发明名称 A process for the preparation of racemic citalopram diol and/or S- or R- citalopram diols and the use of such diols for the preparation of racemic citalopram, R-citalopram and/or S-citalopram
摘要 In the following, citalopram diol means 4-(4-(dimethylamino)-l-(4- fluorophenyl)-1-hydroxybutyl)-3-(hydroxymethyl)-benzonitrile, as free base and/or acid addition salt. The invention relates to a process for the preparation of racemic citalopram diol and/or R- or S-citalopram diol, comprising the separation of a non-racemic mixture of R- and S- citalopram diol with more than 50% of one of the enantiomers into a fraction being enriched with S- or R-citalopram diol and a fraction comprising RS-citalopram diol wherein the ratio of R-citalopram diol:S- citalopram diol is equal to 1:1 or closer to 1:1 than in the initial mixture. The method is characterized in that (i) RS-citalopram diol is precipitated from a solution of the initial non-racemic mixture, or R- or S-citalopram diol is dissolved into a solvent from the initial non- racemic mixture, leaving a residue of RS-citalopram diol, and in that (ii) the residue/precipitate formed is separated from the final solution phase, followed by optional steps of repetition, recrystallisation, purification, isolation and conversion between free base and salts. The invention also relates to a process for the preparation of RS-citalopram, S-citalopram or R-citalopram (all as free base and/or acid addition salt) comprising the method described above followed by ring closure.
申请公布号 ZA200504715(B) 申请公布日期 2006.08.30
申请号 ZA20050004715 申请日期 2005.06.09
申请人 H. LUNDBECK A/S 发明人 HANS PETERSEN;ROBERT DANCER;BRIAN CHRISTIANSEN;HUMBLE, RIKKE, E.
分类号 C07C;C07C253/34;C07D;C07D307/87 主分类号 C07C
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