Preparation of delmopinol
    2.
    发明授权
    Preparation of delmopinol 有权
    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

    IPC分类号: C07D263/06

    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。

    Preparation of delmopinol
    3.
    发明授权
    Preparation of delmopinol 有权
    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

    IPC分类号: C07D265/30 C07D263/06

    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。

    Preparation of Delmopinol
    10.
    发明申请
    Preparation of Delmopinol 有权
    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

    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。