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1. 发明申请

WO2004031168A2 PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF OPTICALLY ACTIVE 3-AMINO-1-(2-THIENYL)-1-PROPANOL DERIVATIVES 审中-公开
标题翻译：制备光学活性3-氨基-1-（2-噻吩基）-1-丙醇衍生物的方法和中间体
公开(公告)号：WO2004031168A2
公开(公告)日：2004-04-15
申请号：PCT/EP2003/011073
申请日：2003-10-07
申请人： LONZA AG , FUCHS, Rudolf , MICHEL, Dominique , BRIEDEN, Walter
发明人： FUCHS, Rudolf , MICHEL, Dominique , BRIEDEN, Walter
IPC分类号： C07D333/20
CPC分类号： C07D493/14 , C07D333/20
摘要： Enantiomerically enriched 3-amino-1-(2-thienyl)-1-propanols of the fomulae (S)-I or (R)-I wherein R 1 and R 2 independently denote H, C 1-6 -alkyl, C 5-7 -cycloalkyl, aralkyl or aryl, were prepared by reducing a 3-amino-1-(2-thienyl)-1-propanone of the formula (II) wherein R 1 and R 2 are defined as above, using a hydrogen donor in the presence of a metal catalyst, an optically active nitrogen-containing ligand and optionally a base.
摘要翻译：式（S）-I或（R）-I对映异构体富集的3-氨基-1-（2-噻吩基）-1-丙醇其中R 1和R 2独立地表示H，C 1-6 - 烷基，C 5-7 - 环烷基，芳烷基或芳基，通过将式（II）的3-氨基-1-（2-噻吩基）-1-丙酮还原，其中R 1和R 2定义为在金属催化剂，光学活性含氮配体和任选的碱的存在下使用氢供体。

2. 发明申请

WO2005080370A1 PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY PURE 1-SUBSTITUTED-3-AMINOALCOHOLS 审中-公开
标题翻译：制备纯化1-取代的3-氨基醇的方法
公开(公告)号：WO2005080370A1
公开(公告)日：2005-09-01
申请号：PCT/EP2005/001781
申请日：2005-02-21
申请人： LONZA AG , MICHEL, Dominique , METTLER, Hanspeter , MCGARRITY, John
发明人： MICHEL, Dominique , METTLER, Hanspeter , MCGARRITY, John
IPC分类号： C07D333/20
CPC分类号： C07C213/00 , C07B2200/07 , C07D333/22
摘要： Provided is a process for the preparation of enantiomerically pure 1-substituted-3-aminoalcohols, particularly of (S)-(-)- and (R)-(+)-3- N -methylamino-l-(2-thienyl)-1-propanol, by asymmetrically hydrogenating salts of a carboxylic acids with an aminoketone of formula (II), wherein R 1 is selected from the group consisting of 2-thienyl, 2-furanyl and phenyl, each optionally substituted with one or more halogen atoms and/or one or more C 1-4 -alkoxy groups, and wherein R 2 is C 1-4 -alkyl or phenyl, each optionally substituted with one or more halogen atoms and/or one or more C 1-4 -alkyl or C 1-4 -alkoxy groups, and wherein the corresponding aminoalcohols are obtained by subsequent hydrolysis of their salts. Furthermore provided are salts of a carboxylic acid with said aminoketones and the aminoalcohols obtained by asymmetriacally hydrogenating said aminoketones, respectively.
摘要翻译：提供了制备对映体纯的1-取代-3-氨基醇，特别是（S） - （ - ） - 和（R） - （+） - 3-N-甲基氨基-1-（2-噻吩基） -1-丙醇，通过用式（II）的氨基酮不对称氢化羧酸盐，其中R 1选自2-噻吩基，2-呋喃基和苯基，各自任选被一个或多个更多的卤素原子和/或一个或多个C 1-4 - 烷氧基，并且其中R 2是C 1-4 - 烷基或苯基，各自任选被一个或多个卤素原子和/或一个或多个C 1-4 - 烷基或C 1-4 - 烷氧基，并且其中相应的氨基醇通过其盐的随后水解获得。此外，还提供了羧酸与所述氨基酮和通过不对称地氢化所述氨基酮而获得的氨基醇的盐。

3. 发明申请

WO2004005239A1 PROCESS FOR THE PREPARATION OF N-MONOSUBSTITUTED β-AMINO ALCOHOLS 审中-公开
标题翻译：制备N-单体制备的β-氨基醇的方法
公开(公告)号：WO2004005239A1
公开(公告)日：2004-01-15
申请号：PCT/EP2003/007411
申请日：2003-07-09
申请人： LONZA AG , MICHEL, Dominique
发明人： MICHEL, Dominique
IPC分类号： C07C213/08
CPC分类号： C07D333/20 , C07C213/00 , C07C221/00 , C07C225/16 , C07D307/42 , C07D307/46 , C07D307/52 , C07D307/80 , C07D333/16 , C07D333/22 , C07D333/56
摘要： The invention relates to a process for the synthesis of N -monosubstituted β-amino alcohols of formula (I) and/or an addition salt of a proton acid, wherein R 1 and R 2 independently represent alkyl, cycloalkyl, aryl or aralkyl, each being optionally further substituted with alkyl, alkoxy and/or halogen via direct preparation of N -monosubstituted β-amino ketones of formula and its addition salts of proton acids, wherein R 1 and R 2 are as defined above.
摘要翻译：本发明涉及合成式（I）的N-单取代的β-氨基醇和/或质子酸的加成盐的方法，其中R 1和R 2独立地代表烷基，环烷基，芳基或芳烷基，其各自任选被烷基，烷氧基和/或卤素任意进一步被烷基，烷氧基和/或卤素取代，直接制备下式的N-单取代的β-氨基酮及其质子酸的加成盐，其中R 1和R 2如所定义以上。

4. 发明申请

WO2006087166A1 PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY PURE 1-SUBSTITUTED-3-AMINOALCOHOLS 审中-公开
标题翻译：制备纯化1-取代的3-氨基醇的方法
公开(公告)号：WO2006087166A1
公开(公告)日：2006-08-24
申请号：PCT/EP2006/001334
申请日：2006-02-14
申请人： LONZA AG , BRIEDEN, Walter , CLAUSEN, Martin , McGARRITY, John , METTLER, Hanspeter , MICHEL, Dominique
发明人： BRIEDEN, Walter , CLAUSEN, Martin , McGARRITY, John , METTLER, Hanspeter , MICHEL, Dominique
IPC分类号： C07C213/08 , C07C215/30 , C07C221/00 , C07C225/16 , C07C303/22 , C07C309/04 , C07C309/07 , C07C309/30 , C07D333/20
CPC分类号： C07C303/22 , C07B2200/07 , C07C213/02 , C07C221/00 , C07C309/04 , C07C309/07 , C07C309/30 , C07C215/30 , C07C225/16
摘要： Provided is a process for the preparation of N -monosubstituted β-aminoalcohol sulfonates of formula (Ia), (Ib) wherein R 1 is C 6-20 aryl or C 4-12 heteroaryl, each optionally being substituted with one or more halogen atoms and/or one or more C 1-4 alkyl or C 1-4 alkoxy groups, R 2 is C 1-4 -alkyl or C 6-20 aryl, each aryl optionally being substituted with one or more halogen atoms and/or one or more C 1-4 -alkyl or C 1-4 -alkoxy groups, and wherein R 3 is selected from the group consisting of C 1-18 alkyl, C 6-20 cycloalkyl, C 6-20 aryl and C 7-20 aralkyl residues, comprising the steps of a) reacting a methyl ketone, a primary amine, formaldehyde and a sulfonic acid, at a pressure above 1.5 bar, optionally in a organic solvent, said organic solvent optionally containing water, to afford N -monosubstituted β-aminoketone sulfonates of formula (II), wherein R 1 , R 2 and R 3 are as defined above, and b) asymmetrically hydrogenating said sulfonates in the presence of a base and a catalyst, comprising a transition metal and a diphosphine ligand, in a polar solvent, optionally in the presence of water.
摘要翻译：提供了制备式（Ia），（Ib）的N-单取代的β-氨基醇磺酸盐的方法，其中R 1为C 6-20芳基或C 1〜每个任选被一个或多个卤素原子和/或一个或多个C 1-4烷基或C 1-4烷基取代的杂芳基 >烷氧基，R 2是C 1-4 - 烷基或C 6-20-20芳基，每个芳基任选被一个或多个卤素原子和/或一个或多个C 1-4 - 烷基或C 1-4 - 烷氧基，并且其中R 3选自由C 1-18烷基，C 6-20环烷基，C 6-20芳基和C 7-20芳基组成的组中，包括以下步骤：a）使甲基酮，伯胺，甲醛和磺酸在高于1.5巴的压力下，任选地在有机溶剂中，任选地含有水的所述有机溶剂与得到形式的N-单取代的β-氨基酮磺酸盐其中R 1，R 2，R 3和R 3如上所定义，并且b）在存在下不对称地氢化所述磺酸盐的碱和催化剂，其包含过渡金属和二膦配体，在极性溶剂中，任选地在水的存在下。

5. 发明申请

WO2004005307A1 PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE 3-N-METHYLAMINO-1-(2-THIENYL)-1-PROPANOL 审中-公开
标题翻译：制备光学活性的3-N-甲基氨基-1-（2-噻吩基）-1-丙醇的方法
公开(公告)号：WO2004005307A1
公开(公告)日：2004-01-15
申请号：PCT/EP2003/007312
申请日：2003-07-08
申请人： LONZA AG , MICHEL, Dominique
发明人： MICHEL, Dominique
IPC分类号： C07H9/04
CPC分类号： C07D493/14 , C07D333/20 , C07H9/04
摘要： Enantiomerically enriched ( S )-(-)-3- N -methylamino-l-(2-thienyl)-1-propanol or ( R )-(+)-3- N -methylamino-l-(2-thienyl)-l-propanol of the formulae, or mirror image are prepared by i) treating an enantiomeric mixture of the amines Ia and Ib with (-)-2,3:4,6-di- O -isopropylidene-2-keto-L-gulonic acid or (+)-2,3:4,6-di- O -isopropylidene-2-keto-D-gulonic acid of the formulae (IIa) or mirror image ii) crystallizing the obtained diastereomerically enriched salts from the reaction mixture obtained in step i), iii) optionally recrystallizing said diastereomerically enriched salts IIIa or IVb, and iv) treating the diastereomerically enriched salts IIIa or IVb obtained in step ii) or step iii) with a base to liberate the enantiomerically enriched amines Ia or Ib.
摘要翻译：对映体富集（S） - （ - ） - 3-N-甲基氨基-1-（2-噻吩基）-1-丙醇或（R） - （+） - 3-N-甲基氨基-1-（2-噻吩基）通过i）将胺Ia和Ib的对映异构体混合物与（ - ） - 2,3：4,6-二-O-异亚丙基-2-酮-L- 古洛糖酸或式（IIa）的（+） - 2,3：4,6-二-O-异亚丙基-2-酮-D-古洛糖酸或反射镜图像ii）将所得非对映体富集的盐从反应混合物在步骤i）中获得，iii）任选地重结晶所述非对映体富集的盐IIIa或IVb，和iv）用碱处理步骤ii）或步骤iii）中获得的非对映体富集的盐IIIa或IVb，以释放对映异构体富集的胺Ia或Ib 。

6. 发明公开

EP1720852A1 PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY PURE 1-SUBSTITUTED-3-AMINOALCOHOLS 有权
标题翻译：用于生产对映体纯的1-取代-3-氨基醇
公开(公告)号：EP1720852A1
公开(公告)日：2006-11-15
申请号：EP05715425.4
申请日：2005-02-21
申请人： Lonza AG
发明人： MICHEL, Dominique , METTLER, Hanspeter , MCGARRITY, John
IPC分类号： C07D333/20 , C07D333/22 , C07C213/00 , C07B53/00
CPC分类号： C07C213/00 , C07B2200/07 , C07D333/22
摘要： Provided is a process for the preparation of enantiomerically pure 1-substituted-3-aminoalcohols, particularly of (S)-(-)- and (R)-(+)-3-N-methylamino-l-(2-thienyl)-1-propanol, by asymmetrically hydrogenating salts of a carboxylic acids with an aminoketone of formula (II), wherein R1 is selected from the group consisting of 2-thienyl, 2-furanyl and phenyl, each optionally substituted with one or more halogen atoms and/or one or more C1-4-alkoxy groups, and wherein R2 is C1-4-alkyl or phenyl, each optionally substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups, and wherein the corresponding aminoalcohols are obtained by subsequent hydrolysis of their salts. Furthermore provided are salts of a carboxylic acid with said aminoketones and the aminoalcohols obtained by asymmetriacally hydrogenating said aminoketones, respectively.

7. 发明授权

EP1720852B1 PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY PURE 1-SUBSTITUTED-3-AMINOALCOHOLS 有权
标题翻译：用于生产对映体纯的1-取代-3-氨基醇
公开(公告)号：EP1720852B1
公开(公告)日：2012-07-11
申请号：EP05715425.4
申请日：2005-02-21
申请人： Lonza AG
发明人： MICHEL, Dominique , METTLER, Hanspeter , MCGARRITY, John
IPC分类号： C07D333/20 , C07D333/22 , C07C213/00 , C07B53/00
CPC分类号： C07C213/00 , C07B2200/07 , C07D333/22
摘要： Provided is a process for the preparation of enantiomerically pure 1-substituted-3-aminoalcohols, particularly of (S)-(-)- and (R)-(+)-3-N-methylamino-l-(2-thienyl)-1-propanol, by asymmetrically hydrogenating salts of a carboxylic acids with an aminoketone of formula (II), wherein R1 is selected from the group consisting of 2-thienyl, 2-furanyl and phenyl, each optionally substituted with one or more halogen atoms and/or one or more C1-4-alkoxy groups, and wherein R2 is C1-4-alkyl or phenyl, each optionally substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups, and wherein the corresponding aminoalcohols are obtained by subsequent hydrolysis of their salts. Furthermore provided are salts of a carboxylic acid with said aminoketones and the aminoalcohols obtained by asymmetriacally hydrogenating said aminoketones, respectively.

8. 发明公开

EP1868983A1 PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY PURE 1-SUBSTITUTED-3-AMINOALCOHOLS 审中-公开
标题翻译：用于生产对映体纯的1-取代-3-氨基醇
公开(公告)号：EP1868983A1
公开(公告)日：2007-12-26
申请号：EP06706940.1
申请日：2006-02-14
申请人： Lonza AG
发明人： BRIEDEN, Walter , CLAUSEN, Martin , McGARRITY, John , METTLER, Hanspeter , MICHEL, Dominique
IPC分类号： C07C213/08 , C07C215/30 , C07C221/00 , C07C225/16 , C07C303/22 , C07C309/04 , C07C309/07 , C07C309/30 , C07D333/20
CPC分类号： C07C303/22 , C07B2200/07 , C07C213/02 , C07C221/00 , C07C309/04 , C07C309/07 , C07C309/30 , C07C215/30 , C07C225/16
摘要： Provided is a process for the preparation of N-monosubstituted β-aminoalcohol sulfonates of formula (Ia), (Ib) wherein R1 is C6-20 aryl or C4-12 heteroaryl, each optionally being substituted with one or more halogen atoms and/or one or more C1-4 alkyl or C1-4 alkoxy groups, R2 is C1-4-alkyl or C6-20 aryl, each aryl optionally being substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups, and wherein R3 is selected from the group consisting of C1-18 alkyl, C6-20 cycloalkyl, C6-20 aryl and C7-20 aralkyl residues, comprising the steps of a) reacting a methyl ketone, a primary amine, formaldehyde and a sulfonic acid, at a pressure above 1.5 bar, optionally in a organic solvent, said organic solvent optionally containing water, to afford N-monosubstituted β-aminoketone sulfonates of formula (II), wherein R1, R2 and R3 are as defined above, and b) asymmetrically hydrogenating said sulfonates in the presence of a base and a catalyst, comprising a transition metal and a diphosphine ligand, in a polar solvent, optionally in the presence of water.

9. 发明授权

EP1539673B1 PROCESS FOR THE PREPARATION OF N -MONOSUBSTITUTED BETA-AMINO ALCOHOLS 有权转让
标题翻译：用于生产N-单取代的氨基醇
公开(公告)号：EP1539673B1
公开(公告)日：2007-10-03
申请号：EP03762669.4
申请日：2003-07-09
申请人： Lonza AG
发明人： MICHEL, Dominique
IPC分类号： C07C213/08 , C07D307/46 , C07D333/22 , C07C225/12 , C07C221/00
CPC分类号： C07C213/00 , C07C221/00 , C07C225/16 , C07D307/46 , C07D333/22
摘要： The invention relates to a process for the synthesis of N-monosubstituted β-amino alcohols of formula (I) and/or an addition salt of a proton acid, wherein R1 and R2 independently represent alkyl, cycloalkyl, aryl or aralkyl, each being optionally further substituted with alkyl, alkoxy and/or halogen via direct preparation of N-monosubstituted β-amino ketones of formula and its addition salts of proton acids, wherein R1 and R2 are as defined above.

10. 发明公开

EP1539673A1 PROCESS FOR THE PREPARATION OF i N /i -MONOSUBSTITUTED &bgr;-AMINO ALCOHOLS 有权转让
标题翻译：用于生产N-单取代的氨基醇
公开(公告)号：EP1539673A1
公开(公告)日：2005-06-15
申请号：EP03762669.4
申请日：2003-07-09
申请人： Lonza AG
发明人： MICHEL, Dominique
IPC分类号： C07C213/08 , C07D307/46 , C07D333/22 , C07C225/12 , C07C221/00
CPC分类号： C07C213/00 , C07C221/00 , C07C225/16 , C07D307/46 , C07D333/22
摘要： The invention relates to a process for the synthesis of N-monosubstituted β-amino alcohols of formula (I) and/or an addition salt of a proton acid, wherein R1 and R2 independently represent alkyl, cycloalkyl, aryl or aralkyl, each being optionally further substituted with alkyl, alkoxy and/or halogen via direct preparation of N-monosubstituted β-amino ketones of formula and its addition salts of proton acids, wherein R1 and R2 are as defined above.

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