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1. 发明授权

US08791294B2 Method for the stereoselective preparation of amino acid derivatives 有权
标题翻译：立体选择性制备氨基酸衍生物的方法
公开(公告)号：US08791294B2
公开(公告)日：2014-07-29
申请号：US12743470
申请日：2008-11-19
申请人： Llorenç Rafecas Jane , Antoni Riera Escale , Rosario Ramon Albalate , Monica Alonso Xalma
发明人： Llorenç Rafecas Jane , Antoni Riera Escale , Rosario Ramon Albalate , Monica Alonso Xalma
IPC分类号： C07C229/36 , C07K5/087
CPC分类号： C07C271/22 , C07B53/00 , C07B2200/07 , C07C67/31 , C07C227/32 , C07C229/36 , C07C247/12 , C07C271/34 , C07C2603/18 , C07D203/02 , C07D203/06 , C07K1/04 , C07K5/0812 , C07C69/732
摘要： The invention relates to a process for the stereoselective preparation of amino acid derivatives, comprising a hydrogenation reaction of the compound of formula (III), alternatively its enantiomer, wherein R is (C1-C8)-alkyl; followed by a hydrolysis reaction to obtain L-mesityl alanine, alternatively its enantiomer D-mesityl alanine and, optionally, subjecting said compound to an amino group protection reaction, particularly as Fmoc. It also comprises Fmoc-L- or Fmoc-D-mesityl alanine as products per se, useful as intermediates in preparing peptides or peptide analogs with therapeutic or biological activity.
摘要翻译：本发明涉及一种用于立体选择性制备氨基酸衍生物的方法，包括式（III）化合物或其对映异构体的氢化反应，其中R是（C 1 -C 8） - 烷基; 然后进行水解反应以获得L-均三甲基丙氨酸，或者其对映体D-均三甲基丙氨酸，以及任选地使所述化合物进行氨基保护反应，特别是作为Fmoc。它还包含Fmoc-L-或Fmoc-D-mesityl丙氨酸作为产品本身，可用作制备具有治疗或生物活性的肽或肽类似物的中间体。

2. 发明申请

US20110082301A1 Preparation of Delmopinol 有权
标题翻译：德莫酚的制备
公开(公告)号：US20110082301A1
公开(公告)日：2011-04-07
申请号：US12972896
申请日：2010-12-20
申请人： Alexander Comely , Llorenç Rafecas Jane , Nicolas Tesson , Antoni Riera Escale
发明人： Alexander Comely , Llorenç Rafecas Jane , Nicolas Tesson , Antoni Riera Escale
IPC分类号： C07D263/06 , C07D263/52 , C07C217/28 , C07D303/04 , C07C19/075 , C07C11/02
CPC分类号： C07D263/06 , C07C11/02 , C07C17/16 , C07C19/075 , C07D265/08 , C07D309/04
摘要： It comprises a process for the production of delmopinol or a pharmaceutically acceptable salt and/or a solvate thereof, by subjecting the compound of formula (II) where R1 and R2 are the same or different, independently selected from the group consisting of H, (C1-C6) alkyl or, alternatively, R1 and R2 form, together with the carbon atom to which they are attached, a (C5-C6) cycloalkyl radical; and R3 is a radical selected from the group consisting of CF3, (C1-C4) alkyl, phenyl, and phenyl mono- or disubstituted by a radical selected from the group consisting of (C1-C4)-alkyl, halogen and nitro to a deprotection and cyclisation reaction. The process is useful to prepare delmopinol or its salts on an industrial scale. The compound of formula (II) is new and also forms part of the present invention, as well as its preparation process and other new intermediates of said preparation process.
摘要翻译：其包括通过使式（II）化合物（其中R 1和R 2相同或不同）独立地选自H，（其中R 1和R 2相同或不同）的方法制备德美洛酚或其药学上可接受的盐和/或其溶剂合物， C 1 -C 6）烷基，或者，R 1和R 2与它们所连接的碳原子一起形成（C5-C6）环烷基; 并且R 3是选自由CF 3，（C 1 -C 4）烷基，苯基和被选自（C 1 -C 4） - 烷基，卤素和硝基的基团单 - 或二取代的基团至去保护和环化反应。该工艺可用于在工业规模上制备德莫莫醇或其盐。式（II）化合物是新的，也是本发明的一部分，以及其制备方法和所述制备方法的其它新中间体。

3. 发明申请

US20100298538A1 METHOD FOR THE STEREOSELECTIVE PREPARATION OF AMINO ACID DERIVATIVES 有权
标题翻译：氨基酸衍生物的立体选择性制备方法
公开(公告)号：US20100298538A1
公开(公告)日：2010-11-25
申请号：US12743470
申请日：2008-11-19
申请人： Llorenç Rafecas Jane , Antonio Riera Escale , Rosario Ramon Albalate , Monica Alonso Xalma
发明人： Llorenç Rafecas Jane , Antonio Riera Escale , Rosario Ramon Albalate , Monica Alonso Xalma
IPC分类号： C07C229/36 , C07C271/08 , C07K1/06
CPC分类号： C07C271/22 , C07B53/00 , C07B2200/07 , C07C67/31 , C07C227/32 , C07C229/36 , C07C247/12 , C07C271/34 , C07C2603/18 , C07D203/02 , C07D203/06 , C07K1/04 , C07K5/0812 , C07C69/732
摘要： The invention relates to a process for the stereoselective preparation of amino acid derivatives, comprising a hydrogenation reaction of the compound of formula (III), alternatively its enantiomer, wherein R is (C1-C8)-alkyl; followed by a hydrolysis reaction to obtain L-mesityl alanine, alternatively its enantiomer D-mesityl alanine and, optionally, subjecting said compound to an amino group protection reaction, particularly as Fmoc. It also comprises Fmoc-L- or Fmoc-D-mesityl alanine as products per se, useful as intermediates in preparing peptides or peptide analogs with therapeutic or biological activity.
摘要翻译：本发明涉及一种用于立体选择性制备氨基酸衍生物的方法，包括式（III）化合物或其对映异构体的氢化反应，其中R是（C 1 -C 8） - 烷基; 然后进行水解反应以获得L-均三甲基丙氨酸，或者其对映体D-均三甲基丙氨酸，以及任选地使所述化合物进行氨基保护反应，特别是作为Fmoc。它还包含Fmoc-L-或Fmoc-D-mesityl丙氨酸作为产品本身，可用作制备具有治疗或生物活性的肽或肽类似物的中间体。

4. 发明授权

US08093398B2 Preparation of delmopinol 有权
标题翻译：德莫林醇的制备
公开(公告)号：US08093398B2
公开(公告)日：2012-01-10
申请号：US12972896
申请日：2010-12-20
申请人： Alexander Comely , Llorenç Rafecas Jane , Nicolas Tesson , Antoni Riera Escale
发明人： Alexander Comely , Llorenç Rafecas Jane , Nicolas Tesson , Antoni Riera Escale
IPC分类号： C07D263/06
CPC分类号： C07D263/06 , C07C11/02 , C07C17/16 , C07C19/075 , C07D265/08 , C07D309/04
摘要： It comprises a process for the production of delmopinol or a pharmaceutically acceptable salt and/or a solvate thereof, by subjecting the compound of formula (II) where R1 and R2 are the same or different, independently selected from the group consisting of H, (C1-C6) alkyl or, alternatively, R1 and R2 form, together with the carbon atom to which they are attached, a (C5-C6) cycloalkyl radical; and R3 is a radical selected from the group consisting of CF3, (C1-C4) alkyl, phenyl, and phenyl mono- or disubstituted by a radical selected from the group consisting of (C1-C4)-alkyl, halogen and nitro to a deprotection and cyclisation reaction. The process is useful to prepare delmopinol or its salts on an industrial scale. The compound of formula (II) is new and also forms part of the present invention, as well as its preparation process and other new intermediates of said preparation process.
摘要翻译：其包括通过使式（II）化合物（其中R 1和R 2相同或不同）独立地选自H，（其中R 1和R 2相同或不同）的方法制备德美洛酚或其药学上可接受的盐和/或其溶剂合物， C 1 -C 6）烷基，或者，R 1和R 2与它们所连接的碳原子一起形成（C5-C6）环烷基; 并且R 3是选自由CF 3，（C 1 -C 4）烷基，苯基和被选自（C 1 -C 4） - 烷基，卤素和硝基的基团单 - 或二取代的基团至去保护和环化反应。该工艺可用于在工业规模上制备德莫莫醇或其盐。式（II）化合物是新的，也是本发明的一部分，以及其制备方法和所述制备方法的其它新中间体。

5. 发明授权

US07893258B2 Preparation of delmopinol 有权
标题翻译：德莫林醇的制备
公开(公告)号：US07893258B2
公开(公告)日：2011-02-22
申请号：US12161593
申请日：2007-01-10
申请人： Alexander Comely , Llorenç Rafecas Jane , Nicolas Tesson , Antoni Riera Escale
发明人： Alexander Comely , Llorenç Rafecas Jane , Nicolas Tesson , Antoni Riera Escale
IPC分类号： C07D265/30 , C07D263/06
CPC分类号： C07D263/06 , C07C11/02 , C07C17/16 , C07C19/075 , C07D265/08 , C07D309/04
摘要： It comprises a preparation process of delmopinol or a pharmaceutically acceptable salt and/or a solvate thereof, by submitting the compound of formula (II) where R1 and R2 are the same or different, independently selected from the group consisting of H, (C1-C6)-alkyl or, alternatively, R1 and R2 form, together with the carbon atom to which they are attached, a (C5-C6)-cycloalkyl radical; and R3 is a radical selected from the group consisting of CF3, (C1-C4)-alkyl, phenyl, and phenyl mono- or disubstituted by a radical selected from the group consisting of (C1-C4)-alkyl, halogen and nitro to a deprotection and cyclisation reaction. The process is useful to prepare delmopinol or its salts on an industrial scale. The compound of formula (II) is new and also forms part of the present invention, as well as its preparation process and other new intermediates of said preparation process.
摘要翻译：它包括德米莫酚或其药学上可接受的盐和/或其溶剂化物的制备方法，其中R 1和R 2相同或不同，式（II）化合物独立地选自H，（C1- C 6） - 烷基，或者，R 1和R 2与它们所连接的碳原子一起形成（C 5 -C 6） - 环烷基; 并且R 3是选自以下的基团：CF 3，（C 1 -C 4） - 烷基，苯基和被选自（C 1 -C 4） - 烷基，卤素和硝基的基团单或双取代的苯基，脱保护和环化反应。该工艺可用于在工业规模上制备德莫莫醇或其盐。式（II）化合物是新的，也是本发明的一部分，以及其制备方法和所述制备方法的其它新中间体。

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