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1. 发明申请

WO2003078417A1 PROCESS FOR SYNTHESIZING CHIRAL N-ARYL PIPERAZINES 审中-公开
标题翻译：合成N-芳基哌嗪的方法
公开(公告)号：WO2003078417A1
公开(公告)日：2003-09-25
申请号：PCT/US2003/007078
申请日：2003-03-10
申请人： WYETH, A CORPORATION OF THE STATE OF DELAWARE , FEIGELSON, Gregg, Brian , ZELDIS, Joseph , JIRKOVSKY, Ivo
发明人： FEIGELSON, Gregg, Brian , ZELDIS, Joseph , JIRKOVSKY, Ivo
IPC分类号： C07D319/18
CPC分类号： C07D405/12 , C07D319/18
摘要： A process for formation of N-aryl piperazines with chiral side-chains having the structure shown in formula below, and for making intermediate compounds therefor: (Formula I). In this process, chirality is introduced at the piperazine ring formation step and 2-aminopyridyl substitution is incorporated via displacement. The resulting N,N'-disubstituted piperazines act on the central nervous system at 5HT receptors.
摘要翻译：用具有下式结构所示结构的手性侧链形成N-芳基哌嗪的方法和用于制备其中间体化合物的方法：（式I）。在该方法中，在哌嗪环形成步骤中引入手性，通过置换并入2-氨基吡啶基取代。所得的N，N'-二取代的哌嗪作用于5HT受体的中枢神经系统。

2. 发明申请

WO03078396A8 PREPARATION OF N1-(2'-PYRIDYL)-1,2-PROPANEDIAMINE SULFAMIC ACID AND ITS USE IN THE SYNTHESIS OF BIOLOGICALLY ACTIVE PIPERAZINES 审中-公开
标题翻译： N1-（2'-吡啶基）-1,2-丙二胺磺酸的制备及其在生物活性哌嗪的合成中的应用
公开(公告)号：WO03078396A8
公开(公告)日：2004-01-29
申请号：PCT/US0307228
申请日：2003-03-10
申请人： WYETH CORP , CHAN ANITA WAI-YIN , FEIGELSON GREGG BRIAN , ZELDIS JOSEPH , JIRKOVSKY IVO
发明人： CHAN ANITA WAI-YIN , FEIGELSON GREGG BRIAN , ZELDIS JOSEPH , JIRKOVSKY IVO
IPC分类号： A61P25/00 , C07D213/74 , C07D213/75 , C07D213/76 , C07D405/12 , A61K31/44
CPC分类号： C07D213/74 , C07D213/75 , C07D213/76 , C07D405/12
摘要： A process for making an N1-(2'-pyridyl)-1,2-alkanediamine sulfamic acid of formula (II) by reacting a compound of formula (I) with NH2R', wherein R and R' are as defined in the specification. The invention also includes the compound of formula (II), and optical isomers thereof. The compound of formula (II) is an intermediate useful for making chiral piperazine derivatives which are active at the 5-HT1A receptor.
摘要翻译：通过使式（I）化合物与NH 2 R'反应制备式（II）的N1-（2'-吡啶基）-1,2-链烷二胺氨基磺酸的方法，其中R和R'如说明书中所定义。本发明还包括式（II）化合物及其旋光异构体。式（II）化合物是可用于制备在5-HT 1A受体上具有活性的手性哌嗪衍生物的中间体。

3. 发明申请

WO2003078420A3 PROCESS FOR MAKING CHIRAL 1,4-DISUBSTITUTED PIPERAZINES 审中-公开
公开(公告)号：WO2003078420A3
公开(公告)日：2003-09-25
申请号：PCT/US2003/007176
申请日：2003-03-10
申请人： WYETH , JIRKOVSKY, Ivo , ZELDIS, Joseph , FEIGELSON, Gregg, Brian
发明人： JIRKOVSKY, Ivo , ZELDIS, Joseph , FEIGELSON, Gregg, Brian
IPC分类号： C07D319/18
摘要： A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula (I) wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders.

4. 发明申请

WO2003078420A2 PROCESS FOR MAKING CHIRAL 1,4-DISUBSTITUTED PIPERAZINES 审中-公开
标题翻译：制备主要的1,4-取代哌嗪的方法
公开(公告)号：WO2003078420A2
公开(公告)日：2003-09-25
申请号：PCT/US2003/007176
申请日：2003-03-10
申请人： WYETH , JIRKOVSKY, Ivo , ZELDIS, Joseph , FEIGELSON, Gregg, Brian
发明人： JIRKOVSKY, Ivo , ZELDIS, Joseph , FEIGELSON, Gregg, Brian
IPC分类号： C07D401/00
CPC分类号： C07D487/10 , C07B2200/07 , C07C229/12 , C07C309/06 , C07D319/18
摘要： A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula (I) wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders.
摘要翻译：用于合成式（I）的光学活性1,4-二取代哌嗪的新型手性氮芥衍生物的立体选择性制备方法，其中R，Ar和Q如本文所述定义，及其中间体化合物。 1,4-二取代的哌嗪作为可用于治疗中枢神经系统（CNS）障碍的5HT1A受体结合剂。

5. 发明申请

WO2003078396A1 PREPARATION OF N1-(2’-PYRIDYL)-1,2-PROPANEDIAMINE SULFAMIC ACID AND ITS USE IN THE SYNTHESIS OF BIOLOGICALLY ACTIVE PIPERAZINES 审中-公开
标题翻译： N1-（2'-吡啶基）-1,2-丙二胺磺酸的制备及其在生物活性哌嗪的合成中的应用
公开(公告)号：WO2003078396A1
公开(公告)日：2003-09-25
申请号：PCT/US2003/007228
申请日：2003-03-10
申请人： WYETH , CHAN, Anita Wai-Yin , FEIGELSON, Gregg, Brian , ZELDIS, Joseph , JIRKOVSKY, Ivo
发明人： CHAN, Anita Wai-Yin , FEIGELSON, Gregg, Brian , ZELDIS, Joseph , JIRKOVSKY, Ivo
IPC分类号： C07D213/76
CPC分类号： C07D213/74 , C07D213/75 , C07D213/76 , C07D405/12
摘要： A process for making an N1-(2’-pyridyl)-1,2-alkanediamine sulfamic acid of formula (II) by reacting a compound of formula (I) with NH 2 R’, wherein R and R’ are as defined in the specification. The invention also includes the compound of formula (II), and optical isomers thereof. The compound of formula (II) is an intermediate useful for making chiral piperazine derivatives which are active at the 5-HT 1A receptor.
摘要翻译：通过使式（I）化合物与NH 2 R'反应制备式（II）的N1-（2'-吡啶基）-1,2-链烷二胺氨基磺酸的方法，其中R和R'如说明书中所定义。本发明还包括式（II）化合物及其旋光异构体。式（II）化合物是可用于制备在5-HT 1A受体上具有活性的手性哌嗪衍生物的中间体。

6. 发明申请

WO2005019201A2 PROCESS FOR THE PREPARATION OF 4-AMINO-3-QUINOLINECARBONITRILES 审中-公开
标题翻译：制备4-氨基-3-喹啉碳纳米管的方法
公开(公告)号：WO2005019201A2
公开(公告)日：2005-03-03
申请号：PCT/US2004/026329
申请日：2004-08-13
申请人： WYETH HOLDINGS CORPORATION , WIGGINS SUTHERLAND, Karen , FEIGELSON, Gregg, Brian , BOSCHELLI, Diane, Harris , BLUM, David, Michael , STRONG, Henry, Lee
发明人： WIGGINS SUTHERLAND, Karen , FEIGELSON, Gregg, Brian , BOSCHELLI, Diane, Harris , BLUM, David, Michael , STRONG, Henry, Lee
IPC分类号： C07D401/00
CPC分类号： C07D405/04 , C07D215/54 , C07D495/04
摘要： This invention discloses a process for the preparation of a 4-amino-3quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up-to tetra-substituted aniline in an alcoholic solvent and a trialkylorthoformate to yield an 2-amino-2-cyanoacrylamide; combining the 3-amino2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine6-carbonitrile comprising combining a 3-amino thiophene with a cyanoacetamide and trial kylorthoformate in an alcoholic solvent to obtain a 3-amino2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride and acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile and also discloses a process for the preparation of a 4 amino-3-quinolinecarbonitrile comprising: combining an amine compound with cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension; to yield cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline with an alcoholic solvent to yield a 4-amino-3-quinolinecarbonitrile, and the invention discloses a process for obtaining a cyanoacetamide.
摘要翻译：本发明公开了一种制备4-氨基-3-喹啉甲腈的方法，该方法包括将胺化合物与氰基乙酸和酸催化剂合并以得到氰基乙酰胺; 使氰基乙酰胺与任选地最多四取代的苯胺在醇溶剂和原甲酸三烷基酯中缩合，得到2-氨基-2-氰基丙烯酰胺; 将3-氨基-2-氰基丙烯酰胺与三氯氧磷在乙腈，丁腈，甲苯或二甲苯中合并，任选在催化剂存在下反应生成4-氨基-3-喹啉甲腈，并且还公开了制备7-氨基 - 噻吩并[ 包括将3-氨基噻吩与氰基乙酰胺和试验原甲酸酯在醇溶剂中混合以获得3-氨基-2-氰基丙烯酰胺; 并任选在催化剂存在下将3-氨基-2-氰基丙烯酰胺与三氯氧化磷和乙腈，丁腈，甲苯或二甲苯合并，得到7-氨基 - 噻吩并[3,2-b]吡啶-6-甲腈，和还公开了一种制备4-氨基-3-喹啉腈的方法，包括：将胺化合物与氰基乙酸和肽偶联剂组合以获得悬浮液; 过滤悬浮液; 生成氰基乙酰胺; 将氰基乙酰胺与任选至多四取代的苯胺与醇溶剂缩合，得到4-氨基-3-喹啉腈，本发明公开了一种获得氰基乙酰胺的方法。

7. 发明申请

WO2005019201A3 PROCESS FOR THE PREPARATION OF 4-AMINO-3-QUINOLINECARBONITRILES 审中-公开
标题翻译：制备4-氨基-3-喹啉酮的方法
公开(公告)号：WO2005019201A3
公开(公告)日：2005-08-04
申请号：PCT/US2004026329
申请日：2004-08-13
申请人： WYETH CORP , WIGGINS SUTHERLAND KAREN , FEIGELSON GREGG BRIAN , BOSCHELLI DIANE HARRIS , BLUM DAVID MICHAEL , STRONG HENRY LEE
发明人： WIGGINS SUTHERLAND KAREN , FEIGELSON GREGG BRIAN , BOSCHELLI DIANE HARRIS , BLUM DAVID MICHAEL , STRONG HENRY LEE
IPC分类号： C07D215/54 , C07D405/04 , C07D495/04
CPC分类号： C07D405/04 , C07D215/54 , C07D495/04
摘要： This invention discloses a process for the preparation of a 4-amino-3quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up-to tetra-substituted aniline in an alcoholic solvent and a trialkylorthoformate to yield an 2-amino-2-cyanoacrylamide; combining the 3-amino2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine6-carbonitrile comprising combining a 3-amino thiophene with a cyanoacetamide and trial kylorthoformate in an alcoholic solvent to obtain a 3-amino2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride and acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile and also discloses a process for the preparation of a 4 amino-3-quinolinecarbonitrile comprising: combining an amine compound with cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension; to yield cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline with an alcoholic solvent to yield a 4-amino-3-quinolinecarbonitrile, and the invention discloses a process for obtaining a cyanoacetamide.
摘要翻译：本发明公开了一种制备4-氨基-3-喹啉腈的方法，包括将胺化合物与氰基乙酸和酸催化剂混合以产生氰基乙酰胺; 将氰基乙酰胺与醇溶剂和原甲酸三烷基酯中的任选的上述四取代的苯胺缩合，得到2-氨基-2-氰基丙烯酰胺; 将3-氨基-2-氰基丙烯酰胺与磷酰氯在乙腈，丁腈，甲苯或二甲苯中，任选在催化剂存在下合并，得到4-氨基-3-喹啉腈，并公开了制备7-氨基 - 噻吩并[ 3,2-b]吡啶-6-甲腈，其包括将3-氨基噻吩与氰基乙酰胺组合并在醇溶剂中试验草酸甲酯，得到3-氨基-2-氰基丙烯酰胺; 并将3-氨基-2-氰基丙烯酰胺与磷酰氯和乙腈，丁腈，甲苯或二甲苯组合，任选在催化剂存在下，得到7-氨基 - 噻吩并[3,2-b]吡啶-6-甲腈和还公开了一种制备4氨基-3-喹啉腈的方法，包括：将胺化合物与氰基乙酸和肽偶联剂混合以获得悬浮液; 过滤悬浮液; 得到氰基乙酰胺; 将氰基乙酰胺与任选至多四取代的苯胺与醇溶剂缩合，得到4-氨基-3-喹啉腈，本发明公开了一种获得氰基乙酰胺的方法。

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