Invention Grant
- Patent Title: Method for preparing citalopram diol intermediate
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Application No.: US15580517Application Date: 2015-06-09
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Publication No.: US10227293B2Publication Date: 2019-03-12
- Inventor: Zunjun Liang , Weifeng Xiao , Caihua Peng , Wenfeng Huang , Guoliang Tu
- Applicant: Zhejiang Huahai Pharmaceutical Co., Ltd , Zhejiang Huahai Licheng Pharmaceutical Co., Ltd , Zhejiang Huahai Jiancheng Pharmaceutical Co., Ltd
- Applicant Address: CN Linhai CN Linhai CN Linhai
- Assignee: Zhejiang Huahai Pharmaceutical Co., Ltd,Zhejiang Huahai Licheng Pharmaceutical Co., Ltd,Zhejiang Huahai Jiancheng Pharmaceutical Co., Ltd
- Current Assignee: Zhejiang Huahai Pharmaceutical Co., Ltd,Zhejiang Huahai Licheng Pharmaceutical Co., Ltd,Zhejiang Huahai Jiancheng Pharmaceutical Co., Ltd
- Current Assignee Address: CN Linhai CN Linhai CN Linhai
- Agency: Norton Rose Fulbright US LLP
- International Application: PCT/CN2015/081054 WO 20150609
- International Announcement: WO2016/197320 WO 20161215
- Main IPC: C07C253/30
- IPC: C07C253/30 ; C07C255/59 ; C07B49/00 ; C07F3/02

Abstract:
The present invention relates to a method for preparing a citalopram diol represented by formula IV, comprising the following steps: in the existence of an auxiliary reagent of metal salt, allowing 5-cyanophthalide to sequentially subjected to Grignard addition reactions with p-fluorophenyl magnesium halide and N, N-dimethylaminopropyl magnesium halide in an organic solvent; and after the reactions are completed, performing hydrolysis and separation to obtain citalopram diol represented by formula IV. In the present invention, by adding an auxiliary reagent of metal salt, the activity and the selectivity of the Grignard reactions are remarkably improved, and the reaction yield is obviously enhanced.
Public/Granted literature
- US20180162805A1 METHOD FOR PREPARING CITALOPRAM DIOL INTERMEDIATE Public/Granted day:2018-06-14
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