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。