发明授权
- 专利标题: Method for the preparation of citalopram
- 专利标题(中): 西酞普兰制备方法
-
申请号: US09830109申请日: 2001-06-01
-
公开(公告)号: US06365747B1公开(公告)日: 2002-04-02
- 发明人: Leone Dall'Asta , Umberto Casazza , Hans Petersen
- 申请人: Leone Dall'Asta , Umberto Casazza , Hans Petersen
- 优先权: ITMI98A2242 19981020; ITMI99A1152 19990525; ITMI99A1724 19990802
- 主分类号: C07D30787
- IPC分类号: C07D30787
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.
信息查询