发明名称 Process for the preparation of pure citalopram (5-cyano-1-(3-dimethylaminopropyl)-1-(4-fluorophenyl)phthalane) by reacting 5-substituted-1-(3-dimethylaminopropyl)-1-(4-fluorophenyl)phthalane with a cyanide source, then subjecting the crude citalopram product to a film distillation process
摘要 Process for the preparation of citalopram of formula I in which a compound of formula II is subjected to a cyanide exchange reaction in which the group Z is exchanged with cyanide by reaction with a cyanide source. The resultant crude citalopram product is optionally subjected to some initial purification. The crude citalopram base is then subjected to a film distillation process. The resulting citalopram product is then optionally further purified and worked up and isolated as the base or a pharmaceutically acceptable salt thereof. In the compound of formula II, Z is I, Br, Cl or CF3-(CF2)n-SO2-O-, where n is 0, 1, 2, 3, 4, 5, 6, 7 or 8. Also described is citalopram whenever prepared by the above-described process.
申请公布号 NZ516299(A) 申请公布日期 2002.12.20
申请号 NZ20010516299 申请日期 2001.12.20
申请人 H 发明人 CASTELLIN, ANDREA;VOLPE, GIULIO;SBROGIO, FEDERICO
分类号 A61P25/24;C07D307/87;(IPC1-7):C07D307/87 主分类号 A61P25/24
代理机构 代理人
主权项
地址