METHOD FOR PREPARING CITALOPRAM DIOL INTERMEDIATE |
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| 申请号 | US15580517 | 申请日 | 2015-06-09 | 公开(公告)号 | US20180162805A1 | 公开(公告)日 | 2018-06-14 |
| 申请人 | Zhejiang Huahai Pharmaceutical Co., Ltd; Zhejiang Huahai Jiancheng Pharmaceutical Co., Ltd; | 发明人 | Zunjun LIANG; Weifeng XIAO; Caihua PENG; Wenfeng HUANG; Guoliang TU; | ||||
| 摘要 | 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. | ||||||
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| 说明书全文 | |||||||
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