发明名称 PROCESS FOR THE PREPARATION OF RACEMIC CITALOPRAM AND/OR S- OR R-CITALOPRAM BY SEPARATION OF A MIXTURE OF R- AND S-CITALOPRAM
摘要 The invention relates to a process for the preparation of racemic citalopram free base or an acid addition salt thereof and/or R- or S-citalopram as the free base or an acid addition salt thereof by separation of a mixture of R- and S-citalopram with more than 50% of one of the enantiomers into a fractio n consisting of racemic citalopram and/or a fraction of S-citalopram or R- citalopram characterized in that i) citalopram is precipitated from a solven t as the free base or as an acid addition salt thereof; ii) the precipitate formed is separated from the mother liquor; iia) if the precipitate is crystalline it is optionally recrystallised one or more times to form racemi c citalopram, and then optionally converted into an acid addition salt thereof ; iib) if the precipitate is not crystalline, steps i) and ii) are optionally repeated until a crystalline precipitate is obtained and the crystalline precipitate is recrystallised one or more times to form racemic citalopram, and then optionally converted into an acid addition salt thereof; iii) the mother liquor is optionally subjected to further purification and S-citalopr am or R-citalopram is isolated from the mother liquor and optionally converted into an acid addition salt thereof.
申请公布号 CA2450890(A1) 申请公布日期 2003.01.03
申请号 CA20022450890 申请日期 2002.06.25
申请人 H. LUNDBECK A/S 发明人 CHRISTENSEN, TROELS VOLSGAARD;HUMBLE, RIKKE EVA;DANCER, ROBERT;PETERSEN, HANS;NIELSEN, OLE;ROCK, MICHAEL HAROLD
分类号 A61K31/343;A61P25/24;C07B57/00;C07C253/30;C07D;C07D307/87;C07D307/93;(IPC1-7):C07D307/87 主分类号 A61K31/343
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