公开(公告)号：EP1678122A1

公开(公告)日：2006-07-12

申请号：EP03769715.8

申请日：2003-10-28

申请人： Wockhardt Limited ,  Jaweed Mukarram, Siddiqui Mohammed ,  Bhargav, Krishnaji Upadhye ,  Mishra, Krishna Gopalji ,  Farooqui, Mohammed Ismail

发明人： JAWEED MUKARRAM, Siddiqui Mohammed, Wockhardt Ltd. ,  BHARGAV, Krishnaji Upadhye, Wockhardt Ltd. ,  MISHRA, Krishna Gopalji, Wockhardt Ltd. ,  FAROOQUI, Mohammed Ismail, Wockhardt Ltd.

IPC分类号： C07C255/00 ,  C07D307/78 ,  C07D307/87

CPC分类号： C07D307/87 ,  C07C215/34

摘要： The present invention describes an improved process for the preparation of extremely pure 1-(4'-Fluorophenyl)-1-(3-dimethylaminopropyl)-5-phthalanecarbonitrile and its bromide salt (citalopram hydrobromide), which is a well known antidepressant. Other aspect of the invention are isolation of crystalline (4-Bromo-2-hydroxymethyl)phenyl-(4-fluorophenyl)-3-(dimethylaminopropyl)methanol (Bromodiol) and conversion of desmethylcitalopram which is formed during the cyanide exchange reaction, to Citalopram by heating with a mixture of formaldhyde and formic acid in chloroform. The resulting citalopram is conventionally purified using extraction methodology.

公开(公告)号：EP1678122A4

公开(公告)日：2007-05-23

申请号：EP03769715

申请日：2003-10-28

申请人： WOCKHARDT LTD ,  JAWEED MUKARRAM SIDDIQUI MOHAM ,  BHARGAV KRISHNAJI UPADHYE ,  MISHRA KRISHNA GOPALJI ,  FAROOQUI MOHAMMED ISMAIL

发明人： JAWEED MUKARRAM SIDDIQUI MOHAM ,  BHARGAV KRISHNAJI UPADHYE ,  MISHRA KRISHNA GOPALJI ,  FAROOQUI MOHAMMED ISMAIL

IPC分类号： C07C255/00 ,  C07C215/34 ,  C07D307/78 ,  C07D307/87

CPC分类号： C07D307/87 ,  C07C215/34

摘要： The present invention describes an improved process for the preparation of extremely pure 1-(4'-Fluorophenyl)-1-(3-dimethylaminopropyl)-5-phthalanecarbonitrile and its bromide salt (citalopram hydrobromide), which is a well known antidepressant. Other aspect of the invention are isolation of crystalline (4-Bromo-2-hydroxymethyl)phenyl-(4-fluorophenyl)-3-(dimethylaminopropyl)methanol (Bromodiol) and conversion of desmethylcitalopram which is formed during the cyanide exchange reaction, to Citalopram by heating with a mixture of formaldhyde and formic acid in chloroform. The resulting citalopram is conventionally purified using extraction methodology.