首页> 外国专利> PROCEDURE FOR THE PREPARATION OF CITALOPRAM RACEMICO AND / OR CITALOPRAM-S OR -R BY SEPARATION OF A MIXTURE OF CITALOPRAM-R AND -S.

PROCEDURE FOR THE PREPARATION OF CITALOPRAM RACEMICO AND / OR CITALOPRAM-S OR -R BY SEPARATION OF A MIXTURE OF CITALOPRAM-R AND -S.

机译:通过分离CITALOPRAM-R和-S的混合物来制备CITALOPRAM RACEMICO和/或CITALOPRAM-S或-R的方法。

摘要

A process for the preparation of a racemic citalopram free base or an acid addition salt thereof and / or citalopram-R or -S as a free base or an acid addition salt thereof by separating a mixture of citalopram-R and -S with more than 50% of one of the enantiomers in a fraction consisting of racemic citalopram and a fraction of citalopram-S or citalopram-R characterized in that: i) citalopram is precipitated from a solvent as a free base or as a salt of acid addition thereof; ii) the precipitate formed is separated from the mother liquor; iia) if the precipitate is crystalline, it is optionally recrystallized one or more times to form racemic 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 this crystalline precipitate is optionally recrystallized one or more times to form racemic citalopram and then optionally converted into a salt of acid addition thereof.
机译:外消旋的西酞普兰游离碱或其酸加成盐和/或作为游离碱的西酞普兰-R或-S或其酸加成盐的制备方法是通过将西酞普兰-R和-S的混合物与在由外消旋西酞普兰和西酞普兰-S或西酞普兰-R组成的馏分中的一种对映体的50%,其特征在于:i)西酞普兰以游离碱或其酸加成盐的形式从溶剂中沉淀出来; ii)将形成的沉淀物与母液分离; iia)如果沉淀是结晶的,则其任选地重结晶一次或多次以形成外消旋西酞普兰,然后任选地转化为其酸加成盐。 iib)如果沉淀物不是结晶的,则任选地重复步骤i)和ii),直到获得结晶沉淀物为止,并且该结晶沉淀物任选地重结晶一次或多次以形成外消旋西酞普兰,然后任选地转化为其酸加成盐。

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