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1. 发明申请

US20120296093A1 EXO- AND DIASTEREO- SELECTIVE SYNTHESIS OF HIMBACINE ANALOGS 有权
标题翻译：乙酰胺类似物的外源和二硫选择性合成
公开(公告)号：US20120296093A1
公开(公告)日：2012-11-22
申请号：US13563136
申请日：2012-07-31
申请人： George Wu , Anantha R. SUDHAKAR , Tao WANG , Ji XIE , Frank Xing CHEN , Marc POIRIER , Mingsheng HUANG , Vijay SABESAN , Daw-long KWOK , Jian CUI , Xiaojing YANG , Tiruvettipuram K. THIRUVENGADAM , Jing LIAO , Ilia A. Zavialov , Hoa N. NGUYEN , Ngiap Kie LIM
发明人： George Wu , Anantha R. SUDHAKAR , Tao WANG , Ji XIE , Frank Xing CHEN , Marc POIRIER , Mingsheng HUANG , Vijay SABESAN , Daw-long KWOK , Jian CUI , Xiaojing YANG , Tiruvettipuram K. THIRUVENGADAM , Jing LIAO , Ilia A. Zavialov , Hoa N. NGUYEN , Ngiap Kie LIM
IPC分类号： C07D405/08 , C07C205/56 , C07D417/08 , C07D307/77 , C07C69/732 , C07F7/18 , C07C205/44 , C07C309/08 , C07C205/55 , C07D277/64 , C07F9/58 , C07C233/09
CPC分类号： C07D263/56 , C07C69/606 , C07C69/732 , C07C201/10 , C07C201/12 , C07C205/44 , C07C205/55 , C07C231/10 , C07C231/12 , C07C235/28 , C07C303/32 , C07C309/08 , C07C2601/16 , C07D277/64 , C07D307/92 , C07D333/56 , C07D405/06 , C07D413/06 , C07D417/06 , C07F7/1804 , C07F9/58 , Y02P20/55 , C07C233/28
摘要： This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:
摘要翻译：本申请公开了一种制备可用作凝血酶受体拮抗剂的烟肼类似物的新方法。该方法部分基于使用手性硝基中心的碱促进的动态差向异构化。本文教导的化学结构可以举例说明如下：

2. 发明授权

US08273790B2 Exo-selective synthesis of himbacine analogs 有权
标题翻译：非选择性合成替卡宾类似物
公开(公告)号：US08273790B2
公开(公告)日：2012-09-25
申请号：US13370768
申请日：2012-02-10
申请人： Tiruvettipuram K. Thiruvengadam , Anantha Sudhakar , Ngiap Kie Lim , Daw-Iong Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
发明人： Tiruvettipuram K. Thiruvengadam , Anantha Sudhakar , Ngiap Kie Lim , Daw-Iong Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
IPC分类号： A61K31/335
CPC分类号： C07D493/10 , C07C235/28 , C07D295/185 , C07D307/92 , C07D317/72 , C07D405/06
摘要： This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists. The chemistry disclosed herein is exemplified in the following synthesis sequence:
摘要翻译：本申请公开了一种用于合成烟肼类似物的新方法，以及由此制备的化合物。合成通过包括环状缩酮酰胺途径，手性氨基甲酸酯酰胺路线和手性氨基甲酸酯路线的替代途径进行。由此制备的化合物可用作凝血酶受体拮抗剂。本文公开的化学例如以下合成顺序：

3. 发明授权

US08138180B2 Exo-selective synthesis of himbacine analogs 有权
公开(公告)号：US08138180B2
公开(公告)日：2012-03-20
申请号：US12827000
申请日：2010-06-30
申请人： Tiruvettipuram K. Thiruvengadam , Anantha Sudhakar , Ngiap Kie Lim , Daw-long Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
发明人： Tiruvettipuram K. Thiruvengadam , Anantha Sudhakar , Ngiap Kie Lim , Daw-long Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
IPC分类号： A61K31/535
CPC分类号： C07D493/10 , C07C235/28 , C07D295/185 , C07D307/92 , C07D317/72 , C07D405/06
摘要： This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists. The chemistry disclosed herein is exemplified in the following synthesis sequence:

4. 发明授权

US5442047A Process for preparing isepamicin 失效
标题翻译：制备异环霉素的方法
公开(公告)号：US5442047A
公开(公告)日：1995-08-15
申请号：US138558
申请日：1993-10-15
申请人： Chou-Hong Tann , Tiruvettipuram K. Thiruvengadam , John S. Chiu , Cesar Colon , Michael D. Green
发明人： Chou-Hong Tann , Tiruvettipuram K. Thiruvengadam , John S. Chiu , Cesar Colon , Michael D. Green
IPC分类号： C07D277/64 , C07D277/74 , C07H15/236 , C07H15/26 , C07H1/00
CPC分类号： C07D277/74 , C07D277/64 , C07H15/236 , C07H15/26
摘要： An improved process for converting gentamicin B to isepamicin comprising forming 3,6'-di-N-formylgentamicin B, acylating the 1-amino group with an N-protected (S)-isoserine compound and removing all the blocking groups under conditions which result in high yields of isepamicin. A novel formylating agent, 2-formylmercaptobenzothiazole, and intermediate compounds are also disclosed.
摘要翻译：一种将庆大霉素B转化为异环磷酰胺的改进方法，包括形成3,6'-二-N-甲酰基阿霉素B，用N-保护的（S） - 异丝氨酸化合物酰化1-氨基，并在产生的条件下除去所有的封闭基团在高产量的异环霉素。还公开了一种新型甲酰化剂，2-甲酰巯基苯并噻唑和中间体化合物。

5. 发明授权

US08383810B2 Process for the synthesis of azetidinones 有权
标题翻译：合成氮杂环丁酮的方法
公开(公告)号：US08383810B2
公开(公告)日：2013-02-26
申请号：US13323366
申请日：2011-12-12
申请人： Tiruvettipuram K. Thiruvengadam , John S. Chiu , Xiaoyong Fu , Timothy L. McAllister
发明人： Tiruvettipuram K. Thiruvengadam , John S. Chiu , Xiaoyong Fu , Timothy L. McAllister
IPC分类号： C07D205/08 , C07H7/02
CPC分类号： C07D205/08 , C07H17/02
摘要： A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.
摘要翻译：提供了一种制备氮杂环丁酮的方法，所述氮杂环丁酮可用作半乳聚糖和低胆固醇血症药物的合成中的中间体，包括使（b） - （取代的 - 氨基）酰胺，和（取代的 - 氨基）酸酯，（取代 - 氨基）硫代碳酸酯与甲硅烷基化剂和选自碱金属羧酸盐，季铵羧酸盐，季铵氢氧化物，季铵醇盐，季铵氧化物及其水合物的环化剂或其反应产物：（i）至少一种季铵卤化物和至少一种碱金属羧酸盐; 或（ii）至少一种季铵氯化物，季铵溴化物或季铵碘化物和至少一种碱金属氟化物，其中环化剂的季铵部分是未取代的或被一至四个独立地选自由烷基，芳烷基和芳基烷基 - 烷基组成。

6. 发明申请

US20120302745A1 EXO-SELECTIVE SYNTHESIS OF HIMBACINE ANALOGS 审中-公开
标题翻译：苯菌胺类似物的选择性合成
公开(公告)号：US20120302745A1
公开(公告)日：2012-11-29
申请号：US13564966
申请日：2012-08-02
申请人： Tiruvettipuram K. Thiruvengadam , Anantha R. Sudhakar , Ngiap Kie Lim , Daw-Iong Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
发明人： Tiruvettipuram K. Thiruvengadam , Anantha R. Sudhakar , Ngiap Kie Lim , Daw-Iong Kwok , George G. Wu , Tao Wang , Mingsheng Huang , Michael D. Green
IPC分类号： C07C269/06 , C07D307/92 , C07D405/08 , C07D317/72 , C07D413/12
CPC分类号： C07D493/10 , C07C235/28 , C07D295/185 , C07D307/92 , C07D317/72 , C07D405/06
摘要： This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists. The chemistry disclosed herein is exemplified in the following synthesis sequence:
摘要翻译：本申请公开了一种用于合成烟肼类似物的新方法，以及由此制备的化合物。合成通过包括环状缩酮酰胺途径，手性氨基甲酸酯酰胺路线和手性氨基甲酸酯路线的替代途径进行。由此制备的化合物可用作凝血酶受体拮抗剂。本文公开的化学例如以下合成顺序：

7. 发明授权

US07678948B2 Synthesis of 3-(5-nitrocyclohex-1-enyl) acrylic acid and esters thereof 失效
标题翻译： 3-（5-硝基环己-1-烯基）丙烯酸及其酯的合成
公开(公告)号：US07678948B2
公开(公告)日：2010-03-16
申请号：US12274075
申请日：2008-11-19
申请人： Tiruvettipuram K. Thiruvengadam , Tao Wang , John S. Chiu , Jing Liao
发明人： Tiruvettipuram K. Thiruvengadam , Tao Wang , John S. Chiu , Jing Liao
IPC分类号： C07C205/01
CPC分类号： C07C251/44 , C07C201/06 , C07C249/08 , C07C2601/16 , C07C205/56 , C07C251/42
摘要： This application discloses provides a process for the introduction of nitro-group functionality into a compound which contains also a site of unsaturation and/or oxygen functionality by direct (one step) oxidation of an oxime functional group mediated by a molybdenum VI/VII peroxo complex, the process comprising: (a) providing a substrate of Formula I containing an oxime functional group; wherein R1 and R2 are selected independently from linear, branched or cyclic alkyl and linear, branched or cyclic alkenyl groups, optionally substituted, with the proviso that at least one of R1 or R2 contains a carbon/carbon double bond; and (b) contacting said substrate of Formula I with a molybdenum oxidation complex, thereby oxidizing said oxime functional group to a nitro functional group to yield the structure of Formula III. Where R1 and R2 are as defined above.
摘要翻译：本申请公开提供了一种通过由钼VI / VII过氧配合物介导的肟官能团的直接（一步）氧化将硝基官能团引入到还含有不饱和位和/或氧官能团位点的化合物的方法该方法包括：（a）提供含有肟官能团的式I的底物; 其中R 1和R 2独立地选自直链，支链或环状的烷基和直链，支链或环状烯基，任选被取代，条件是R 1或R 2中的至少一个含有碳/碳双键; 和（b）使式I的底物与钼氧化络合物接触，从而将所述肟官能团氧化为硝基官能团，得到式III的结构。其中R1和R2如上所定义。

8. 发明授权

US06872826B2 Stereoselective alkylation of chiral 2-methyl-4-protected piperazines 失效
标题翻译：手性2-甲基-4-保护的哌嗪的立体选择性烷基化
公开(公告)号：US06872826B2
公开(公告)日：2005-03-29
申请号：US10400429
申请日：2003-03-27
申请人： Wenxue Wu , Hongbiao Liao , David J. S. Tsai , David R. Andrews , Dinesh Gala , Gary M. Lee , Martin Lawrence Schwartz , Timothy L. McAllister , Xiaoyong Fu , Donal Maloney , Tiruvettipuram K. Thiruvengadam , Chou-Hang Tann
发明人： Wenxue Wu , Hongbiao Liao , David J. S. Tsai , David R. Andrews , Dinesh Gala , Gary M. Lee , Martin Lawrence Schwartz , Timothy L. McAllister , Xiaoyong Fu , Donal Maloney , Tiruvettipuram K. Thiruvengadam , Chou-Hang Tann
IPC分类号： C07D241/04 , C07B53/00 , C07B61/00 , C07C45/51 , C07C303/28 , C07C309/73 , C07D295/084 , C07D295/088 , C07D295/185 , C07D295/192 , C07D295/205 , C07D295/067
CPC分类号： C07D295/185 , C07B2200/07 , C07C45/512 , C07C67/343 , C07C309/73 , C07D295/088 , C07D295/092 , C07D295/192 , C07D295/205 , C07C49/255 , C07C69/734 , C07C49/84
摘要： In an illustrative embodiment, the present invention describes the synthesis of the following compound and similar compounds, in high stereochemical purity by a novel stereoselective alkylation process:
摘要翻译：在说明性实施方案中，本发明通过新的立体选择性烷基化方法描述了具有高立体化学纯度的以下化合物和类似化合物的合成：

9. 发明授权

US5616742A Process for preparing .DELTA.9,11 and 21-chloro corticosteroids 失效
标题翻译：制备DELTA 9,11和21-氯皮质类固醇的方法
公开(公告)号：US5616742A
公开(公告)日：1997-04-01
申请号：US446982
申请日：1995-05-22
申请人： Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam , Chou-Hong Tann , Cesar Colon
发明人： Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam , Chou-Hong Tann , Cesar Colon
IPC分类号： C07J20060101 , C07J5/00 , C07J7/00 , C07J51/00 , C07J75/00
CPC分类号： C07J7/0085 , C07J5/0076 , C07J51/00
摘要： Described is a process for the regioselective dehydration of 11-hydroxy steroids using PCl.sub.5, PCl.sub.3, POCl.sub.3 or either SO.sub.2 Cl.sub.2 and imidazole, or PPh.sub.3 and CCl.sub.4. The disclosed process selectively forms .DELTA..sup.9,11 steroids from either 11-.alpha.- or 11-.beta.-hydroxy steroids, and can also be used for the one-step conversion of 11,21-dihydroxy steroids to 21-chloro-.DELTA..sup.9,11 steroids.Also disclosed are processes for the regioselective conversion of 11-.beta.-chloro steroids to .DELTA..sup.9,11 steroids, and for regioselectively converting an 11,17,21-trihydroxy streoid to a 21-chloro-11,17-dihydroxy steroid.
摘要翻译：描述了使用PCl5，PCl3，POCl3或SO2Cl2和咪唑或PPh3和CCl4区域选择性脱水11-羟基类固醇的方法。所公开的方法选择性地从11-α或11-β-羟基类固醇形成DELTA 9,11类固醇，并且还可用于11,21-二羟基类固醇一步转化为21-氯-DTA 9， 11种类固醇。还公开了将11-β-氯类固醇区域选择性转化为DELTA 9,11类固醇的方法，并将11,17,21-三羟基链霉亲和力区域选择性地转化为21-氯-11,17-二羟基类固醇。

10. 发明授权

US5539121A 2-formylmercaptobenzothiazole 失效
标题翻译： 2-甲酰巯基苯并噻唑
公开(公告)号：US5539121A
公开(公告)日：1996-07-23
申请号：US442084
申请日：1995-05-16
申请人： Chou-Hong Tann , Tiruvettipuram K. Thiruvengadam , John S. Chiu , Cesar Colon , Michael D. Green
发明人： Chou-Hong Tann , Tiruvettipuram K. Thiruvengadam , John S. Chiu , Cesar Colon , Michael D. Green
IPC分类号： C07D277/64 , C07D277/74 , C07H15/236 , C07H15/26 , C07D417/00
CPC分类号： C07D277/74 , C07D277/64 , C07H15/236 , C07H15/26
摘要： There is disclosed a novel formylating agent, 2-formylmercaptobenzothiazole.
摘要翻译：公开了一种新的甲酰化剂2-甲酰巯基苯并噻唑。

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