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79 条记录 (耗时 0.028 秒)

    Method for the preparation of citalopram
    24.
    发明授权
    Method for the preparation of citalopram 失效
    西酞普兰制备方法

    公开(公告)号：US06509483B2

    公开(公告)日：2003-01-21

    申请号：US09930110

    申请日：2001-08-14

    申请人： Hans Petersen ,  Haleh Ahmadian ,  Robert Dancer

    发明人： Hans Petersen ,  Haleh Ahmadian ,  Robert Dancer

    IPC分类号： C07D30787

    CPC分类号： C07D307/87

    摘要： A method for the preparation of citalopram comprising reacting 5-carboxyphthalide successively with a Grignard reagent of 4-halo-fluorophenyl and a Grignard reagent of 3-halo-N,N-dimethyl-propylamine and then effecting ring closure of the resulting compound of Formula XI to a compound of Formula IV followed by conversion of the compound of Formula IV into citalopram is disclosed. Methods for the manufacture and conversion of the compound of Formula IV are also disclosed.

    摘要翻译： 一种制备西酞普兰的方法，其包括使5-羧基邻苯二甲酸酯与4-卤代 - 氟苯基的格氏试剂和3-卤代-N，N-二甲基 - 丙胺的格氏试剂依次反应，然后使所得到的式 公开了通过式IV化合物转​​化为西酞普兰的式IV化合物。 还公开了制备和转化式IV化合物的方法。

    Method for manufacture of THIP
    25.
    发明授权
    Method for manufacture of THIP 失效
    制造THIP的方法

    公开(公告)号：US07371863B2

    公开(公告)日：2008-05-13

    申请号：US10570551

    申请日：2004-09-01

    申请人： Hans Petersen ,  Michael Bech Sommer ,  Robert Dancer

    发明人： Hans Petersen ,  Michael Bech Sommer ,  Robert Dancer

    IPC分类号： C07D471/02 ,  C07D491/02 ,  C07D498/02

    CPC分类号： C07D498/04

    摘要： The present invention relates to a new method of preparing gaboxadol (THIP), which is useful for treating sleep disorders. In particular a method of preparing THIP comprising reacting a compound of formula (8b) or a salt thereof with an acid, typically a mineral acid, to obtain THIP as an acid addition salt. The present invention also relates to several intermediates

    摘要翻译： 本发明涉及一种制备加波沙朵（THIP）的新方法，其可用于治疗睡眠障碍。 特别是制备THIP的方法，包括使式（8b）的化合物或其盐与酸（通常为无机酸）反应，得到THIP作为酸加成盐。 本发明还涉及几种中间体

    Method for manufacture of thip
    26.
    发明申请
    Method for manufacture of thip 失效
    制造勺子的方法

    公开(公告)号：US20070112198A1

    公开(公告)日：2007-05-17

    申请号：US10570551

    申请日：2004-09-01

    申请人： Hans Petersen ,  Michael Sommer ,  Robert Dancer

    发明人： Hans Petersen ,  Michael Sommer ,  Robert Dancer

    IPC分类号： C07D491/02

    CPC分类号： C07D498/04

    摘要： The present invention relates to a new method of preparing gaboxadol (THIP), which is useful for treating sleep disorders. In particular a method of preparing THIP comprising reacting a compound of formula (8b) or a salt thereof with an acid, typically a mineral acid, to obtain THIP as an acid addition salt. The present invention also relates to several intermediates.

    摘要翻译： 本发明涉及一种制备加波沙朵（THIP）的新方法，其可用于治疗睡眠障碍。 特别是制备THIP的方法，包括使式（8b）的化合物或其盐与酸（通常为无机酸）反应，得到THIP作为酸加成盐。 本发明还涉及几种中间体。

    Process for the preparation of racemic citalopram diol and/or s-or r-citalopram diols and the use of such diols for the preparation o racemic citalopram, r-citalopram and/or s-citalopram
    27.
    发明申请
    Process for the preparation of racemic citalopram diol and/or s-or r-citalopram diols and the use of such diols for the preparation o racemic citalopram, r-citalopram and/or s-citalopram 失效
    用于制备外消旋西酞普兰二醇和/或s-或r-西酞普兰二醇的方法和使用这种二醇制备外消旋西酞普兰，西酞普兰和/或西酞普兰

    公开(公告)号：US20060020140A1

    公开(公告)日：2006-01-26

    申请号：US10540300

    申请日：2003-12-18

    申请人： Hans Petersen ,  Brian Christiansen ,  Robert dancer ,  Rikke Humble

    发明人： Hans Petersen ,  Brian Christiansen ,  Robert dancer ,  Rikke Humble

    IPC分类号： C07D307/78

    CPC分类号： C07D307/87 ,  C07C253/34

    摘要： In the following, citalopram diol means 4-(4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl)-3-(hydroxymethyl)-benzonitrile, as free base and/or acid addition salt. The invention relates to a process for the preparation of racemic citalopram diol and/or R- or S-citalopram diol, comprising the separation of a non-racemic mixture of R- and S-citalopram diol with more than 50% of one of the enantiomers into a fraction being enriched with S- or R-citalopram diol and a fraction comprising RS-citalopram diol wherein the ratio of R-citalopram diol:S-citalopram diol is equal to 1:1 or closer to 1:1 than in the initial mixture. The method is characterized in that (i) RS-citalopram diol is precipitated from a solution of the initial non-racemic mixture, or R- or S-citalopram diol is dissolved into a solvent from the initial non-racemic mixture, leaving a residue of RS-citalopram diol, and in that (ii) the residue/precipitate formed is separated from the final solution phase, followed by optional steps of repetition, recrystallisation, purification, isolation and conversion between free base and salts. The invention also relates to a process for the preparation of RS-citalopram, S-citalopram or R-citalopram (all as free base and/or acid addition salt) comprising the method described above followed by ring closure.

    摘要翻译： 在下文中，西酞普兰二醇是指作为游离碱和/或酸加成盐的4-（4-（二甲基氨基）-1-（4-氟苯基）-1-羟基丁基）-3-（羟甲基） - 苄腈。 本发明涉及一种制备外消旋西酞普兰二醇和/或R-或S-西酞普兰二醇的方法，包括将R-和S-西酞普兰二醇的非外消旋混合物与50％以上的 对映体转化成富含S-或R-西酞普兰二醇的级分和包含RS-西酞普兰二醇的级分，其中R-西酞普兰二醇：西西酞普兰二醇的比例等于1:1或比1:1 初始混合物。 该方法的特征在于（i）RS-西酞普兰二醇从初始非外消旋混合物的溶液中沉淀，或将R-或S-西酞普兰二醇从初始非外消旋混合物中溶解到溶剂中，留下残余物 的RS-西酞普兰二醇，并且（ii）所形成的残余物/沉淀物与最终溶液相分离，随后重复，重结晶，纯化，分离和转化游离碱和盐之间的任选步骤。 本发明还涉及一种制备RS-西酞普兰，西酞普兰或R-西酞普兰（均为游离碱和/或酸加成盐）的方法，包括上述方法，然后闭环。

    CRYSTALLINE BASE OF CITALOPRAM
    28.
    发明申请
    CRYSTALLINE BASE OF CITALOPRAM 审中-公开
    CITALOPRAM的晶体碱基

    公开(公告)号：US20060229459A1

    公开(公告)日：2006-10-12

    申请号：US11425308

    申请日：2006-06-20

    申请人： Hans Petersen ,  Klaus Bogeso ,  Per Holm

    发明人： Hans Petersen ,  Klaus Bogeso ,  Per Holm

    IPC分类号： C07D307/02

    CPC分类号： C07D307/81 ,  H01M8/04156 ,  H01M8/04171 ,  H01M8/04186 ,  H01M8/1009 ,  H01M8/1011 ,  H01M8/241 ,  H01M8/2455 ,  H01M8/246 ,  Y02E60/523

    摘要： The present invention relates to the crystalline base of the well known antidepressant drug citalopram, 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile, formulations of said base, a process for the preparation of purified salts of citalopram, such as the hydrobromide, using the base, the salts obtained by said process and formulations containing such salts.

    摘要翻译： 本发明涉及众所周知的抗抑郁药物西酞普兰，1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈的结晶碱，所述碱的制剂， 制备西酞普兰纯化盐的方法，例如使用碱的氢溴酸盐，通过所述方法获得的盐和含有这些盐的制剂。