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公开(公告)号：US08242277B2
公开(公告)日：2012-08-14
申请号：US12518430
申请日：2007-12-10
申请人： Gary L. Cantrell , Dan P. Magparangalan , Frank W. Moser , Jian Bao , Christopher W. Grote , Peter X. Wang
发明人： Gary L. Cantrell , Dan P. Magparangalan , Frank W. Moser , Jian Bao , Christopher W. Grote , Peter X. Wang
IPC分类号： C07D217/02
CPC分类号： C07D217/20 , Y02P20/55
摘要： The present invention is directed to processes for the synthesis of morphinans. In particular, a process for the asymmetric reduction of an imine moiety in a 3,4-dihydroisoquinoline to produce a tetrahydroisoquinoline, followed by a Birch reduction to produce a hexahydroisoquinoline. In various embodiments, the 3,4-dihydroisoquinoline contains a phenol moiety protected with a labile protecting group. In other embodiments, the imine reduction reaction mixture contains silver tetrafluoroborate.
摘要翻译： 本发明涉及合成吗啡喃的方法。 特别地，涉及在3,4-二氢异喹啉中不对称还原亚胺部分以产生四氢异喹啉的方法，然后进行桦木还原以产生六氢异喹啉。 在各种实施方案中，3,4-二氢异喹啉含有用不稳定保护基团保护的苯酚部分。 在其它实施方案中，亚胺还原反应混合物含有四氟硼酸银。
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公开(公告)号：US20110071299A1
公开(公告)日：2011-03-24
申请号：US12889484
申请日：2010-09-24
IPC分类号： C07D217/16
CPC分类号： C07D217/20
摘要： The present invention provides an efficient process for the preparation of hexahydroisoquinolines from amides. In particular, the invention provides a good yielding, one-pot process for the synthesis of hexahydroisoquinolines.
摘要翻译： 本发明提供从酰胺制备六氢异喹啉的有效方法。 特别地，本发明提供了合成六氢异喹啉的良好产率的一锅法。
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公开(公告)号：US20100113788A1
公开(公告)日：2010-05-06
申请号：US12630171
申请日：2009-12-03
申请人： Christopher W. Grote , Peter X. Wang , Tao Jiang , Gary L. Cantrell , Frank W. Moser , Catherine E. Thomasson
发明人： Christopher W. Grote , Peter X. Wang , Tao Jiang , Gary L. Cantrell , Frank W. Moser , Catherine E. Thomasson
IPC分类号： C07D489/02
CPC分类号： C07D489/02 , Y02P20/55
摘要： The present invention is directed to the preparation of 6-keto morphinans.
摘要翻译： 本发明涉及6-酮吗啡喃的制备。
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4.发明授权公开(公告)号：US08232400B2
公开(公告)日：2012-07-31
申请号：US12482014
申请日：2009-06-10
IPC分类号： C07D217/02
CPC分类号： C07C235/34 , C07C231/02 , C07C309/77 , Y02P20/55
摘要： The present invention is directed to processes for the synthesis of morphinans. In particular, a process for coupling a carboxylic acid compound with an amine compound to form an amide product that can then be isolated or the crude amide product can be cyclized to form a 3,4-dihydroisoquinoline. In one embodiment, the carboxylic acid contains a phenol moiety protected with a labile protecting group. The protected phenol reduces reaction times, simplifies work-up of the product, and reduces the amount of cyclizing agent, POCl3 that is necessary to form the 3,4-dihydroisoquinoline.
摘要翻译： 本发明涉及合成吗啡喃的方法。 特别是一种使羧酸化合物与胺化合物偶联以形成酰胺产物的方法，然后可以将其分离，或者可将粗酰胺产物环化以形成3,4-二氢异喹啉。 在一个实施方案中，羧酸含有用不稳定保护基团保护的苯酚部分。 受保护的苯酚减少反应时间，简化了产品的后处理，并减少了形成3,4-二氢异喹啉所需的环化剂POCl 3的量。
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5.发明授权Process for the preparation of hexahydroisoquinolines from 1,2,3,4-tetrahydroisoquinolines 有权从1,2,3,4-四氢异喹啉制备六氢异喹啉的方法公开(公告)号：US08227611B2
公开(公告)日：2012-07-24
申请号：US12482036
申请日：2009-06-10
申请人： Gary L. Cantrell , Dan P. Magparangalan , Frank W. Moser , Jian Bao , Christopher W. Grote , Peter X. Wang
发明人： Gary L. Cantrell , Dan P. Magparangalan , Frank W. Moser , Jian Bao , Christopher W. Grote , Peter X. Wang
IPC分类号： C07D217/02
CPC分类号： C07D217/20 , Y02P20/55
摘要： The present invention is directed to processes for the synthesis of morphinans. In particular, a process for the asymmetric reduction of an imine moiety in a 3,4-dihydroisoquinoline to produce a tetrahydroisoquinoline, followed by a Birch reduction to produce a hexahydroisoquinoline. In various embodiments, the 3,4-dihydroisoquinoline contains a phenol moiety protected with a labile protecting group. In other embodiments, the imine reduction reaction mixture contains silver tetrafluoroborate.
摘要翻译： 本发明涉及合成吗啡喃的方法。 特别地，涉及在3,4-二氢异喹啉中不对称还原亚胺部分以产生四氢异喹啉的方法，然后进行桦木还原以产生六氢异喹啉。 在各种实施方案中，3,4-二氢异喹啉含有用不稳定保护基团保护的苯酚部分。 在其它实施方案中，亚胺还原反应混合物含有四氟硼酸银。
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6.发明授权Preparation of substituted morphinan-6-ones and salts and intermediates thereof 有权取代的吗啡喃-6-酮及其盐及其中间体的制备公开(公告)号：US08115002B2
公开(公告)日：2012-02-14
申请号：US12441397
申请日：2007-09-06
IPC分类号： C07D221/28
CPC分类号： C07D217/20
摘要： The present invention is directed to processes for the synthesis of morphinan-6-ones and salts, intermediates, and analogs thereof.
摘要翻译： 本发明涉及吗啡喃-6-酮及其盐，中间体和类似物的合成方法。
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公开(公告)号：US20100081818A1
公开(公告)日：2010-04-01
申请号：US12630192
申请日：2009-12-03
申请人： Christopher W. Grote , Peter X. Wang , Tao Jiang , Gary L. Cantrell , Frank W. Moser , Catherine E. Thomasson
发明人： Christopher W. Grote , Peter X. Wang , Tao Jiang , Gary L. Cantrell , Frank W. Moser , Catherine E. Thomasson
IPC分类号： C07D489/00
CPC分类号： C07D489/02 , Y02P20/55
摘要： The present invention is directed to the preparation of 6-hydroxy morphinans having formula (II) or N-alkylated 6-hydroxy morphinans having formula (III).
摘要翻译： 本发明涉及具有式（II）的6-羟基吗啡烷或具有式（III）的N-烷基化的6-羟基吗啡喃的制备。
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公开(公告)号：US20100063290A1
公开(公告)日：2010-03-11
申请号：US12518434
申请日：2007-12-10
IPC分类号： C07D217/00
CPC分类号： C07C235/34 , C07C231/02 , C07C309/77 , Y02P20/55
摘要： The present invention is directed to processes for the synthesis of morphinans. In particular, a process for coupling a carboxylic acid compound with an amine compound to form an amide product that can then be isolated or the crude amide product can be cyclized to form a 3,4-dihydroisoquinoline. In one embodiment, the carboxylic acid contains a phenol moiety protected with a labile protecting group. The protected phenol reduces reaction times, simplifies work-up of the product, and reduces the amount of cyclizing agent, POCl3 that is necessary to form the 3,4-dihydroisoquinoline.
摘要翻译： 本发明涉及合成吗啡喃的方法。 特别是一种使羧酸化合物与胺化合物偶联以形成酰胺产物的方法，然后可以将其分离，或者可将粗酰胺产物环化以形成3,4-二氢异喹啉。 在一个实施方案中，羧酸含有用不稳定保护基团保护的苯酚部分。 受保护的苯酚减少反应时间，简化了产品的后处理，并减少了形成3,4-二氢异喹啉所需的环化剂POCl 3的量。
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公开(公告)号：US20100022776A1
公开(公告)日：2010-01-28
申请号：US12518430
申请日：2007-12-10
申请人： Gary L. Cantrell , Dan P. Magparangalan , Frank W. Moser , Jian Bao , Christopher W. Grote , Peter X. Wang
发明人： Gary L. Cantrell , Dan P. Magparangalan , Frank W. Moser , Jian Bao , Christopher W. Grote , Peter X. Wang
IPC分类号： C07D217/02
CPC分类号： C07D217/20 , Y02P20/55
摘要： The present invention is directed to processes for the synthesis of morphinans. In particular, a process for the asymmetric reduction of an imine moiety in a 3,4-dihydroisoquinoline to produce a tetrahydroisoquinoline, followed by a Birch reduction to produce a hexahydroisoquinoline. In various embodiments, the 3,4-dihydroisoquinoline contains a phenol moiety protected with a labile protecting group. In other embodiments, the imine reduction reaction mixture contains silver tetrafluoroborate.
摘要翻译： 本发明涉及合成吗啡喃的方法。 特别地，涉及在3,4-二氢异喹啉中不对称还原亚胺部分以产生四氢异喹啉的方法，然后进行桦木还原以产生六氢异喹啉。 在各种实施方案中，3,4-二氢异喹啉含有用不稳定保护基团保护的苯酚部分。 在其它实施方案中，亚胺还原反应混合物含有四氟硼酸银。
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公开(公告)号：US20130137874A1
公开(公告)日：2013-05-30
申请号：US13749805
申请日：2013-01-25
IPC分类号： C07D217/20 , C07D217/16
CPC分类号： C07D217/20
摘要： The present invention provides an efficient process for the preparation of hexahydroisoquinolines from amides. In particular, the invention provides a good yielding, one-pot process for the synthesis of hexahydroisoquinolines.
摘要翻译： 本发明提供从酰胺制备六氢异喹啉的有效方法。 特别地，本发明提供了合成六氢异喹啉的良好产率的一锅法。
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