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1. 发明申请

WO2008073389A2 PREPARATION OF HEXAHYDROISOQUINOLINES FROM DIHYDROISOQUINOLINES 审中-公开
标题翻译：从二氢异喹啉制备六氢异喹啉
公开(公告)号：WO2008073389A2
公开(公告)日：2008-06-19
申请号：PCT/US2007025262
申请日：2007-12-10
申请人： MALLINCKRODT INC , WANG PETER X , CANTRELL GARY L , MAGPARANGALAN DAN P , MOSER FRANK W , BAO JIAN , GROTE CHRISTOPHER W
发明人： WANG PETER X , CANTRELL GARY L , MAGPARANGALAN DAN P , MOSER FRANK W , BAO JIAN , GROTE CHRISTOPHER W
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。具体地说，是一种不对称还原3,4-二氢异喹啉中的亚胺部分以产生四氢异喹啉，接着进行Birch还原以产生六氢异喹啉的方法。在各种实施方案中，3,4-二氢异喹啉含有用不稳定保护基保护的酚部分。在其他实施方案中，亚胺还原反应混合物含有四氟硼酸银。

2. 发明申请

WO2011038169A3 OXALAMIDE DERIVATIVE AS UMAMI FLAVOURING AGENT 审中-公开
标题翻译：氧酰胺衍生物作为UMAMI FLAVORING AGENT
公开(公告)号：WO2011038169A3
公开(公告)日：2011-05-19
申请号：PCT/US2010050093
申请日：2010-09-24
申请人： MALLINCKRODT INC , GROTE CHRISTOPHER W , MOSER FRANK W , WANG PETER X , CANTRELL GARY L , BERBERICH DAVID W
发明人： GROTE CHRISTOPHER W , MOSER FRANK W , WANG PETER X , CANTRELL GARY L , BERBERICH DAVID W
IPC分类号： C07D217/20
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：本发明提供了一种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。

3. 发明申请

WO2008073390A3 PREPARATION OF 3,4-DIHYDROISOQUINOLINES FROM AN ACID AND AN AMINE 审中-公开
标题翻译：从酸和胺制备3,4-二氢异喹啉
公开(公告)号：WO2008073390A3
公开(公告)日：2008-10-09
申请号：PCT/US2007025263
申请日：2007-12-10
申请人： MALLINCKRODT INC , GROTE CHRISTOPHER W , WANG PETER X , MOSER FRANK W , CANTRELL GARY L
发明人： GROTE CHRISTOPHER W , WANG PETER X , MOSER FRANK W , CANTRELL GARY L
IPC分类号： C07C235/34 , C07D217/20
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, POCl 3 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。具体地讲，一种将羧酸化合物与胺化合物偶联形成酰胺产物然后可以分离的方法或粗酰胺产物可以环化形成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保护的酚部分。被保护的苯酚减少了反应时间，简化了产物的后处理，并且减少了形成3,4-二氢异喹啉所需的环化剂POCl 3的量。

4. 发明申请

WO2010028004A2 SUBSTITUTED BERBINES AND PROCESSES FOR THEIR SYNTHESIS 审中-公开
标题翻译：取代的BERBINES及其合成方法
公开(公告)号：WO2010028004A2
公开(公告)日：2010-03-11
申请号：PCT/US2009055676
申请日：2009-09-02
申请人： MALLINCKRODT INC , WANG PETER X , MOSER FRANK W , CANTRELL GARY L , GROTE CHRISTOPHER W
发明人： WANG PETER X , MOSER FRANK W , CANTRELL GARY L , GROTE CHRISTOPHER W
IPC分类号： C07D217/02 , C07D455/03
CPC分类号： C07D455/03 , B01J31/2295 , B01J2231/643 , B01J2531/821 , C07D217/20
摘要： The present invention provides processes for the synthesis of substituted berbine compounds. Also provided are intermediates used in the synthesis of substituted berbine compounds.
摘要翻译：本发明提供了合成取代的铍化合物的方法。还提供了用于合成取代的伯贝宁化合物的中间体。

5. 发明申请

WO2008109156A2 PROCESS FOR THE PREPARATION OF QUATERNARY N-ALKYL MORPHINAN ALKALOID SALTS 审中-公开
标题翻译：制备季铵化N-烷基吗啡烷烷醇盐的方法
公开(公告)号：WO2008109156A2
公开(公告)日：2008-09-12
申请号：PCT/US2008003070
申请日：2008-03-06
申请人： MALLINCKRODT INC , CANTRELL GARY L , WANG PETER X , HALVACHS ROBERT E , ROESCH KEVIN R , BUEHLER HENRY J , HAAR JOSEPH P
发明人： WANG PETER X , HALVACHS ROBERT E , ROESCH KEVIN R , BUEHLER HENRY J , HAAR JOSEPH P
CPC分类号： C07D489/08 , C07D489/02 , C07D489/04 , Y02P20/582
摘要： An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.
摘要翻译：用于叔吗啡喃生物碱碱的N-烷基化以形成相应的季铵盐型吗啡喃生物碱衍生物的改进方法。

6. 发明申请

WO2010039209A3 PROCESSES FOR THE ALKYLATION OF SECONDARY AMINE GROUPS OF MORPHINAN DERIVATIVES 审中-公开
标题翻译：二氢卟吩衍生物亚胺基团的制备方法
公开(公告)号：WO2010039209A3
公开(公告)日：2010-09-16
申请号：PCT/US2009005356
申请日：2009-09-29
申请人： MALLINCKRODT INC , WANG PETER X , JIANG TAO , BERBERICH DAVID W
发明人： WANG PETER X , JIANG TAO , BERBERICH DAVID W
IPC分类号： C07D489/12
CPC分类号： C07D489/12
摘要： The invention provides processes for the preparation of morphinans having a tertiary amine. In particular, the present invention provides processes for the formation of tertiary amine alkaloids by direct N-alkylation of secondary amine alkaloids, the processes co-mediated by an alkylating agent and a protic solvent or a mixture of a protic solvent and an aprotic solvent.
摘要翻译：本发明提供了制备具有叔胺的吗啡喃的方法。特别地，本发明提供了通过仲胺生物碱的直接N-烷基化形成叔胺生物碱的方法，该方法由烷基化剂和质子溶剂或质子溶剂和非质子溶剂的混合物共同介导。

7. 发明专利

JP2011057703A Preparation of amide from acid and amine for intermediate in synthesis of morphinan 有权
标题翻译：用于中和合成麦芽糖的酸和胺的酰胺的制备
公开(公告)号：JP2011057703A
公开(公告)日：2011-03-24
申请号：JP2010275152
申请日：2010-12-09
申请人： Mallinckrodt Inc , マリンクロットインコーポレイテッド
发明人： GROTE CHRISTOPHER W , WANG PETER X , MOSER FRANK W , CANTRELL GARY L
IPC分类号： C07C231/02 , C07C231/12 , C07C233/22 , C07C303/28 , C07C309/66
CPC分类号： C07C235/34 , C07C231/02 , C07C309/77 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide a method of synthesis dispensing with a further strong synthesis step for removing a phenol protective group.
SOLUTION: 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 bond. The amide product 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 aftertreatment of the product, and reduces the amount of cyclizing agent, POCl
3 that is necessary to form the 3,4-dihydroisoquinoline.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供一种合成方法，分配更强的合成步骤，用于除去苯酚保护基。解决方案：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键的方法。然后可以分离酰胺产物，或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，简化了产物的后处理，并减少了形成3,4-二氢异喹啉所需的环化剂POCl 3 SB 3的量。版权所有（C）2011，JPO＆INPIT

8. 发明专利

JP2011098988A Method for preparing quaternary n-alkyl morphinan alkaloid salt 有权
标题翻译：制备季戊四醇盐酸吗啉盐的方法
公开(公告)号：JP2011098988A
公开(公告)日：2011-05-19
申请号：JP2011033923
申请日：2011-02-18
申请人： Mallinckrodt Inc , マリンクロットインコーポレイテッド
发明人： WANG PETER X , CANTRELL GARY L , HALVACHS ROBERT E , ROESCH KEVIN R , BUEHLER HENRY J , HAAR JOSEPH P
IPC分类号： C07D489/08
CPC分类号： C07D489/08 , C07D489/02 , C07D489/04 , Y02P20/582
摘要： PROBLEM TO BE SOLVED: To provide an improved method for the N-alkylation of tertiary morphinan alkaloid bases to form a corresponding quaternary morphinan alkaloid derivative. SOLUTION: The invention is directed to a method for preparation of a quaternary derivative of a tertiary N-substituted morphinan alkaloid. The method comprises (i) combining a tertiary N-substituted morphinan alkaloid substrate, or a suspension of a tertiary N-substituted morphinan alkaloid substrate in an anhydrous solvent system with an alkylating agent, or a solution of the alkylating agent in the anhydrous solvent system, to form a reaction product mixture containing the quaternary derivative of the tertiary N-substituted morphinan alkaloid substrate and any unreacted tertiary N-substituted morphinan alkaloid substrate, and (ii) adding a non-solubilizing solvent to the reaction product mixture to precipitate the quaternary derivative. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：为提供叔吗啉生物碱碱基的N-烷基化的改进方法以形成相应的季吗啡喃生物碱衍生物。解决方案：本发明涉及一种制备叔N-取代的吗啡喃生物碱的季衍生物的方法。该方法包括（i）将叔N-取代的吗啡喃生物碱底物或叔N-取代的吗啡喃生物碱底物在无水溶剂体系中的悬浮液与烷基化剂或烷基化剂在无水溶剂体系中的溶液形成含有叔N-取代的吗啡喃生物碱底物的季衍生物和任何未反应的叔取代的吗啡喃生物碱底物的反应产物混合物，和（ii）向反应产物混合物中加入不溶溶剂以沉淀季铵盐衍生物。版权所有（C）2011，JPO＆INPIT

9. 发明专利

JP2011052013A Method for preparing hexahydroisoquinoline from 1,2,3,4-tetrahydroisoquinoline 审中-公开
标题翻译：从1,2,3,4-四氢喹啉中制备十六氢喹啉的方法
公开(公告)号：JP2011052013A
公开(公告)日：2011-03-17
申请号：JP2010267843
申请日：2010-11-30
申请人： Mallinckrodt Inc , マリンクロットインコーポレイテッド
发明人： WANG PETER X , CANTRELL GARY L , MAGPARANGALAN DAN P , MOSER FRANK W , BAO JIAN , GROTE CHRISTOPHER W
IPC分类号： C07D217/20 , C07B61/00
CPC分类号： C07D217/20 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To fulfill a desire for a more efficient method for synthesizing a hexahydroisoquinoline in improved yield and enantiomeric excess, because hexahydroisoquinoline and its derivative are important synthetic intermediates for many morphinan compounds.
SOLUTION: There is directed to a method for the synthesis of morphinan, in particular, a method for the asymmetric reduction of an imine moiety in 3,4-dihydroisoquinoline to produce a tetrahydroisoquinoline, followed by a Birch reduction to produce 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.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：为了实现以更高的收率和对映体过量合成六氢异喹啉的更有效的方法，因为六氢异喹啉及其衍生物是许多吗啡喃化合物的重要合成中间体。解决方案：涉及合成吗啡喃的方法，特别是在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。版权所有（C）2011，JPO＆INPIT

10. 发明专利

JP2011068674A Improved method for preparation of 3,4-dihydroisoquinoline in synthesis of morphinan 有权
标题翻译：改进的合成三羟甲基吗啉的改进方法
公开(公告)号：JP2011068674A
公开(公告)日：2011-04-07
申请号：JP2010275153
申请日：2010-12-09
申请人： Mallinckrodt Inc , マリンクロットインコーポレイテッド
发明人： GROTE CHRISTOPHER W , WANG PETER X , MOSER FRANK W , CANTRELL GARY L
IPC分类号： C07D217/20
CPC分类号： C07C235/34 , C07C231/02 , C07C309/77 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide a synthetic method dispensing with further severe synthetic step for eliminating a phenol protection group. SOLUTION: There is provided a method for synthesis of morphinan. In particular, a method for coupling a carboxylic acid compound with an amine compound to form an amide bond. The formed amide product 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 post-processing of the product, and reduces the amount of POCl 3 that is a cyclizing agent necessary to form the 3,4-dihydroisoquinoline. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供一种分配进一步严格的合成步骤以消除苯酚保护基团的合成方法。解决方案：提供了吗啡喃合成方法。特别是一种使羧酸化合物与胺化合物偶合形成酰胺键的方法。然后可以分离形成的酰胺产物，或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。被保护的苯酚减少反应时间，简化了产物的后处理，并且减少了形成3,4-二氢异喹啉所必需的环化剂的POCl 3 SB 3的量。版权所有（C）2011，JPO＆INPIT

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