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79 条记录 (耗时 0.031 秒)

    Method for the preparation of citalopram
    71.
    发明申请
    Method for the preparation of citalopram 失效
    西酞普兰制备方法

    公开(公告)号：US20050124817A1

    公开(公告)日：2005-06-09

    申请号：US10958067

    申请日：2004-10-04

    申请人： Hans Petersen

    发明人： Hans Petersen

    IPC分类号： A61K31/34 ,  A61K31/343 ,  A61P25/24 ,  C07D307/78 ,  C07D307/81 ,  C07D307/87

    CPC分类号： C07D307/87

    摘要： A method for the preparation of citalopram comprising reductive hydrolysis of a compound of Formula (IV) wherein R is a N,N-disubstituted amid group or an optionally substituted 4,5-dihydro-1,3-oxazol-2-yl group, and conversion of the resulting 5-formyl compound to citalopram.

    摘要翻译： 一种制备西酞普兰的方法，包括式（IV）化合物的还原性水解，其中R是N，N-二取代的酰胺基团或任选取代的4,5-二氢-1,3-恶唑-2-基， 并将所得的5-甲酰基化合物转化成西酞普兰。

    Method for the preparation of citalopram
    72.
    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：US06849749B2

    公开(公告)日：2005-02-01

    申请号：US09977920

    申请日：2001-10-15

    申请人： Hans Petersen

    发明人： Hans Petersen

    IPC分类号： A61K31/34 ,  A61K31/343 ,  A61P25/24 ,  C07D307/78 ,  C07D307/81 ,  C07D307/87 ,  C07D307/93

    CPC分类号： C07D307/87

    摘要： A method for the preparation of citalopram comprising reductive hydrolysis of a compound of Formula (IV): wherein R is a N,N-disubstituted amid group or an optionally substituted 4,5-dihydro-1,3-oxazol-2-yl group, and conversion of the resulting 5-formyl compound to citalopram.

    摘要翻译： 一种制备西酞普兰的方法，包括式（IV）化合物的还原水解：其中R是N，N-二取代的酰胺基团或任选取代的4,5-二氢-1,3-恶唑-2-基 ，并将所得5-甲酰基化合物转化成西酞普兰。

    Method for the preparation of 5-carboxyphthalide
    73.
    发明授权
    Method for the preparation of 5-carboxyphthalide 失效
    5-羧基苯酞的制备方法

    公开(公告)号：US06403813B1

    公开(公告)日：2002-06-11

    申请号：US09692653

    申请日：2000-10-19

    申请人： Hans Petersen ,  Poul Dahlberg Nielsen

    发明人： Hans Petersen ,  Poul Dahlberg Nielsen

    IPC分类号： C07D30700

    CPC分类号： C07D307/88

    摘要： 5-carboxyphthalide is obtained with very high purity and in high yields by a convenient process comprising reaction of terephthalic acid with paraformaldehyde HO(CH2)nH in oleum.

    摘要翻译： 通过方便的方法获得非常高的纯度和高产率的5-羧基邻苯二甲酰亚胺，其包括对苯二甲酸与发烟硫酸中的多聚甲醛HO（CH 2）nH的反应。

    Method for the preparation of 5-cyanophthalide
    74.
    发明授权
    Method for the preparation of 5-cyanophthalide 有权

    公开(公告)号：US06392060B1

    公开(公告)日：2002-05-21

    申请号：US09888067

    申请日：2001-06-22

    申请人： Hans Petersen ,  Poul Dahlberg Nielsen

    发明人： Hans Petersen ,  Poul Dahlberg Nielsen

    IPC分类号： C07D30787

    摘要： A method for the preparation of 5-cyanophthalide in which 5-carboxyphthalide is converted to the corresponding amide of Formula (IV) in which R is hydrogen or C1-6 alkyl, which is then reacted with a dehydrating agent thereby obtaining 5-cyanophthalide. The conversion of 5-carboxyphthalide to the corresponding amide of Formula (IV) may be carried out via the corresponding C1-6 alkyl or phenyl ester or the acid chloride, which is converted to the amide of Formula (IV) by amidation with ammonia or a C1-6 alkylamine. By the process 5-cyanophthalide, an important intermediate used in the preparation of the antidepressant citalopram, is prepared in high yields by a convenient, cost effective procedure.

    Method for the preparation of citalopram
    75.
    发明授权
    Method for the preparation of citalopram 有权
    西酞普兰制备方法

    公开(公告)号：US06365747B1

    公开(公告)日：2002-04-02

    申请号：US09830109

    申请日：2001-06-01

    申请人： Leone Dall'Asta ,  Umberto Casazza ,  Hans Petersen

    发明人： Leone Dall'Asta ,  Umberto Casazza ,  Hans Petersen

    IPC分类号： C07D30787

    CPC分类号： C07D307/87 ,  C07D263/14 ,  C07D413/04

    摘要： The present invention relates to a method for the preparation of citalopram or any of its enantiomers and acid addition salts thereof comprising treatment of a compound of formula (IV), wherein X is O or S; R1-R2 are each independently selected from hydrogen and C1-6 alkyl, or R1 and R2 together form a C2-5 alkylene chain thereby forming a spiro-ring; R3 is selected from hydrogen and C1-6 alkyl, R4 is selected from hydrogen, C1-6 alkyl, a carboxy group or a precursor group therefore, or R3 and R4 together form a C2-5 alkylene chain thereby forming a spiro-ring, with a dehydration agent or alternatively where X is S, thermally cleavage of the thiazoline ring, or treatment in presence of a radical initiator, to form citalopram. The invention also relates to intermediates used in the new process for the preparation of citalopram, as well as citalopram prepared according to the new process.

    摘要翻译： 本发明涉及一种制备西酞普兰或其任何对映异构体及其酸加成盐的方法，包括处理式（IV）化合物，其中X为O或S; R 1 -R 2各自独立地选自氢和C 1-6烷基，或者R 1和R 2一起形成C 2-5亚烷基链，从而形成螺环; R3选自氢和C 1-6烷基，因此R4选自氢，C 1-6烷基，羧基或前体基，或者R 3和R 4一起形成C 2-5亚烷基链，从而形成螺环， 用脱水剂或者其中X是S，噻唑啉环的热裂解，或在自由基引发剂的存在下进行处理以形成西酞普兰。 本发明还涉及用于制备西酞普兰的新方法的中间体以及根据新方法制备的西酞普兰。