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1. 发明授权

US06307048B1 Enantioselective alkylation of tricyclic compounds 有权
标题翻译：三环化合物的对映选择性烷基化
公开(公告)号：US06307048B1
公开(公告)日：2001-10-23
申请号：US09442511
申请日：1999-11-18
申请人： Shen-Chun Kuo , Charles F. Bernard , Frank Xing Chen , Donald Hou , Agnes S. Kim-Meade , George G. Wu
发明人： Shen-Chun Kuo , Charles F. Bernard , Frank Xing Chen , Donald Hou , Agnes S. Kim-Meade , George G. Wu
IPC分类号： C07D40102
CPC分类号： C07D401/04 , C07D401/14 , Y02P20/55
摘要： Disclosed is a process for preparing a compound of the formula: wherein X1, X2, X3, X4, and X5 are independently selected from the group consisting of H, halo, alkyl, alkoxy, aryl, and aryloxy, and R is a protecting group, in which a compound having the formula wherein X1, X2, X3, X4, and X5 are as defined above, is treated with the following, in any sequence: (a) a non-nucleophilic strong base; (b) a chiral amino alcohol; and (c) a compound having the formula wherein L is a leaving group and R is as defined above. The compounds made by this process are useful intermediates for preparing compounds that are inhibitors of farnesyl protein transferase.
摘要翻译：公开了一种制备下式化合物的方法：其中X 1，X 2，X 3，X 4和X 5独立地选自H，卤素，烷基，烷氧基，芳基和芳氧基，R是保护基其中具有如下定义的具有如下定义的化合物：（a）非亲核性强碱;（b）手性氨基醇（其中R 1，R 2，R 3，X 4， ; 和（c）具有甲醛的化合物L是离去基团，R如上定义。通过该方法制备的化合物是制备法呢基蛋白转移酶抑制剂的化合物的有用中间体。

2. 发明授权

US08076479B2 Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3,3a-dihydro-pyrazolo[1,5-a]pyrimidin-7-yl)-amino derivatives and intermediates 有权
标题翻译：合成（3-烷基-5-哌啶-1-基-3,3a-二氢 - 吡唑并[1,5-a]嘧啶-7-基） - 氨基衍生物和中间体的方法和中间体
公开(公告)号：US08076479B2
公开(公告)日：2011-12-13
申请号：US11893857
申请日：2007-08-17
申请人： Frank Xing Chen , Kartik M. Keertikar , Shen-Chun Kuo , Hong-Chang Lee , Ramani R. Raghavan , George G. Wu , Ji Xie
发明人： Frank Xing Chen , Kartik M. Keertikar , Shen-Chun Kuo , Hong-Chang Lee , Ramani R. Raghavan , George G. Wu , Ji Xie
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： Disclosed is a process for the synthesis of compounds of Formula I by sequentially aminating, first with a primary amine and then with a secondary amine, an intermediate compound of the structure of Formula E1, wherein R1 is a linear, branched, or cyclic alkyloxy functional group of the structure (—R2a—OH), R2a is a linear, branched or cyclic alkyl group, R2 is a linear, branched or cyclic alkyl group, and R3 is an alkylene-heterocycle, said process comprising forming intermediate compound of Formula E1 by reacting, in a refluxing reaction solvent selected from alcohols having 5 or less carbon atoms and mixtures of two or more thereof, a methanol solution of a salt of a 4-alkyl-3-amino-pyrazole compound of Formula C1, with a diamidization reagent selected from dimethylmalonate, monomethylmalonyl-chloride, and malonyl dichloride in the presence of a Lewis base having sufficient proton affinity to abstract a proton from the 1-position nitrogen on the pyrazole ring.
摘要翻译：公开了通过依次胺化伯胺，然后通过仲胺，式E1结构的中间体化合物，其中R 1是直链，支链或环烷基官能的化合物来合成式I化合物的方法（-R2a-OH）基，R2a是直链，支链或环状烷基，R2是直链，支链或环状的烷基，R3是亚烷基 - 杂环，所述方法包括形成式E1的中间体化合物通过使选自具有5个或更少碳原子的醇的回流反应溶剂及其两种或更多种的混合物，将式C1的4-烷基-3-氨基 - 吡唑化合物的盐与二酰胺化反应在具有足够的质子亲和力的路易斯碱存在下，选自丙二酸二甲酯，单甲基丙二酰氯和丙二酰氯的试剂从吡唑环上的1位氮抽出质子。

3. 发明授权

US06495689B2 Synthesis of intermediates useful in preparing tricyclic compounds 有权
标题翻译：可用于制备三环化合物的中间体的合成
公开(公告)号：US06495689B2
公开(公告)日：2002-12-17
申请号：US09886845
申请日：2001-06-21
申请人： Charles F. Bernard , Michael Casey , Frank Xing Chen , Denise C. Grogan , Marc Poirier , Robert P. Williams , Yee-Shing Wong , George G. Wu
发明人： Charles F. Bernard , Michael Casey , Frank Xing Chen , Denise C. Grogan , Marc Poirier , Robert P. Williams , Yee-Shing Wong , George G. Wu
IPC分类号： C07D22116
CPC分类号： C07D221/16
摘要： Disclosed is a process for preparing a compound having the formula: wherein R, R1, R2, R3, and R4 are independently selected from the group consisting of H, Br, Cl, F, alkyl, or alkoxy.
摘要翻译：公开了一种制备具有下式的化合物的方法：其中R，R 1，R 2，R 3和R 4独立地选自H，Br，Cl，F，烷基或烷氧基。

4. 发明授权

US06372909B1 Synthesis of intermediates useful in preparing tricyclic compounds 有权
标题翻译：可用于制备三环化合物的中间体的合成
公开(公告)号：US06372909B1
公开(公告)日：2002-04-16
申请号：US09442512
申请日：1999-11-18
申请人： Charles F. Bernard , Michael Casey , Frank Xing Chen , Denise C. Grogan , Marc Poirier , Robert P. Williams , Yee-Shing Wong , George G. Wu
发明人： Charles F. Bernard , Michael Casey , Frank Xing Chen , Denise C. Grogan , Marc Poirier , Robert P. Williams , Yee-Shing Wong , George G. Wu
IPC分类号： C07F980
CPC分类号： C07D221/16
摘要： Disclosed is a process for preparing a compound having the formula: wherein R, R1, R2, R3, and R4 are independently selected from the group consisting of H, Br, Cl, F, alkyl, or alkoxy, by (A) reacting a compound having the formula wherein RA, RC, RD, and RE are independently selected from the group consisting of H, halo, alkyl, or alkoxy, and R5 is aryl or heteroaryl, with a dehydrating agent to produce an imine having the formula: (B) hydrolyzing the imine produced in step (A) to produce the compound having formula (I). Also disclosed are novel intermediates having the formula: wherein RA, RB, RC, RD, and RE are independently selected from the group consisting of H, halo, alkyl, or alkoxy, and R5 is aryl or heteroaryl. Also disclosed is a process for preparing a compound having the formula: comprising: reacting a compound having the formula: with NH2R5 in the presence of a palladium catalyst, carbon monoxide, a base, and an ether selected from the group consisting of: CH3OCH2CH2OCH3; CH3OCH2CH2OCH2CH2OCH3; and CH3OCH2CH2OCH2CH2OCH2CH2OCH3, wherein X is H, Br, Cl, or F, and R5 is aryl or heteroaryl. The compounds made by these processes are useful intermediates for preparing compounds that are antihistamines or inhibitors of farnesyl protein transferase.
摘要翻译：公开了一种制备具有下式的化合物的方法：其中R，R 1，R 2，R 3和R 4独立地选自H，Br，Cl，F，烷基或烷氧基，通过（A）使具有下式的化合物其中RA，RC，RD和RE独立地选自H，卤素，烷基或烷氧基，R5是芳基或杂芳基，与脱水剂反应生成具有下式的亚胺：（B ）水解步骤（A）中产生的亚胺以制备具有式（I）的化合物。还公开了具有下式的新型中间体：其中RA，RB，RC，RD和RE独立地选自H，卤素，烷基或烷氧基，R5是芳基或杂芳基。还公开了制备具有下式的化合物的方法：包括：在钯催化剂，一氧化碳，碱和选自以下的醚的存在下使具有下式的化合物与NH 2 R 5反应：CH 3 OCH 2 CH 2 OCH 3; CH3OCH2CH2OCH2CH2OCH3; 和CH 3 OCH 2 CH 2 OCH 2 CH 2 OCH 2 CH 2 OCH 3，其中X是H，Br，Cl或F，R 5是芳基或杂芳基。通过这些方法制备的化合物是制备抗组胺剂或法呢基蛋白转移酶抑制剂的化合物的有用中间体。

5. 发明授权

US06288233B1 Enantioselective alkylation of tricyclic compounds 有权
标题翻译：三环化合物的对映选择性烷基化
公开(公告)号：US06288233B1
公开(公告)日：2001-09-11
申请号：US09667411
申请日：2000-09-21
申请人： Shen-Chun Kuo , Frank Xing Chen
发明人： Shen-Chun Kuo , Frank Xing Chen
IPC分类号： C07D22106
CPC分类号： C07D401/04 , C07D401/14 , Y02P20/55
摘要： Disclosed is a process for preparing a compound of the formula: wherein X1, X2, X3, X4, and X5 are independently selected from the group consisting of H, halo, alkyl, alkoxy, aryl, and aryloxy, and R is a protecting group, in which a compound having the formula wherein X1, X2, X3, X4, and X5 are as defined above, is treated with the following, in any sequence: (a) a non-nucleophilic strong base; (b) a chiral amino alcohol; and (c) a compound having the formula wherein L is a leaving group and R is as defined above. The compounds made by this process are useful intermediates for preparing compounds that are inhibitors of farnesyl protein transferase. Also disclosed is a compound having the formula:
摘要翻译：公开了一种制备下式化合物的方法：其中X 1，X 2，X 3，X 4和X 5独立地选自H，卤素，烷基，烷氧基，芳基和芳氧基，R是保护基其中具有如下定义的具有如下定义的化合物：（a）非亲核性强碱;（b）手性氨基醇（其中R 1，R 2，R 3，X 4， ; 和（c）具有甲醛的化合物L是离去基团，R如上定义。通过该方法制备的化合物是制备法呢基蛋白转移酶抑制剂的化合物的有用中间体。还公开了具有下式的化合物：

6. 发明申请

US20110124867A1 Process and intermediates for the Synthesis of heterocyclic Substituted Piperazines with CXCR3 Antagonist Activity 审中-公开
标题翻译：用CXCR3拮抗剂活性合成杂环取代的哌嗪的方法和中间体
公开(公告)号：US20110124867A1
公开(公告)日：2011-05-26
申请号：US12809101
申请日：2008-12-16
申请人： Frank Xing Chen , Timothy D. Cutarelli , Xiayong Fu , Xian Liang , Timothy L. McAllister , Robert K. Orr , Jianguo Yin , Kelvin H. Yong , Man Zhu
发明人： Frank Xing Chen , Timothy D. Cutarelli , Xiayong Fu , Xian Liang , Timothy L. McAllister , Robert K. Orr , Jianguo Yin , Kelvin H. Yong , Man Zhu
IPC分类号： C07D413/14 , C07D401/14 , C07D403/04 , C07D241/04 , C07D211/44
CPC分类号： C07D413/14 , C07D211/44 , C07D239/42 , C07D295/205
摘要： The present invention relates to novel processes for the preparation of the compound of the Formula A45: or a physiologically acceptable salt, solvate or prodrug thereof, which has utility, for example, as a pharmaceutically active compound with CXCR3 antagonist activity, and to novel intermediates useful in the synthesis thereof.
摘要翻译：本发明涉及制备式A45化合物或其生理上可接受的盐，溶剂合物或前体药物的新方法，其可用于例如具有CXCR3拮抗剂活性的药物活性化合物和新中间体可用于其合成。

7. 发明授权

US07582763B2 Enantioselective process 失效
标题翻译：对映选择性工艺
公开(公告)号：US07582763B2
公开(公告)日：2009-09-01
申请号：US11287041
申请日：2005-11-23
申请人： Frank Xing Chen , Yee-Shing Wong , Feng Liang , Marc Poirier , George Wu
发明人： Frank Xing Chen , Yee-Shing Wong , Feng Liang , Marc Poirier , George Wu
IPC分类号： C07D221/22
CPC分类号： C07D401/14 , C07D221/16
摘要： An enantioselective process for preparing intermediates useful in the preparation of the chiral tricyclic compound of formula I is disclosed.
摘要翻译：公开了用于制备可用于制备式I的手性三环化合物的中间体的对映选择性方法。

8. 发明授权

US07786306B2 Process for resolving chiral piperidine alcohol and process for synthesis of pyrazolo[1,5-a] pyrimidine derivatives using same 有权
标题翻译：用于拆分手性哌啶醇的方法和使用其合成吡唑并[1,5-a]嘧啶衍生物的方法
公开(公告)号：US07786306B2
公开(公告)日：2010-08-31
申请号：US11893850
申请日：2007-08-17
申请人： Frank Xing Chen , Maria M. Tamarez , Ji Xie
发明人： Frank Xing Chen , Maria M. Tamarez , Ji Xie
IPC分类号： C07D487/00 , C07D211/00
CPC分类号： C07D487/04 , C07D211/22 , C07D471/04
摘要： The present invention provides a method of resolving piperdin-yl-alkylene-alcohols, in high yield at high enantiomeric purity, for example 2-piperidin-2-yl-ethanol.
摘要翻译：本发明提供以高对映体纯度的高收率例如2-哌啶-2-基 - 乙醇来分解哌啶基 - 亚烷基 - 醇的方法。

9. 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：

10. 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：

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