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1. 发明授权

US07687631B2 Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate 有权
标题翻译： {[5-（3-氟苯基） - 吡啶-2-基]甲基}膦酸二乙酯的合成
公开(公告)号：US07687631B2
公开(公告)日：2010-03-30
申请号：US11824245
申请日：2007-06-29
申请人： Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam
发明人： Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam
IPC分类号： C07D405/06
CPC分类号： C07D405/06 , C07F9/58
摘要： This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: wherein R9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X2 is Cl, Br, or I; X3 is selected from Cl and Br; and PdLn is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.
摘要翻译：本申请公开了一种制备膦酸酯的新方法，其可用作制备作为凝血酶受体拮抗剂的替卡宾类似物的中间体。本文教导的化学实例可以通过以下方案来举例说明：其中R9选自具有1-10个碳原子的烷基，芳基杂芳基和芳基烷基，R11各自独立地选自烷基，芳基杂芳基和具有1至 10个碳原子和氢，X2是Cl，Br或I; X3选自Cl和Br; PdLn是负载型钯金属催化剂或可溶性多相钯催化剂。 L-衍生试剂是将化合物137D的醇官能团转化成可被三有机 - 亚磷酸酯膦酸酯取代的任何离去基团的部分。

2. 发明申请

US20100137597A1 SYNTHESIS Of DIETHYLPHOSPHONATE 有权
标题翻译：二乙基磷酸酯的合成
公开(公告)号：US20100137597A1
公开(公告)日：2010-06-03
申请号：US12701174
申请日：2010-02-05
申请人： Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam
发明人： Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam
IPC分类号： C07F9/40
CPC分类号： C07D405/06 , C07F9/58
摘要： This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: wherein R9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X2 is Cl, Br, or I; X3 is selected from Cl and Br; and PdLn is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.
摘要翻译：本申请公开了一种制备膦酸酯的新方法，其可用作制备作为凝血酶受体拮抗剂的替卡宾类似物的中间体。本文教导的化学实例可以通过以下方案来举例说明：其中R9选自具有1-10个碳原子的烷基，芳基杂芳基和芳基烷基，R11各自独立地选自烷基，芳基杂芳基和具有1至 10个碳原子和氢，X2是Cl，Br或I; X3选自Cl和Br; PdLn是负载型钯金属催化剂或可溶性多相钯催化剂。 L-衍生试剂是将化合物137D的醇官能团转化成可被三有机 - 亚磷酸酯膦酸酯取代的任何离去基团的部分。

3. 发明授权

US07605275B2 Exo- and diastereo- selective syntheses of himbacine analogs 有权
标题翻译：烟草类似物的外切和非对映选择性合成
公开(公告)号：US07605275B2
公开(公告)日：2009-10-20
申请号：US11331324
申请日：2006-01-12
申请人： Frank Xing Chen , Marc Poirier , Mingsheng Huang , Vijay Sabesan , George Wu , Anantha R. Sudhakar , Tao Wang , Ji Xie , Jing Liao , Ilia A. Zavialov , Hoa N. Nguyen , Ngiap Kie Lim , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam
发明人： Frank Xing Chen , Marc Poirier , Mingsheng Huang , Vijay Sabesan , George Wu , Anantha R. Sudhakar , Tao Wang , Ji Xie , Jing Liao , Ilia A. Zavialov , Hoa N. Nguyen , Ngiap Kie Lim , Daw-long Kwok , Jian Cui , Xiaojing Yang , Tiruvettipuram K. Thiruvengadam
IPC分类号： C07D307/92
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：

4. 发明申请

US20110251392A1 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：US20110251392A1
公开(公告)日：2011-10-13
申请号：US13168029
申请日：2011-06-24
申请人： George Wu , Anantha R. Sudhakar , Mingsheng Huang , Tao Wang , Vijay Sabesan , Ji Xie , Frank Xing Chen , Marc Poirier , 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 , Mingsheng Huang , Tao Wang , Vijay Sabesan , Ji Xie , Frank Xing Chen , Marc Poirier , 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： C07F9/141 , C07C205/56 , C07C309/16 , C07D213/02 , C07C235/00 , C07C205/44 , C07D307/77 , C07D277/64
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：

5. 发明申请

US20090281321A1 EXO- AND DIASTEREO- SELECTIVE SYNTHESES OF HIMBACINE ANALOGS 有权
标题翻译：乙酰胺类似物的外 - 和二选择性合成
公开(公告)号：US20090281321A1
公开(公告)日：2009-11-12
申请号：US12505079
申请日：2009-07-17
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： C07C69/608 , C07D405/08 , C07F9/40 , C07D307/92 , C07D417/08 , C07D277/64
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：

6. 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。

7. 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：

8. 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。

9. 发明授权

US5750745A Process for preparing delta 9, 11 and 21-chlorocorticosteroids 失效
标题翻译：制备δ9,11和21-氯皮质激素的方法
公开(公告)号：US5750745A
公开(公告)日：1998-05-12
申请号：US737690
申请日：1996-11-18
申请人： Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam , Chou-Hong Tann , Junning Lee , Cesar Colon
发明人： Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam , Chou-Hong Tann , Junning Lee , 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： PCT No.PCT / US95 / 06600 Sec。 371日期：1996年11月18日 102（e）1996年11月18日日期PCT提交1995年5月30日PCT公布。第WO95 / 32989号公报日期1995年12月7日描述了使用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，并且也可用于11,21-二羟基类固醇到21-氯-DTA 9,11的一步转化类固醇。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. 发明申请

US20110144327A1 PROCESS FOR THE SYNTHESIS OF AZETIDINONES 审中-公开
标题翻译：合成AZETIDINONES的方法
公开(公告)号：US20110144327A1
公开(公告)日：2011-06-16
申请号：US13008458
申请日：2011-01-18
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
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。

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