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1. 发明申请

WO2004035575A8 PROCESS FOR THE PREPARATION OF (S,S)-CIS-2-BENZHYDRYL-3-BENZYLAMINOQUINUCLIDINE 审中-公开
标题翻译：制备（S，S）-CIS-2-苯甲酰基-3-苯甲酰氨基胆碱的方法
公开(公告)号：WO2004035575A8
公开(公告)日：2005-05-12
申请号：PCT/US0332275
申请日：2003-10-10
申请人： PFIZER PROD INC , DSM PHARMACEUTICALS INC , NUGENT THOMAS C , SEEMAYER ROBERT
发明人： NUGENT THOMAS C , SEEMAYER ROBERT
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： A process for preparing (S,S)-cis-2-benzhydryl-3-benzylaminoquinuclidine. The process includes the steps of contacting a compound containing a mixture of R- and S-isomers and having Formula (I), with an effective amount of a chiral organic acid in the presence of an organic solvent and an effective amount of an organic carboxylic acid for converting the R-isomer into an acid salt of the S isomer, wherein the organic solvent is capable of solubilizing the compound containing the mixture of R- and S-isomers, while precipitating the acid salt and the organic carboxylic acid is different from the chiral organic acid; neutralizing the acid salt with a base to provide an S-isomer of a chiral ketone of Formula (II), and reacting the chiral ketone with an organic amine in the presence of a Lewis acid to provide the corresponding imine and reducing the imine.
摘要翻译：制备（S，S） - 顺式-2-二苯甲基-3-苄基氨基奎宁环的方法。该方法包括以下步骤：在有机溶剂和有效量的有机羧酸的存在下，将含有R-和S-异构体的混合物和具有式（I）的化合物与有效量的手性有机酸接触用于将R-异构体转化为S异构体的酸性盐的酸，其中有机溶剂能够溶解含有R-和S-异构体的混合物的化合物，同时沉淀酸盐和有机羧酸不同于手性有机酸; 用碱中和酸盐以提供式（II）的手性酮的S-异构体，并在路易斯酸存在下使手性酮与有机胺反应，得到相应的亚胺并还原亚胺。

2. 发明申请

WO2004037174A3 PROCESS FOR THE PREPARATION OF (S,S)-CIS-2-PHENYL-3-AMINOPIPERIDINE 审中-公开
标题翻译：制备（S，S）-CIS-2-苯基-3-氨基哌啶的方法
公开(公告)号：WO2004037174A3
公开(公告)日：2004-08-12
申请号：PCT/US0332620
申请日：2003-10-15
申请人： PFIZER PROD INC , DSM PHARMACEUTICALS INC , NUGENT THOMAS C , SEEMAYER ROBERT , LIANG JACK
发明人： NUGENT THOMAS C , SEEMAYER ROBERT , LIANG JACK
IPC分类号： C07D211/56 , C07D211/98
CPC分类号： C07D211/56 , Y02P20/55
摘要： The present invention is directed to a process for preparing (S,S)-cis-2-phenyl-3-aminopiperidine which comprises: (a) reacting the amino acid, ornithine or salt having a protecting group on the amino groups on the alpha and delta carbons thereof, having the formula (I) with N-methoxy-N-methylamino or salt thereof under amide forming conditions to produce an amide of the formula in the S configuration (II) (b) adding said amide to an effective amount of a Grignard reagent of the formula Ph MgX to form a ketone of the formula in the S configuration (III) (c) selectively deprotecting the amino group on the delta carbon under conditions sufficient to cyclize said ketone to form a cyclic imine and reducing the resulting imine to form a product of the formula in the (S,S) configuration (IV) and (d) removing the amino protecting group on the alpha-carbon to form said (S,S)-cis-2-phenyl-3-aminopiperidine, wherein P1 and P2 are different amino protecting groups, which are removed under different reaction conditions and X is halide. When P1 is t-butyloxycarbonyl the above process is also used to prepare (S,S)-cis-2-phenyl-3-tertbutoxycarbonylaminopiperidine.
摘要翻译：本发明涉及一种制备（S，S） - 顺-2-苯基-3-氨基哌啶的方法，其包括：（a）使氨基酸，鸟氨酸或具有保护基的盐在α 和其碳原子在酰胺形成条件下具有式（I）的N-甲氧基-N-甲基氨基或其盐，以在S构型（II）（b）中制备下式的酰胺：（b）将所述酰胺加入有效量的式Ph MgX的格氏试剂以形成S构型（III）中的下式的酮（c）在足以使所述酮环化以形成环状亚胺的条件下选择性地使δ碳上的氨基脱保护并还原得到亚胺以形成（S，S）构型（IV）和（d）中的式的产物，除去α-碳上的氨基保护基，形成所述（S，S） - 顺-2-苯基-3 - 氨基哌啶，其中P1和P2是不同的氨基保护基，其在不同的情况下被除去 nt反应条件，X是卤化物。当P1是叔丁氧基羰基时，上述方法也用于制备（S，S） - 顺式-2-苯基-3-叔丁氧羰基氨基哌啶。

3. 发明申请

WO2004037174A2 PROCESS FOR THE PREPARATION OF (S,S)-CIS-2-PHENYL-3-AMINOPIPERIDINE 审中-公开
标题翻译：（S，S） - 顺式-2-苯基-3-氨基哌啶的制备方法
公开(公告)号：WO2004037174A2
公开(公告)日：2004-05-06
申请号：PCT/US2003/032620
申请日：2003-10-15
申请人： PFIZER PRODUCTS, INC. , DSM PHARMACEUTICALS, INC. , NUGENT, Thomas, C. , SEEMAYER, Robert , LIANG, Jack
发明人： NUGENT, Thomas, C. , SEEMAYER, Robert , LIANG, Jack
IPC分类号： A61K
CPC分类号： C07D211/56 , Y02P20/55
摘要： The present invention is directed to a process for preparing (S,S)-cis-2-phenyl-3-aminopiperidine which comprises: (a) reacting the amino acid, ornithine or salt having a protecting group on the amino groups on the α and δ carbons thereof, having the formula (I) with N-methoxy-N-methylamino or salt thereof under amide forming conditions to produce an amide of the formula in the S configuration (II) (b) adding said amide to an effective amount of a Grignard reagent of the formula Ph MgX to form a ketone of the formula in the S configuration (III) (c) selectively deprotecting the amino group on the δ carbon under conditions sufficient to cyclize said ketone to form a cyclic imine and reducing the resulting imine to form a product of the formula in the (S,S) configuration (IV) and (d) removing the amino protecting group on the α-carbon to form said (S,S)-cis-2-phenyl-3-aminopiperidine, wherein P 1 and P 2 are different amino protecting groups, which are removed under different reaction conditions and X is halide. When P 1 is t-butyloxycarbonyl the above process is also used to prepare (S,S)-cis-2-phenyl-3-tertbutoxycarbonylaminopiperidine.
摘要翻译：本发明涉及制备（S，S） - 顺式-2-苯基-3-氨基哌啶的方法，其包括：（a）使具有保护基的氨基酸，鸟氨酸或盐（I）与N-甲氧基-N-甲基氨基或其盐在酰胺形成条件下反应，生成式（II）的通式（II）的酰胺（b ）将所述酰胺加入到有效量的式PhMgX的格氏试剂中以形成S构型（III）中的式（III）的酮：（c）在足以环化所述酮的条件下选择性地将δ碳上的氨基脱保护（S，S）构型（IV）和（d）除去α-碳上的氨基保护基以形成所述（S，S）构型的产物， - 顺-2-苯基-3-氨基哌啶，其中P 1和P 2是不同的氨基保护基，其中a 在不同反应条件下重新除去，X是卤化物。当P 1为叔丁氧基羰基时，上述方法也用于制备（S，S） - 顺式-2-苯基-3-叔丁氧基羰基氨基哌啶。

4. 发明申请

WO2004035575A1 PROCESS FOR THE PREPARATION OF (S,S)-CIS-2-BENZHYDRYL-3-BENZYLAMINOQUINUCLIDINE 审中-公开
标题翻译：制备（S，S）-CIS-2-苯甲酰基-3-苯甲酰氨基胆碱的方法
公开(公告)号：WO2004035575A1
公开(公告)日：2004-04-29
申请号：PCT/US2003/032275
申请日：2003-10-10
申请人： PFIZER PRODOUCTS, INC , DSM PHARMACEUTICALS, INC. , NUGENT, Thomas, C. , SEEMAYER, Robert
发明人： NUGENT, Thomas, C. , SEEMAYER, Robert
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： A process for preparing (S,S)-cis-2-benzhydryl-3-benzylaminoquinuclidine. The process includes the steps of contacting a compound containing a mixture of R- and S-isomers and having Formula (I), with an effective amount of a chiral organic acid in the presence of an organic solvent and an effective amount of an organic carboxylic acid for converting the R-isomer into an acid salt of the S isomer, wherein the organic solvent is capable of solubilizing the compound containing the mixture of R- and S-isomers, while precipitating the acid salt and the organic carboxylic acid is different from the chiral organic acid; neutralizing the acid salt with a base to provide an S-isomer of a chiral ketone of Formula (II), and reacting the chiral ketone with an organic amine in the presence of a Lewis acid to provide the corresponding imine and reducing the imine.
摘要翻译：制备（S，S） - 顺式-2-二苯甲基-3-苄基氨基奎宁环的方法。该方法包括以下步骤：在有机溶剂和有效量的有机羧酸的存在下，将含有R-和S-异构体的混合物和具有式（I）的化合物与有效量的手性有机酸接触用于将R-异构体转化为S异构体的酸性盐的酸，其中有机溶剂能够溶解含有R-和S-异构体的混合物的化合物，同时沉淀酸盐和有机羧酸不同于手性有机酸; 用碱中和酸盐以提供式（II）的手性酮的S-异构体，并在路易斯酸存在下使手性酮与有机胺反应，得到相应的亚胺并还原亚胺。

5. 发明申请

WO03062181A8 PROCESS FOR THE PREPARATION OF NONRACEMIC SYN-1-(4-HYDROXY-PHENYL)-2-(4-HYDROXY-4-PHENYL.PIPERIDIN-1Yl)-1-PROPANOL COMPOUNDS 审中-公开
标题翻译：制备非线性SYN-1-（4-羟基苯基）-2-（4-羟基-4-苯基 - 哌啶-1-基）-1-丙醇化合物的方法
公开(公告)号：WO03062181A8
公开(公告)日：2004-07-08
申请号：PCT/US0302290
申请日：2003-01-24
申请人： DSM PHARMACEUTICALS INC , PFIZER PROD INC , TUCKER CHARLES E , JIANG QIONGZHONG
发明人： TUCKER CHARLES E , JIANG QIONGZHONG
IPC分类号： B01J31/02 , B01J31/18 , B01J31/22 , B01J31/24 , C07B53/00 , C07B61/00 , C07C29/143 , C07C29/145 , C07D211/52 , C07D277/24 , C07D307/44 , C07D333/16 , C07D333/56 , C07F9/38 , C07F15/00 , C07C33/34 , C07C257/10 , C07C279/04 , C07C279/16 , C07D239/00 , C07F9/06 , C07F9/6584
CPC分类号： C07F15/0053 , B01J31/1805 , B01J31/226 , B01J31/24 , B01J31/2409 , B01J2231/643 , B01J2531/821 , C07B53/00 , C07B2200/07 , C07C29/143 , C07C29/145 , C07D211/52 , C07D277/24 , C07D307/44 , C07D333/16 , C07D333/56 , C07F9/3813
摘要： the present invention provides a process for the preparation of a nonracemic diastereorner of 1-(4-benezoxy-phenyl)-2-(4-hydroxy-4-phenyl-piperidin-1-yl)-1-propanol by hydrogenation of a corresponding noracemic 1-(4-benzoxy-phenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-1-propane using a catalyst system comprising ruthenium, a nonracemic diphosphine ligand, a bidentate amine ligand selected from amino-thioethers and achiral diamines, and a base.
摘要翻译：本发明提供了通过相应的氢化制备1-（4-苯氧基 - 苯基）-2-（4-羟基-4-苯基 - 哌啶-1-基）-1-丙醇的非芳香非对映体的方法使用包含钌，非环状二膦配体，二齿胺配位体的催化剂体系的非芳族1-（4-苯氧基 - 苯基）-2-（4-羟基-4-苯基哌啶-1-基）-1-丙烷，氨基 - 硫醚和非手性二胺，以及碱。

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