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1. 发明申请

US20080262231A1 Processes for Preparing Morphinans and Intermediates Thereof 有权
标题翻译：制备吗啡喃及其中间体的方法
公开(公告)号：US20080262231A1
公开(公告)日：2008-10-23
申请号：US11908136
申请日：2006-02-23
申请人： Peter Xianqi Wang , Frank W. Moser , Gary L. Cantrell , Jian Bao
发明人： Peter Xianqi Wang , Frank W. Moser , Gary L. Cantrell , Jian Bao
IPC分类号： C07D221/28 , C07D217/00 , C07D217/02
CPC分类号： C07D491/10 , C07D217/20 , C07D221/28 , C07D489/02
摘要： The present invention is directed to processes for the synthesis of morphinans. In particular, a process for cyclizing a β,γ-bicyclic ketone compound to form a nordihydrothebainone product using the Grewe cyclization reaction is improved by forming a reaction mixture comprising a β,γ-bicyclic ketone compound, a cyclizing acid and a water scavenging cyclization additive. In one embodiment, the Grewe transformation occurs in the presence of an acid anhydride as the cyclization additive. Further, the present invention is directed to processes for converting α,β-bicyclic ketone compounds (e.g., by-products of the Grewe cyclization reaction) to β,γ-bicyclic ketone compounds, wherein the β,γ-bicyclic ketone compounds may be recovered to further undergo Grewe cyclization and form the nordihydrothebainone product.
摘要翻译：本发明涉及合成吗啡喃的方法。特别地，通过形成包含β，γ-双环酮化合物，环化酸和清除水的环化反应的反应混合物，可以改进使用Grewe环化反应使β，γ-双环酮化合物环化形成一种二氢噻吩酮产物的方法添加剂。在一个实施方案中，Grewe转化发生在作为环化添加剂的酸酐的存在下。此外，本发明涉及将α，β-二环酮化合物（例如，Grewe环化反应的副产物）转化成β，γ-双环酮化合物的方法，其中β，γ-双环酮化合物可以是回收进一步进行Grewe环化并形成去氢二苯酮产物。

2. 发明授权

US07838677B2 Processes for preparing morphinans and intermediates thereof 有权
标题翻译：制备吗啡喃及其中间体的方法
公开(公告)号：US07838677B2
公开(公告)日：2010-11-23
申请号：US11908136
申请日：2006-02-23
申请人： Peter Xianqi Wang , Frank W. Moser , Gary L. Cantrell , Jian Bao
发明人： Peter Xianqi Wang , Frank W. Moser , Gary L. Cantrell , Jian Bao
IPC分类号： C07D221/22 , C07D489/02
CPC分类号： C07D491/10 , C07D217/20 , C07D221/28 , C07D489/02
摘要： The present invention is directed to processes for the synthesis of morphinans. In particular, a process for cyclizing a β,γ-bicyclic ketone compound to form a nordihydrothebainone product using the Grewe cyclization reaction is improved by forming a reaction mixture comprising a β,γ-bicyclic ketone compound, a cyclizing acid and a water scavenging cyclization additive. In one embodiment, the Grewe transformation occurs in the presence of an acid anhydride as the cyclization additive. Further, the present invention is directed to processes for converting α,β-bicyclic ketone compounds (e.g., by-products of the Grewe cyclization reaction) to β,γ-bicyclic ketone compounds, wherein the β,γ-bicyclic ketone compounds may be recovered to further undergo Grewe cyclization and form the nordihydrothebainone product.
摘要翻译：本发明涉及合成吗啡喃的方法。特别地，通过形成包含γ-双环酮化合物，环化酸和水的反应混合物，使Gewe环化反应使γ-二环酮化合物环化以形成一种二氢苯乙酮产物的方法得到改善清除环化添加剂。在一个实施方案中，Grewe转化发生在作为环化添加剂的酸酐的存在下。此外，本发明涉及将α，bb-二环酮化合物（例如，Grewe环化反应的副产物）转化为γ-双环酮化合物的方法，其中γ-双环酮可以回收化合物以进一步进行Grewe环化并形成去氢二苯酮产物。

3. 发明授权

US07834184B2 Opiate intermediates and methods of synthesis 有权
标题翻译：鸦片剂中间体和合成方法
公开(公告)号：US07834184B2
公开(公告)日：2010-11-16
申请号：US11718263
申请日：2005-10-21
申请人： Peter Xianqi Wang , Frank W. Moser , Gary L. Cantrell , Daniel P. Magparangalan
发明人： Peter Xianqi Wang , Frank W. Moser , Gary L. Cantrell , Daniel P. Magparangalan
IPC分类号： C07D221/28 , C07D217/04
CPC分类号： C07C235/34 , C07D217/20 , C07D221/28
摘要： Novel opiate intermediate compositions and methods of synthesis that include changing the substitution pattern on the aromatic ring of the pre-Grewe intermediate are provided. The intermediates are morphinane derivatives of formula (10), wherein X is a F or Cl and R is selected from the group consisting of an H, alkyl, aryl, acyl, formyl, COR″, CONHR″, COOR, Bn(benzyl), alkyl(methyl), and sulfonamide SO2CH2COPh.
摘要翻译：提供了新型鸦片中间体组合物和合成方法，其包括改变前Grewe中间体的芳环上的取代模式。中间体是式（10）的吗啡烷衍生物，其中X是F或Cl，R选自H，烷基，芳基，酰基，甲酰基，COR“，CONHR”，COOR，Bn（苄基），烷基（甲基）和磺酰胺SO2CH2COPh。

4. 发明授权

US07622586B2 Opiate intermediates and methods of synthesis 有权
公开(公告)号：US07622586B2
公开(公告)日：2009-11-24
申请号：US11741932
申请日：2007-04-30
申请人： Peter Xianqi Wang , Frank W. Moser , Gary L. Cantrell
发明人： Peter Xianqi Wang , Frank W. Moser , Gary L. Cantrell
IPC分类号： C07D217/20
CPC分类号： C07D217/20
摘要： Novel opiate intermediate compositions and methods of synthesis that include changing the substitution pattern on the aromatic ring of the pre-Grewe intermediate are provided.

5. 发明授权

US07511060B2 Opiate intermediates and methods of synthesis 有权
标题翻译：鸦片剂中间体和合成方法
公开(公告)号：US07511060B2
公开(公告)日：2009-03-31
申请号：US11741910
申请日：2007-04-30
申请人： Peter Xianqi Wang , Frank W. Moser
发明人： Peter Xianqi Wang , Frank W. Moser
IPC分类号： C07D217/00 , A61K31/47
CPC分类号： C07D217/16
摘要： Novel opiate intermediate compositions and methods of synthesis that include changing the substitution pattern on the aromatic ring of the pre-Grewe intermediate are provided.
摘要翻译：提供了新型鸦片中间体组合物和合成方法，其包括改变前Grewe中间体的芳环上的取代模式。

6. 发明授权

US07312368B2 Method for selective reduction of aromatic compounds 有权
公开(公告)号：US07312368B2
公开(公告)日：2007-12-25
申请号：US10581418
申请日：2004-12-02
申请人： Peter Xianqi Wang , Frank W. Moser
发明人： Peter Xianqi Wang , Frank W. Moser
IPC分类号： C07C17/10
CPC分类号： C07B35/02 , C07B31/00 , C07C213/08 , C07C231/12 , C07C2601/10 , C07C2601/16 , C07C217/60 , C07C233/34
摘要： A method for the selective reduction of an aromatic compound. The present invention provides a method for pre-venting the reduction of at least one halogen substituted aromatic ring of an aromatic compound, while allowing the reduction of at least one functional group on the aromatic compound. In the present invention at least one hydroxyl group is placed on the at least one halogen substituted aromatic ring to be protected from reduction. The aromatic compound is then reacted with at least one alkali metal in at least one nitrogen containing base and at least one alcohol at a ratio of the alcohol to the nitrogen containing base at which the aromatic ring with the hydroxyl group is protected from reduction, while the desired functional group is reduced.

7. 发明授权

US07321038B2 Method for the catalytic production of hydrocodone and hydromorphone 有权
标题翻译：氢可酮和氢吗啡酮的催化生产方法
公开(公告)号：US07321038B2
公开(公告)日：2008-01-22
申请号：US10973031
申请日：2004-10-25
申请人： Peter Xianqi Wang , Carl Ray White
发明人： Peter Xianqi Wang , Carl Ray White
IPC分类号： C07D489/02 , C07D489/00
CPC分类号： B01J31/2404 , B01J31/1658 , B01J2231/76 , B01J2531/821 , B01J2531/822 , B01J2531/827 , C07D489/02
摘要： A method for the catalytic conversion of codeine, morphine or analogs thereof into hydrocodone, hydromorphone or analogs thereof utilizing a transition metal catalyst of the formula [M(PR3R4R5)nXm]p; wherein R1 is H, alkyl, aryl or acyl; M is a Group VIII transition metal; R3, R4 and R5 are selected from the group consisting of alkyl, aryl, alkoxyl, phenoxyl and combinations thereof; X is a halide or an anion; n is 1, 2, 3 or 4; m is 1 or 2; and p is at least 1.
摘要翻译：利用过渡金属催化剂将式可待因，吗啡或其类似物催化转化为氢可酮，氢吗啡酮或其类似物的方法，其用式[M（PR 3 其中R 1是H，烷基，芳基或酰基; M是第VIII族过渡金属; R 3，R 4和R 5选自烷基，芳基，烷氧基，苯氧基及其组合; X是卤素或阴离子; n为1,2,3或4; m为1或2; p至少为1。

8. 发明授权

US07323565B2 Method for the catalytic production of hydrocodone and hydromorphone 有权
标题翻译：氢可酮和氢吗啡酮的催化生产方法
公开(公告)号：US07323565B2
公开(公告)日：2008-01-29
申请号：US10495503
申请日：2003-11-05
申请人： Peter Xianqi Wang , Carl Ray White
发明人： Peter Xianqi Wang , Carl Ray White
IPC分类号： C07D489/02 , C07D489/00
CPC分类号： C07D489/02
摘要： A method for the catalytic conversion of codeine, morphine or analogs thereof into hydrocodone, hydromorphone or analogs thereof utilizing a transition metal complex of a tertiary phosphine halide as catalyst.
摘要翻译：使用叔膦卤化物作为催化剂的过渡金属络合物，将可待因，吗啡或其类似物催化转化为氢可酮，氢吗啡酮或其类似物的方法。

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