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    Method for the preparation of pure citalopram
    1.
    发明申请
    Method for the preparation of pure citalopram 失效
    纯西酞普兰的制备方法

    公开(公告)号：US20020120005A1

    公开(公告)日：2002-08-29

    申请号：US10046126

    申请日：2002-01-08

    Applicant: H. Lundbeck A/S

    Inventor： Marco Villa ,  Federico Sbrogio ,  Robert Dancer

    IPC: A61K031/36 ,  C07D37/81

    CPC classification number: C07D307/87

    Abstract: The present invention relates to the process for the preparation and purification of citalopram (I) 1 in which a compound of formula (II) 2 wherein Z is iodo, bromo, chloro or CF3null(CF2)nnullSO2nullOnull, n being 0, 1, 2, 3, 4, 5, 6, 7 or 8, is subjected to a cyanide exchange reaction with a cyanide source; the resultant crude citalopram product is optionally subjected to some initial purification and subsequently treated with an amide or an amide-like group forming agent; the reaction mixture is then subjected to an acid/base wash and/or crystallisation and recrystallisation of citalopram in order to remove the amides formed from the crude citalopram mixture; and the resulting citalopram product is optionally further purified, worked up and isolated as the base or a pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明涉及西酞普兰（I）的制备和纯化方法，其中Z为碘，溴，氯或CF 3 - （CF 2）n -SO 2 -O-的式（II）化合物，n为0 ，1，2，3，4，5，6，7或8，与氰化物源进行氰化物交换反应; 所得粗制西酞普兰产品任选进行一些初始纯化，随后用酰胺或类酰胺形成剂处理; 然后将反应混合物进行酸/碱洗涤和/或结晶并重结晶西酞普兰以除去由西酞普兰粗制混合物形成的酰胺; 任选地进一步纯化，后处理和分离得到的西酞普兰产物作为碱或其药学上可接受的盐。

    Benzofuran derivatives, their preparation and use
    2.
    发明申请
    Benzofuran derivatives, their preparation and use 失效
    苯并呋喃衍生物，其制备和用途

    公开(公告)号：US20020032205A1

    公开(公告)日：2002-03-14

    申请号：US09874392

    申请日：2001-06-04

    Applicant: H. Lundbeck A/S

    Inventor： Kim Andersen ,  Mario Rottlander ,  Klaus Peter Bogeso ,  Henrik Pedersen ,  Thomas Ruhland ,  Robert Dancer

    IPC: A61K031/496 ,  C07D49/02 ,  A61K031/4525 ,  A61K031/352

    CPC classification number: C07D307/87 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D471/04

    Abstract: The present invention relates to benzofuran derivatives having general Formula (I) 1 wherein A is selected from (1), (2), (3), (4) 2 wherein Z is O or S; s is 0 or 1; q is 0 or 1; R4 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C26-alkynyl, C1-6-alkyl-aryl, or C1-6-alkyl-O-aryl; D is a spacer group selected from branched or straight chain C1-6-alkylene, C2-6-alkenylene and C2-6-alkynylene; its enantiomers, and pharmaceutically acceptable acid addition salt thereof. The compounds are potently binding to the 5-HT1A receptor.

    Abstract translation: 本发明涉及通式（I）的苯并呋喃衍生物，其中A选自（1），（2），（3），（4）其中Z为O或S; s为0或1; q为0或1; R 4是氢，C 1-6 - 烷基，C 2-6烯基，C 2-6炔基，C 1-6 - 烷基 - 芳基或C 1-6 - 烷基-O-芳基; D是选自支链或直链C 1-6 - 亚烷基，C 2-6亚烯基和C 2-6亚炔基的间隔基; 其对映体及其药学上可接受的酸加成盐。 这些化合物与5-HT1A受体有很强的结合。

    Method for the preparation of citalopram
    3.
    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：US20030134895A1

    公开(公告)日：2003-07-17

    申请号：US10291174

    申请日：2002-11-08

    Applicant: H. Lundbeck A/S

    Inventor： Hans Petersen ,  Robert Dancer

    IPC: C07D307/87 ,  A61K031/343

    CPC classification number: C07D307/87 ,  C07D307/88

    Abstract: A method for the preparation of citalopram comprising reaction of a compound of formula 5-aminomethyl-1-(3-dimethylamino-propyl)-1-(4-fluoro-phenyl)-1,3-dihydro-isobenzofuran with an oxidising agent to prepare citalopram.

    Abstract translation: 一种制备西酞普兰的方法，其包括将式5-氨基甲基-1-（3-二甲基氨基 - 丙基）-1-（4-氟 - 苯基）-1,3-二氢异苯并呋喃与氧化剂的化合物反应 准备西酞普兰

    Method for the preparation of citalopram
    6.
    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：US20020026062A1

    公开(公告)日：2002-02-28

    申请号：US09930110

    申请日：2001-08-14

    Applicant: H. Lundbeck A/S

    Inventor： Hans Petersen ,  Haleh Ahmadian ,  Robert Dancer

    IPC: C07D37/81

    CPC classification number: C07D307/87

    Abstract: 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 1 to a compound of Formula IV 2 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.

    Abstract translation: 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 XI公开了式IV化合物，随后将式IV化合物转​​化为西酞普兰。 还公开了制备和转化式IV化合物的方法。

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