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。

公开(公告)号：US20030178295A1

公开(公告)日：2003-09-25

申请号：US10361800

申请日：2003-02-10

Applicant: H. LUNDBECK A/S

Inventor： Andrea Castellin ,  Giulio Volpe ,  Federico Sbrogio

IPC: B01D003/28

CPC classification number: C07D307/87

Abstract: A process for the preparation of citalopram of formula (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 in which the group Z is exchanged with cyanide by reaction with a cyanide source; the resultant crude citalopram product is optionally subjected to some initial purification and the crude citalopram base is subsequently subjected to a film distillation process; the resulting citalopram product is then optionally further purified and worked up and isolated as the base or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20020087012A1

公开(公告)日：2002-07-04

申请号：US10035005

申请日：2001-12-20

Applicant: H. Lundbeck A/S

Inventor： Andrea Castellin ,  Giulio Volpe ,  Federico Sbrogio

IPC: C07D307/87

CPC classification number: C07D307/87

Abstract: A process for the preparation of citalopram of formula (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 in which the group Z is exchanged with cyanide by reaction with a cyanide source; the resultant crude citalopram product is optionally subjected to some initial purification and the crude citalopram base is subsequently subjected to a film distillation process; the resulting citalopram product is then optionally further purified and worked up and isolated as the base or a pharmaceutically acceptable salt thereof.

Abstract translation: 制备式（I）西酞普兰的方法，其中Z为碘，溴，氯或CF 3 - （CF 2）n -SO 2 -O-的式（II）化合物为0,1,2,3 ，4，5，6，7或8进行氰化物交换反应，其中基团Z与氰化物通过与氰化物源反应而与氰化物进行交换; 所得粗制西酞普兰产品任选进行一些初步纯化，随后对粗制西酞普兰碱进行膜蒸馏处理; 然后任选地将所得西酞普兰产物进一步纯化和处理并分离为碱或其药学上可接受的盐。