- 专利标题: Method for the preparation of citalopram
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申请号: US09794762申请日: 2001-02-26
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公开(公告)号: US06420574B1公开(公告)日: 2002-07-16
- 发明人: Hans Petersen , Michael Harold Rock , Haleh Ahmadian
- 申请人: Hans Petersen , Michael Harold Rock , Haleh Ahmadian
- 优先权: DK200000296 20000224; DK200000401 20000313
- 主分类号: C07D30778
- IPC分类号: C07D30778
摘要:
The present invention relates to a method for the preparation of citalopram comprising reaction a compound of formula (I) with a compound having the formula wherein X is a suitable leaving group and R is —CH2—O—Pg, —CH2—NPg1Pg2, —CO—N(CH3)2, —CH(OR1)(OR2), —C(OR4)(OR5)(OR6), —COOR3, —CH2—CO—NH2, —CH═CHR7 and —CONHR8, wherein Pg is a protection group for an alcohol group, Pg1 and Pg2 are protection groups for an amino group, R1 and R2 are independently selected from alkyl, alkenyl, alkynyl and optionally alkyl substituted aryl or aralkyl groups or R1 and R2 together form a chain of 2 to 4 carbon atoms, each of R3, R4, R5, R6 and R7 are independently selected from alkyl, alkenyl, alkynyl and optionally alkyl substituted aryl or aralkyl and R8 is hydrogen or methyl; to form a compound of the formula wherein R is as defined above; followed by conversion of the R group and isolation of citalopram base or a pharmaceutically acceptable salt thereof.
公开/授权文献
- US20010027256A1 Method for the preparation of citalopram 公开/授权日:2001-10-04
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