bienewald
发明人： Reinhold Öhrlein , Gabriele Baisch , Hans Jörg Kirner , Stephan Burkhardt , Martin Studer , Frank Bienewald
IPC分类号： C07C229/00 , C07C233/00
CPC分类号： C07C69/67 , C07C69/716 , C07C69/732 , C07C69/738 , C07C227/32 , C07C229/22 , C07C235/06 , C07C235/74 , C12P7/62 , Y02P20/55
摘要： The invention relates to novel synthesis methods for the preparation of the intermediates, which are suitable for the preparation of statin derivatives, especially to novel synthesis methods of the intermediate of formula VI wherein Ra′ and Rc′ are each independently of the other hydrogen or a hydroxy-protecting group or together are a bridging hydroxy-protecting group, and Rb is a carboxy-protecting group, which methods are carried out by conversion of the intermediate of formula XVI wherein Ra′ and Rc′ are each independently of the other hydrogen or a hydroxy-protecting group, R* and R** are each independently of the other hydrogen or an amide-protecting group, and Rb is a carboxy-protecting group; which methods proceed to further new intermediates and methods for their preparation
摘要翻译： 本发明涉及用于制备适于制备他汀类衍生物的中间体的新型合成方法，特别涉及式VI中间体的新型合成方法，其中R a'和R“ > C独立地是氢或羟基保护基，或者一起是桥接羟基保护基，R b是羧基保护基，这些方法是 通过式XVI的中间体的转化而进行，其中R a a和R c'各自独立地是氢或羟基保护基，R *和R **各自独立地为另一个氢或酰胺保护基团，并且R b为羧基保护基团; 哪些方法进行进一步的新中间体及其制备方法
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3.发明授权Process for the preparation of 7-amino syn 3,5-dihydroxy heptanoic acid derivatives via 6-cyano syn 3,5-dihydroxy hexanoic acid derivatives 失效通过6-氰基顺式3,5-二羟基己酸衍生物制备7-氨基顺式3,5-二羟基庚酸衍生物的方法公开(公告)号：US07692034B2
公开(公告)日：2010-04-06
申请号：US11657808
申请日：2007-01-24
申请人： Reinhold Öhrlein , Gabriele Baisch , Hans Jürg Kirner , Frank Bienewald , Stephan Burkhardt , Martin Studer
发明人： Reinhold Öhrlein , Gabriele Baisch , Hans Jürg Kirner , Frank Bienewald , Stephan Burkhardt , Martin Studer
IPC分类号： C07C229/00
CPC分类号： C07C69/67 , C07C69/716 , C07C69/732 , C07C69/738 , C07C227/32 , C07C229/22 , C07C235/06 , C07C235/74 , C12P7/62 , Y02P20/55
摘要： The invention relates to novel synthesis methods for the preparation of the intermediates, which are suitable for the preparation of statin derivatives, especially to novel synthesis methods of the intermediate of formula VI wherein Ra and Rc are each independently of the other hydrogen or a hydroxy-protecting group or together are a bridging hydroxy-protecting group, and Rb is a carboxy-protecting group, which methods are carried out by conversion of the intermediate of formula XIX wherein Ra and Rc are each independently of the other hydrogen or a hydroxy-protecting group, and Rb is a carboxy-protective group.
摘要翻译： 本发明涉及适用于制备他汀类衍生物的中间体的新型合成方法，特别是式VI中间体的新合成方法，其中R a和R c各自独立地为氢或羟基 - 保护基或一起是桥接羟基保护基，Rb是羧基保护基，该方法通过式XIX的中间体转化而进行，其中R a和R c各自独立地为氢或羟基保护基 基团，Rb是羧基保护基。
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4.发明授权Process for the preparation of 7-amino syn 3,5-dihydroxy heptanoic acid derivatives via 6-cyano syn 3,5-dihydroxy hexanoic acid derivatives 失效通过6-氰基顺式3,5-二羟基己酸衍生物制备7-氨基顺式3,5-二羟基庚酸衍生物的方法公开(公告)号：US07199261B2
公开(公告)日：2007-04-03
申请号：US10481704
申请日：2002-07-02
申请人： Reinhold Öhrlein , Gabriele Baisch , Hans Jürg Kirner , Frank Bienewald , Stephan Burkhardt , Martin Studer
发明人： Reinhold Öhrlein , Gabriele Baisch , Hans Jürg Kirner , Frank Bienewald , Stephan Burkhardt , Martin Studer
IPC分类号： C07C229/00
CPC分类号： C07C69/67 , C07C69/716 , C07C69/732 , C07C69/738 , C07C227/32 , C07C229/22 , C07C235/06 , C07C235/74 , C12P7/62 , Y02P20/55
摘要： The invention relates to novel synthesis methods for the preparation of the intermediates, which are suitable for the preparation of statin derivatives, especially to novel synthesis methods of the intermediate of formula VI wherein Ra and Rc are each independently of the other hydrogen or a hydroxy-protecting group or together are a bridging hydroxy-protecting group, and Rb is a carboxy-protecting group, which methods are carried out by conversion of the intermediate of formula XIX wherein Ra and Rc are each independently of the other hydrogen or a hydroxy-protecting group, and Rb is a carboxy-protective group
摘要翻译： 本发明涉及用于制备适于制备他汀类衍生物的中间体的新型合成方法，特别涉及式VI中间体的新型合成方法，其中R a a， C 1各自独立地为另一个氢或羟基保护基团，或者一起是桥接羟基保护基团，并且R b是羧基保护基团，该方法进行 通过其中R a a和R c C分别独立于另一个氢或羟基保护基的式XIX的中间体的转化，并且R b' SUB>是羧基保护基
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5.发明授权Process for the preparation of intermediates useful in the synthesis of statin derivatives especially 7-amino-3.5-dihydroxyhepanoic acid derivatives and intermediates thereof 有权制备可用于合成他汀类衍生物，特别是7-氨基-3,5-二羟基庚酸衍生物的中间体的方法及其中间体公开(公告)号：US07855302B2
公开(公告)日：2010-12-21
申请号：US12220390
申请日：2008-07-24
IPC分类号： C07C69/66 , C07C259/06 , C07C69/22
CPC分类号： C07C235/74 , C07C69/67 , C07C69/716 , C07C69/732 , C07C69/738 , C07C227/32 , C07C229/22 , C07C235/06 , C12P7/62 , Y02P20/55
摘要： The invention relates to novel synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I wherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or —N(CH3)OCH3, Ra is a hydroxy-protecting group and Rb is a carboxy-protecting group, and, as well as to the compound of formula I, to further new intermediates and methods for their preparation by Friedel-Crafts acylation.
摘要翻译： 本发明涉及用于制备他汀类衍生物的新型合成方法，该方法通过式I的关键中间体进行，其中X是卤素，酰氧基，活化的烃氧基，活化的烃基硫基或-N（CH 3）OCH 3，R a是羟基 保护基团，Rb是羧基保护基团，以及式I化合物，用于通过Friedel-Crafts酰化进一步制备新的中间体及其制备方法。
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6.发明授权Process for the preparation of intermediates useful in the synthesis of statin derivatives especially 7-amino 3,5-dihydroxy heptanoic acid derivatives, and intermediates thereof 有权制备可用于合成他汀类衍生物，特别是7-氨基3,5-二羟基庚酸衍生物的中间体的方法及其中间体公开(公告)号：US07420078B2
公开(公告)日：2008-09-02
申请号：US10482463
申请日：2002-07-02
IPC分类号： C07C69/66 , C07C259/06 , C07C69/22
CPC分类号： C07C235/74 , C07C69/67 , C07C69/716 , C07C69/732 , C07C69/738 , C07C227/32 , C07C229/22 , C07C235/06 , C12P7/62 , Y02P20/55
摘要： The invention relates to synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I wherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or N(CH3)OCH3, Ra is a hydroxy-protecting group, and Rb is a carboxy-protecting group, and, as well as to the compound of formula I, to further intermediates and methods for their preparation by Friedel-Crafts acylation.
摘要翻译： 本发明涉及用于制备他汀类衍生物的合成方法，该方法通过式I的关键中间体进行，其中X是卤素，酰氧基，活化的烃氧基，活化的烃基硫基或N（CH 3） OCH 3，R a是羟基保护基，R b是羧基保护基，以及对于 式I化合物，其进一步的中间体及其通过Friedel-Crafts酰化制备的方法。
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7.发明授权Process for the preparation of intermediates useful in the synthesis of statin derivatives 有权制备可用于合成他汀类衍生物的中间体的方法公开(公告)号：US08026383B2
公开(公告)日：2011-09-27
申请号：US12939401
申请日：2010-11-04
IPC分类号： C07C69/66 , C07C259/06 , C07C69/22
CPC分类号： C07C235/74 , C07C69/67 , C07C69/716 , C07C69/732 , C07C69/738 , C07C227/32 , C07C229/22 , C07C235/06 , C12P7/62 , Y02P20/55
摘要： The invention relates to novel synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I wherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or —N(CH3)OCH3, Ra is a hydroxy-protecting group and Rb is a carboxy-protecting group, and, as well as to the compound of formula I, to further new intermediates and methods for their preparation by Friedel-Crafts acylation.
摘要翻译： 本发明涉及用于制备他汀类衍生物的新型合成方法，该方法通过式I的关键中间体进行，其中X是卤素，酰氧基，活化的烃氧基，活化的烃基硫基或-N（CH 3）OCH 3，R a是羟基 保护基团，Rb是羧基保护基团，以及式I化合物，用于通过Friedel-Crafts酰化进一步制备新的中间体及其制备方法。
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8.发明申请PROCESS FOR THE PREPARATION OF INTERMEDIATES USEFUL IN THE SYNTHESIS OF STATIN DERIVATIVES 有权制备苯丙氨酸衍生物合成中的有用途的方法公开(公告)号：US20110046411A1
公开(公告)日：2011-02-24
申请号：US12939401
申请日：2010-11-04
IPC分类号： C07C227/00 , C07C69/67
CPC分类号： C07C235/74 , C07C69/67 , C07C69/716 , C07C69/732 , C07C69/738 , C07C227/32 , C07C229/22 , C07C235/06 , C12P7/62 , Y02P20/55
摘要： The invention relates to novel synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I wherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or —N(CH3)OCH3, Ra is a hydroxy-protecting group and Rb is a carboxy-protecting group, and, as well as to the compound of formula I, to further new intermediates and methods for their preparation by Friedel-Crafts acylation.
摘要翻译： 本发明涉及用于制备他汀类衍生物的新型合成方法，该方法通过式I的关键中间体进行，其中X是卤素，酰氧基，活化的烃氧基，活化的烃基硫基或-N（CH 3）OCH 3，R a是羟基 保护基团，Rb是羧基保护基团，以及式I化合物，用于通过Friedel-Crafts酰化进一步制备新的中间体及其制备方法。
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9.发明申请Process for the preparation of 7-amino syn 3,5-dihydroxy heptanoic acid derivatives via 6-cyano syn 3,5-dihydroxy hexanoic acid derivatives 失效通过6-氰基顺式3,5-二羟基己酸衍生物制备7-氨基顺式3,5-二羟基庚酸衍生物的方法公开(公告)号：US20050033086A1
公开(公告)日：2005-02-10
申请号：US10481704
申请日：2002-07-02
申请人： Reinhold Ohrlein , Gabriele Baisch , Hans Kirner , Frank Bienewald , Stephan Burkhardt , Martin Studer
发明人： Reinhold Ohrlein , Gabriele Baisch , Hans Kirner , Frank Bienewald , Stephan Burkhardt , Martin Studer
IPC分类号： C07C67/307 , C07B53/00 , C07B61/00 , C07C67/30 , C07C67/31 , C07C69/67 , C07C69/675 , C07C69/708 , C07C69/716 , C07C69/732 , C07C69/738 , C07C227/06 , C07C227/16 , C07C227/32 , C07C229/22 , C07C231/02 , C07C235/06 , C07C235/74 , C07C247/12 , C07C253/30 , C07D207/34 , C12P7/62
CPC分类号： C07C69/67 , C07C69/716 , C07C69/732 , C07C69/738 , C07C227/32 , C07C229/22 , C07C235/06 , C07C235/74 , C12P7/62 , Y02P20/55
摘要： The invention relates to novel synthesis methods for the preparation of the intermediates, which are suitable for the preparation of statin derivatives, especially to novel synthesis methods of the intermediate of formula VI wherein Ra and Rc are each independently of the other hydrogen or a hydroxy-protecting group or together are a bridging hydroxy-protecting group, and Rb is a carboxy-protecting group, which methods are carried out by conversion of the intermediate of formula XIX wherein Ra and Rc are each independently of the other hydrogen or a hydroxy-protecting group, and Rb is a carboxy-protective group.
摘要翻译： 本发明涉及适用于制备他汀类衍生物的中间体的新型合成方法，特别是式VI中间体的新合成方法，其中R a和R c各自独立地为氢或羟基 - 保护基或一起是桥接羟基保护基，Rb是羧基保护基，该方法通过式XIX的中间体转化而进行，其中R a和R c各自独立地为氢或羟基保护基 基团，Rb是羧基保护基。
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10.发明申请PROCESS FOR THE PREPARATION OF 7-AMINO SYN 3,5-DIHYDROXY HEPTANOIC ACID DERIVATIVES, INTERMEDIATES THEREOF AND METHODS FOR THEIR PREPARATION 失效制备7-氨基-3,5-二羟基丙酸衍生物的方法，其中间体及其制备方法公开(公告)号：US20080125601A1
公开(公告)日：2008-05-29
申请号：US11941347
申请日：2007-11-16
申请人： Reinhold Ohrlein , Gabriele Baisch , Hans Jorg Kirner , Stephan Burkhardt , Martin Studer , Frank Bienewald
发明人： Reinhold Ohrlein , Gabriele Baisch , Hans Jorg Kirner , Stephan Burkhardt , Martin Studer , Frank Bienewald
IPC分类号： C07C233/08
CPC分类号： C07C69/67 , C07C69/716 , C07C69/732 , C07C69/738 , C07C227/32 , C07C229/22 , C07C235/06 , C07C235/74 , C12P7/62 , Y02P20/55
摘要： Synthesis methods for the preparation of intermediates which are suitable for the preparation of statin derivatives, and especially to synthesis methods for the intermediate of formula (VI) wherein Ra′ and Rc′ are each independently of the other hydrogen or hydroxy-protecting group, or together are a bridging hydroxy-protecting group; and Rb is a carboxy-protecting group.
摘要翻译： 制备适于制备他汀类衍生物的中间体的合成方法，特别是其中R a和R c的中间体的合成方法 各自独立地为氢或羟基保护基，或者一起是桥羟基保护基; R b是羧基保护基。
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