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1. 发明授权

US08293927B2 Efficient synthesis of morphine and codeine 失效
标题翻译：吗啡和可待因的高效合成
公开(公告)号：US08293927B2
公开(公告)日：2012-10-23
申请号：US12778466
申请日：2010-05-12
申请人： Philip D. Magnus , Benjamin P. Fauber , Neeraj Sane
发明人： Philip D. Magnus , Benjamin P. Fauber , Neeraj Sane
IPC分类号： C07D307/94
CPC分类号： C07D489/08 , C07D307/91 , C07D311/96 , C07D489/02 , C07D491/18
摘要： The present invention relates to methods for the synthesis of morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.
摘要翻译：本发明涉及合成吗啡，中间体，盐及其衍生物的方法。在优选的实施方案中，本发明涉及用于提高所述吗啡，吗啡相关衍生物及其中间体的效率和总产率的方法。在另外的实施方案中，本发明涉及用于提高雪花胺及其中间体的效率和总产率的方法。

2. 发明授权

US06667410B2 Conversion of &agr;,&bgr;-unsaturated ketones and &agr;,&bgr;-unsaturated esters into &agr;-hydroxy ketones and &agr;-hydroxy esters using Mn(III) catalyst, phenylsilane and dioxygen 失效
公开(公告)号：US06667410B2
公开(公告)日：2003-12-23
申请号：US09952326
申请日：2001-09-14
申请人： Philip D. Magnus , Andrew H. Payne
发明人： Philip D. Magnus , Andrew H. Payne
IPC分类号： C07J500
CPC分类号： C07C403/16 , C07B2200/07 , C07C45/62 , C07C45/64 , C07C2601/14 , C07C2601/16 , C07F7/1892 , C07J13/005 , C07C49/04 , C07C49/647 , C07C49/21 , C07C49/403 , C07C49/792 , C07C49/17 , C07C49/747 , C07C49/707 , C07C49/743 , C07C49/713
摘要： The present invention provides a novel process for the conversion of &agr;,&bgr;-unsaturated ketones. This invention is an improvement over existing processes in that it operates at neutral reaction conditions that prevent the formation of side reactions and that it is a single step, which proceeds with complete selectivity and gives a yield that is approximately 30% higher than the currently used processes. An example of this process is the conversion of 16-dehydroprogesterone into 17 &agr;-hydroxyprogesterone.

3. 发明授权

US08450365B2 Efficient synthesis of galanthamine 失效
标题翻译：高效合成雪花胺
公开(公告)号：US08450365B2
公开(公告)日：2013-05-28
申请号：US12778515
申请日：2010-05-12
申请人： Philip D. Magnus , Ben Fauber , Neeraj Sane
发明人： Philip D. Magnus , Ben Fauber , Neeraj Sane
IPC分类号： C07D307/77 , A61K31/343
CPC分类号： C07D489/08 , C07D307/91 , C07D311/96 , C07D489/02 , C07D491/18
摘要： The present invention relates to methods for the synthesis of galanthamine, morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.
摘要翻译：本发明涉及合成雪花胺，吗啡，中间体，其盐及其衍生物的方法。在优选的实施方案中，本发明涉及用于提高所述吗啡，吗啡相关衍生物及其中间体的效率和总产率的方法。在另外的实施方案中，本发明涉及用于提高雪花胺及其中间体的效率和总产率的方法。

4. 发明申请

US20100292466A1 Efficient Synthesis Of Galanthamine 失效
标题翻译：高效合成加兰他敏
公开(公告)号：US20100292466A1
公开(公告)日：2010-11-18
申请号：US12778515
申请日：2010-05-12
申请人： Philip D. Magnus , Benjamin P. Fauber , Neeraj Sane
发明人： Philip D. Magnus , Benjamin P. Fauber , Neeraj Sane
IPC分类号： C07D223/14 , C07D311/78
CPC分类号： C07D489/08 , C07D307/91 , C07D311/96 , C07D489/02 , C07D491/18
摘要： The present invention relates to methods for the synthesis of galanthamine, morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.
摘要翻译：本发明涉及合成雪花胺，吗啡，中间体，其盐及其衍生物的方法。在优选的实施方案中，本发明涉及用于提高所述吗啡，吗啡相关衍生物及其中间体的效率和总产率的方法。在另外的实施方案中，本发明涉及用于提高雪花胺及其中间体的效率和总产率的方法。

5. 发明授权

US5739337A Process for preparing dibenzo-1-carboxamido-1,4-azabicyclo�3.2.1!octanes 失效
标题翻译：制备二苯并-1-甲酰氨基-1,4-氮杂双环[3.2.1]辛烷的方法
公开(公告)号：US5739337A
公开(公告)日：1998-04-14
申请号：US613030
申请日：1996-03-08
申请人： Philip D. Magnus
发明人： Philip D. Magnus
IPC分类号： C07D451/02 , C07D221/22
CPC分类号： C07D451/02
摘要： Disclosed are a process and novel compounds useful for preparing compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, inorganic or optionally substituted organic substituents; and R.sub.3 is hydrogen, or an optionally substituted organic group, the process comprising cyclizing a tetrahydroisoquinoline of the formula ##STR2## where Y is a leaving group, in the presence of a stong base. The invention also encompasses a process for preparing the tetrahydroisoquinoline; and a process for converting the tetrahydroisoquinoline to the final amide I.
摘要翻译：公开了用于制备式I化合物的方法和新化合物，其中R 1和R 2独立地表示氢，无机或任选取代的有机取代基; 并且R 3是氢或任选取代的有机基团，所述方法包括在贱碱存在下环化式为“IMAGE”的四氢异喹啉，其中Y是离去基团。本发明还包括制备四氢异喹啉的方法; 以及将四氢异喹啉转化为最终酰胺I的方法。

6. 发明授权

US5220016A Synthesis of navelbine analogs 失效
标题翻译：诺维本类似物的合成
公开(公告)号：US5220016A
公开(公告)日：1993-06-15
申请号：US736300
申请日：1991-07-29
申请人： Philip D. Magnus , Lee S. Thurston
发明人： Philip D. Magnus , Lee S. Thurston
IPC分类号： C07D471/20 , C07D519/04
CPC分类号： C07D519/04 , Y02P20/55
摘要： The invention is a de novo synthesis of the norcatharanthine moiety of navelbine. The synthesis includes condensing a Grignard reagent prepared from an amine-protected R(+)-piperidinyl methanol with an N-protected 2-methoxyoxalyl indole. The indole N-protecting group is removed to provide a 2-methoxyindole hydroxy ester which is coupled to vindoline. After removal of the amineprotecting group from the piperidinyl group, ring closure to the indole moiety provides dihydrodesethyl navelbine. Other derivatives and analogs of navelbine with potential clinical applications in cancer chemotherapy may be readily synthesized. The synthesis opens a route to a wide variety of navelbine modifications, including modifications at or near the tryptamine bridge.
摘要翻译：本发明是诺维本的去甲肾上腺素部分的从头合成。该合成包括将由胺保护的R（+） - 哌啶基甲醇制备的格氏试剂与N-保护的2-甲氧基草酰基吲哚缩合。除去吲哚N-保护基，得到与维链二氢吡喃偶联的2-甲氧基吲哚羟基酯。从哌啶基除去氨基保护基后，向吲哚部分的闭环提供了二氢去乙基诺维本。可以容易地合成其他具有潜在临床应用于癌症化学疗法的衍生物和类似物。合成开启了各种诺维巴修饰的途径，包括在色胺桥附近的修饰。

7. 发明申请

US20100292489A1 Cross-conjugated 2,5-cyclohexadienone and related synthesis methods 失效
标题翻译：交联共轭的2,5-环己二烯酮及相关合成方法
公开(公告)号：US20100292489A1
公开(公告)日：2010-11-18
申请号：US12778392
申请日：2010-05-12
申请人： Philip D. Magnus , Benjamin P. Fauber , Neeraj Sane
发明人： Philip D. Magnus , Benjamin P. Fauber , Neeraj Sane
IPC分类号： C07D311/96 , C07C47/228
CPC分类号： C07D489/08 , C07D307/91 , C07D311/96 , C07D489/02 , C07D491/18
摘要： The present invention relates to methods for the synthesis of galanthamine, morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.
摘要翻译：本发明涉及合成雪花胺，吗啡，中间体，其盐及其衍生物的方法。在优选的实施方案中，本发明涉及用于提高所述吗啡，吗啡相关衍生物及其中间体的效率和总产率的方法。在另外的实施方案中，本发明涉及用于提高雪花胺及其中间体的效率和总产率的方法。

8. 发明授权

US5442065A Synthesis of tetrahydroquinoline enediyne core analogs of dynemicin 失效
标题翻译： dynemicin四氢喹啉烯二烯核心类似物的合成
公开(公告)号：US5442065A
公开(公告)日：1995-08-15
申请号：US118862
申请日：1993-09-09
申请人： Philip D. Magnus , Theodore Iliadis , Shane A. Eisenbeis , Robin A. Fairhurst
发明人： Philip D. Magnus , Theodore Iliadis , Shane A. Eisenbeis , Robin A. Fairhurst
IPC分类号： C07D221/22 , C07F7/02 , C07D221/06
CPC分类号： C07D221/22 , Y02P20/55
摘要： A process is described for the preparation of the core azobicyclo[7.3.1]tridecaenediyne moiety of the antitumor antibiotic dynemicin. The synthesis allows efficient production of the enediyne as a stable, compound in good yield from the adamantyl N-protected azabicyclo[7.3.1]tridecadiyne. The adamantyl protecting group is employed in the starting material, N-adamantyl dihydroquinoline or N-adamantyl 6-methoxy quinoline. Also disclosed are process for the synthesis of 3-hydroxy-6-methoxyquinoline and several N-substituted derivatives of azobicyclo[7.3.1]tridecaenediyne. Solid tumor and leukemia assays were performed on the analogs of dynemicin. The results suggest a method that these compounds will useful in treating certain types of leukemias and solid tumors. The disclosed synthesis provides a route to new dynemicin intermediates and analogs which will allow development of second and third generation dynemicins.
摘要翻译：描述了制备抗肿瘤抗生素dynemicin的核心偶氮二环[7.3.1]十三碳二烯部分的方法。该合成允许以金刚烷基N-保护的氮杂双环[7.3.1]十三烷二炔作为稳定的化合物有效生产烯二醇。金刚烷基保护基用于起始原料，N-金刚烷基二氢喹啉或N-金刚烷基6-甲氧基喹啉。还公开了合成3-羟基-6-甲氧基喹啉和若干N-取代的偶氮二环[7.3.1]十一碳二烯的衍生物的方法。对dynemicin类似物进行实体瘤和白血病检测。结果表明这些化合物可用于治疗某些类型的白血病和实体瘤的方法。所公开的综合提供了新的dynemicin中间体和类似物的途径，其将允许开发第二代和第三代dynemicins。

9. 发明授权

US08362283B2 Cross-conjugated 2,5-cyclohexadienone and related synthesis methods 失效
标题翻译：交联共轭的2,5-环己二烯酮及相关合成方法
公开(公告)号：US08362283B2
公开(公告)日：2013-01-29
申请号：US12778392
申请日：2010-05-12
申请人： Philip D. Magnus , Benjamin P. Fauber , Neeraj Sane
发明人： Philip D. Magnus , Benjamin P. Fauber , Neeraj Sane
IPC分类号： C07D317/70 , C07D307/94
CPC分类号： C07D489/08 , C07D307/91 , C07D311/96 , C07D489/02 , C07D491/18
摘要： The present invention relates to methods for the synthesis of galanthamine, morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.
摘要翻译：本发明涉及合成雪花胺，吗啡，中间体，其盐及其衍生物的方法。在优选的实施方案中，本发明涉及用于提高所述吗啡，吗啡相关衍生物及其中间体的效率和总产率的方法。在另外的实施方案中，本发明涉及用于提高雪花胺及其中间体的效率和总产率的方法。

10. 发明申请

US20100292475A1 Efficient Synthesis Of Morphine And Codeine 失效
标题翻译：吗啡和可待因的高效合成
公开(公告)号：US20100292475A1
公开(公告)日：2010-11-18
申请号：US12778466
申请日：2010-05-12
申请人： Philip D. Magnus , Benjamin P. Fauber , Neeraj Sane
发明人： Philip D. Magnus , Benjamin P. Fauber , Neeraj Sane
IPC分类号： C07D489/00 , C07D311/78
CPC分类号： C07D489/08 , C07D307/91 , C07D311/96 , C07D489/02 , C07D491/18
摘要： The present invention relates to methods for the synthesis of morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.
摘要翻译：本发明涉及合成吗啡，中间体，盐及其衍生物的方法。在优选的实施方案中，本发明涉及用于提高所述吗啡，吗啡相关衍生物及其中间体的效率和总产率的方法。在另外的实施方案中，本发明涉及用于提高雪花胺及其中间体的效率和总产率的方法。

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