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公开(公告)号：US06506908B2
公开(公告)日：2003-01-14
申请号：US09838989
申请日：2001-04-20
IPC分类号： C07D33302
CPC分类号： C07D213/81 , C07C45/673 , C07C49/747 , C07C51/09 , C07C57/60 , C07C67/317 , C07C67/343 , C07C69/65 , C07C69/738 , C07C69/757 , C07C245/18 , C07C2601/08 , C07C2602/18 , C07D239/28 , C07D263/16
摘要： Processes are disclosed for preparing 3-hydroxymethylcyclopentanone compounds, which are useful as intermediates in the preparation of HIV chemokine CCR-5 receptor antagonists. A process is described in which the compounds are prepared by opening the cyclopropyl ring of a (1-alkoxycarbonyl-2-oxo)-trans-bicyclo[3.1.0]hexane compound by addition of a nucleophile to the cyclopropyl ring, and then decarboxylating the resulting 2-alkoxycarbonyl-3-(Nu-methyl)-cyclopentanone (Nu=the added nucleophilic group) via base solvolysis. Also described is a process for preparing the bicyclo[3.1.0]hexane precursors by the catalyzed cyclopropanation of a suitable alpha-diazo-beta-ketoester. The preparation of the alpha-diazo-beta-ketoesters and precursors thereto are also disclosed.
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公开(公告)号：US06706885B2
公开(公告)日：2004-03-16
申请号：US10191042
申请日：2002-06-05
申请人： Nobuyoshi Yasuda , Michael Palucki , Yi Xiao , Frederick W. Hartner , Lushi Tan
发明人： Nobuyoshi Yasuda , Michael Palucki , Yi Xiao , Frederick W. Hartner , Lushi Tan
IPC分类号： C07D21353
CPC分类号： C07D213/40 , C07D213/38 , C07D401/14
摘要： A novel process is provided for the preparation of optionally protected 2,5-di-(3′-aminopropyl)-pyridines which are useful in the synthesis of &agr;v integrin receptor antagonists. Also provided are useful intermediates obtained from the process.
摘要翻译： 提供了用于制备可用于合成αphav整联蛋白受体拮抗剂的任选受保护的2,5-二（3'-氨基丙基） - 吡啶的新方法。 还提供了从该方法获得的有用的中间体。
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3.发明授权Process and intermediates for the preparation of imidazolidinone &agr;v integrin antagonists 失效用于制备咪唑啉酮阿拉夫综合素拮抗剂的方法和中间体公开(公告)号：US06407241B1
公开(公告)日：2002-06-18
申请号：US09707403
申请日：2000-11-07
申请人： Mark S Jensen , Michael Palucki , Nelo R. Rivera , Kenneth M. Wells , Yi Xiao , Yaling Wang , Chunhua Yang , Nobuyoshi Yasuda
发明人： Mark S Jensen , Michael Palucki , Nelo R. Rivera , Kenneth M. Wells , Yi Xiao , Yaling Wang , Chunhua Yang , Nobuyoshi Yasuda
IPC分类号： C07D47104
CPC分类号： C07D213/64 , C07D471/04
摘要： A novel process is provided for the preparation of imidazolidinone &agr;v&bgr;3/&agr;v&bgr;5 integrin antagonists, and the useful intermediates obtained therein. These compounds are antagonists of &agr;v&bgr;3/&agr;v&bgr;5 integrin receptors and thus useful for inhibiting bone resorption and treating and preventing osteoporosis. Also disclosed is 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3(S)-(6-methoxy-pyridin-3-yl)-propionic acid in the form of a hemihydrate.
摘要翻译： 提供了一种新的制备咪唑啉酮αphavbeta3/ alphavbeta5整联蛋白拮抗剂及其中获得的有用中间体的方法。 这些化合物是alphavbeta3 / alphavbeta5整联蛋白受体的拮抗剂，因此可用于抑制骨吸收和治疗和预防骨质疏松症。 还公开了3- {2-氧代-3- [3-（5,6,7,8-四氢 - [1,8]萘啶-2-基） - 丙基]咪唑烷-1-基} -3（S ） - 半水合物形式的（6-甲氧基 - 吡啶-3-基） - 丙酸。
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![Process and intermediates to a tetrahydro-[1,8]-naphthyridine](/abs-image/US/2001/07/17/US06262268B1/abs.jpg.150x150.jpg)
公开(公告)号：US06262268B1
公开(公告)日：2001-07-17
申请号：US09709083
申请日：2000-11-09
IPC分类号： C07D21338
CPC分类号： C07D213/40 , C07D213/38 , C07D471/04
摘要： A novel process is provided for the preparation of 3-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-propylamine which is useful in the synthesis of &agr;v integrin receptor antagonists. Also provided are useful intermediates obtained from the process.
摘要翻译： 提供了一种制备3-（5,6,7,8-四氢 - [1,8] - 萘啶-2-基） - 丙胺的新方法，其可用于合成αphav整联蛋白受体拮抗剂。 还提供了从该方法获得的有用的中间体。
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公开(公告)号：US07026498B2
公开(公告)日：2006-04-11
申请号：US10004101
申请日：2001-10-23
IPC分类号： C07F7/04 , C07F9/02 , C07C255/47 , C07C273/02
CPC分类号： C07C1/26 , C07C1/321 , C07C17/16 , C07C17/263 , C07C29/32 , C07C29/38 , C07C37/18 , C07C41/30 , C07C45/68 , C07C45/71 , C07C49/675 , C07C67/31 , C07C201/12 , C07C209/10 , C07C209/18 , C07C211/59 , C07C213/02 , C07C213/08 , C07C221/00 , C07C225/12 , C07C227/08 , C07C227/18 , C07C231/08 , C07C231/12 , C07C249/02 , C07C249/16 , C07C251/24 , C07C253/30 , C07C2531/24 , C07C2531/26 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D213/50 , C07D213/72 , C07D213/74 , C07D295/023 , C07D295/033 , C07D295/096 , C07D295/112 , C07D295/13 , C07D295/155 , C07D307/33 , C07D317/22 , C07D317/26 , C07D317/66 , C07D333/08 , C07D333/66 , C07D401/04 , C07F7/1892 , C07F9/4875 , C07F9/5022 , C07F9/5027 , C07F9/5728 , C07F9/653 , C07F9/6547 , C07F9/65719 , C07F15/0066 , C07C25/18 , C07C49/255 , C07C49/213 , C07C49/657 , C07C49/67 , C07C49/84 , C07C49/245 , C07C49/755 , C07C49/215 , C07C49/683 , C07C47/575 , C07C49/782 , C07C69/92 , C07C211/48 , C07C211/55 , C07C217/40 , C07C217/84 , C07C217/92 , C07C225/22 , C07C229/36 , C07C229/60 , C07C233/07 , C07C235/46 , C07C251/86 , C07C255/33 , C07C255/50 , C07C255/54 , C07C255/56 , C07C255/58 , C07C15/14 , C07C35/21 , C07C33/24 , C07C205/04 , C07C205/06 , C07C43/205 , C07C43/225 , C07C39/15 , C07C35/08
摘要： One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.
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公开(公告)号：US07718796B2
公开(公告)日：2010-05-18
申请号：US12226113
申请日：2007-04-06
IPC分类号： C07D401/14 , C07D471/04
CPC分类号： C07D223/12 , C07D471/04
摘要： An efficient syntheses for the preparation of (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one.
摘要翻译： （3R，6S）-3-氨基-6-（2,3-二氟苯基）-1-（2,2,2-三氟乙基）氮杂环庚烷-2-酮的制备的有效合成。
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公开(公告)号：US07560582B2
公开(公告)日：2009-07-14
申请号：US11781651
申请日：2007-07-23
CPC分类号： C07C1/26 , C07C1/321 , C07C17/16 , C07C17/263 , C07C29/32 , C07C29/38 , C07C37/18 , C07C41/30 , C07C45/68 , C07C45/71 , C07C49/675 , C07C67/31 , C07C201/12 , C07C209/10 , C07C209/18 , C07C211/59 , C07C213/02 , C07C213/08 , C07C221/00 , C07C225/12 , C07C227/08 , C07C227/18 , C07C231/08 , C07C231/12 , C07C249/02 , C07C249/16 , C07C251/24 , C07C253/30 , C07C2531/24 , C07C2531/26 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D213/50 , C07D213/72 , C07D213/74 , C07D295/023 , C07D295/033 , C07D295/096 , C07D295/112 , C07D295/13 , C07D295/155 , C07D307/33 , C07D317/22 , C07D317/26 , C07D317/66 , C07D333/08 , C07D333/66 , C07D401/04 , C07F7/1892 , C07F9/4875 , C07F9/5022 , C07F9/5027 , C07F9/5728 , C07F9/653 , C07F9/6547 , C07F9/65719 , C07F15/0066 , C07C25/18 , C07C49/255 , C07C49/213 , C07C49/657 , C07C49/67 , C07C49/84 , C07C49/245 , C07C49/755 , C07C49/215 , C07C49/683 , C07C47/575 , C07C49/782 , C07C69/92 , C07C211/48 , C07C211/55 , C07C217/40 , C07C217/84 , C07C217/92 , C07C225/22 , C07C229/36 , C07C229/60 , C07C233/07 , C07C235/46 , C07C251/86 , C07C255/33 , C07C255/50 , C07C255/54 , C07C255/56 , C07C255/58 , C07C15/14 , C07C35/21 , C07C33/24 , C07C205/04 , C07C205/06 , C07C43/205 , C07C43/225 , C07C39/15 , C07C35/08
摘要： One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.
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8.发明授权公开(公告)号：US06395916B1
公开(公告)日：2002-05-28
申请号：US09113478
申请日：1998-07-10
IPC分类号： C07F704
CPC分类号： C07D213/74 , C07C1/26 , C07C17/263 , C07C41/30 , C07C45/68 , C07C45/71 , C07C67/31 , C07C201/12 , C07C209/10 , C07C209/18 , C07C211/59 , C07C213/02 , C07C213/08 , C07C221/00 , C07C225/12 , C07C227/08 , C07C227/18 , C07C231/12 , C07C249/02 , C07C249/16 , C07C251/24 , C07C253/30 , C07C2601/02 , C07C2601/08 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D213/50 , C07D213/72 , C07D295/023 , C07D295/033 , C07D295/096 , C07D295/112 , C07D295/13 , C07D295/155 , C07D307/33 , C07D317/22 , C07D317/26 , C07D317/66 , C07D333/08 , C07D333/66 , C07D401/04 , C07F7/1892 , C07F9/4875 , C07F9/5022 , C07F9/5027 , C07F9/5728 , C07F9/653 , C07F9/6547 , C07F9/65719 , C07F15/0066 , C07C25/18 , C07C49/255 , C07C49/213 , C07C49/657 , C07C49/67 , C07C49/84 , C07C49/245 , C07C49/755 , C07C49/215 , C07C49/683 , C07C47/575 , C07C49/782 , C07C69/92 , C07C211/48 , C07C211/55 , C07C217/40 , C07C217/84 , C07C217/92 , C07C225/22 , C07C229/36 , C07C229/60 , C07C233/07 , C07C235/46 , C07C251/86 , C07C255/33 , C07C255/50 , C07C255/54 , C07C255/56 , C07C255/58 , C07C205/04 , C07C205/06 , C07C43/225 , C07C43/205
摘要： One aspect of the present invention relates to novel, electron-rich bidentate ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.
摘要翻译： 本发明的一个方面涉及用于过渡金属的新型富电子二齿配位体。 本发明的第二方面涉及包含这些配体的催化剂在过渡金属催化的碳 - 杂原子和碳 - 碳键形成反应中的用途。 本发明方法提供了过渡金属催化反应的许多特征的改进，包括合适底物的范围，反应条件和效率。
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9.发明申请Process for the Preparation of Pyridine Heterocycle Cgrp Antagonist Intermediate 审中-公开制备吡啶杂环Cgrp拮抗剂中间体的方法公开(公告)号：US20090176986A1
公开(公告)日：2009-07-09
申请号：US12226126
申请日：2007-04-06
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： An efficient syntheses for the preparation of the intermediate 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride, and other salt forms of 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine.
摘要翻译： 制备中间体2-氧代-1-（4-哌啶基）-2,3-二氢-1H-咪唑并[4,5-b]吡啶二盐酸盐和其它盐形式的2-氧代-1 - （4-哌啶基）-2,3-二氢-1H-咪唑并[4,5-b]吡啶。
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公开(公告)号：US20080033171A1
公开(公告)日：2008-02-07
申请号：US11781651
申请日：2007-07-23
申请人： Stephen Buchwald , David Old , John Wolfe , Michael Palucki , Ken Kamikawa
发明人： Stephen Buchwald , David Old , John Wolfe , Michael Palucki , Ken Kamikawa
IPC分类号： C07D295/00 , C07D211/70 , C07F7/04 , C07F9/02
CPC分类号： C07C1/26 , C07C1/321 , C07C17/16 , C07C17/263 , C07C29/32 , C07C29/38 , C07C37/18 , C07C41/30 , C07C45/68 , C07C45/71 , C07C49/675 , C07C67/31 , C07C201/12 , C07C209/10 , C07C209/18 , C07C211/59 , C07C213/02 , C07C213/08 , C07C221/00 , C07C225/12 , C07C227/08 , C07C227/18 , C07C231/08 , C07C231/12 , C07C249/02 , C07C249/16 , C07C251/24 , C07C253/30 , C07C2531/24 , C07C2531/26 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D213/50 , C07D213/72 , C07D213/74 , C07D295/023 , C07D295/033 , C07D295/096 , C07D295/112 , C07D295/13 , C07D295/155 , C07D307/33 , C07D317/22 , C07D317/26 , C07D317/66 , C07D333/08 , C07D333/66 , C07D401/04 , C07F7/1892 , C07F9/4875 , C07F9/5022 , C07F9/5027 , C07F9/5728 , C07F9/653 , C07F9/6547 , C07F9/65719 , C07F15/0066 , C07C25/18 , C07C49/255 , C07C49/213 , C07C49/657 , C07C49/67 , C07C49/84 , C07C49/245 , C07C49/755 , C07C49/215 , C07C49/683 , C07C47/575 , C07C49/782 , C07C69/92 , C07C211/48 , C07C211/55 , C07C217/40 , C07C217/84 , C07C217/92 , C07C225/22 , C07C229/36 , C07C229/60 , C07C233/07 , C07C235/46 , C07C251/86 , C07C255/33 , C07C255/50 , C07C255/54 , C07C255/56 , C07C255/58 , C07C15/14 , C07C35/21 , C07C33/24 , C07C205/04 , C07C205/06 , C07C43/205 , C07C43/225 , C07C39/15 , C07C35/08
摘要： One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.
摘要翻译： 本发明的一个方面涉及用于过渡金属的新配体。 本发明的第二方面涉及包含这些配体的催化剂在过渡金属催化的碳 - 杂原子和碳 - 碳键形成反应中的用途。 本发明方法提供了过渡金属催化反应的许多特征的改进，包括合适底物的范围，反应条件和效率。
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