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Process for the preparation of the Racemic citalopram and citalopram or - S - R through the separation of a mixture of R - and S - citalopram
专利权人:
H. LUNDBECK A/S
发明人:
申请号:
ARP110103869
公开号:
AR083483A2
申请日:
2011.10.19
申请国别(地区):
AR
年份:
2013
代理人:
摘要:
A process for the preparation of Racemic citalopram in the form of a Free Base or an Acid Addition Salt thereof, and / or for the preparation of R - or S - citalopram in the form of a Free Base or an Acid Addition Salt thereof, through the separation of a m Ezcla of R - and S - containing one of citalopram enantiomers in a concentration higher than 50%.In a fraction of a fraction of Racemic citalopram and citalopram or S - R - Where: (i) citalopram citalopram is precipitated from the Solvent, in the form of a Free Base or a Salt thereof obtained by adding an Acid precipitated material; (ii) Formed is separated from the mother Liquor; ii) if the precipitated material is Crystalline,Optionally, one or more times is recrystallized by way of Forming Racemic citalopram, after which is optionally converted into a Salt thereof obtained by the addition of an Acid; b) if the material is not Crystalline Precipitate, optionally repeating the steps (i) and (ii) Sta to obtain a material precipitated CrystallineAnd the Crystalline precipitate recrystallised material is optionally one or more times by way of Forming Racemic citalopram, after which is optionally converted into a Salt thereof by the addition of an Acid; (iii) optionally the mother Liquor is subjected to further purification Onal,The S - and R - citalopram or citalopram is isolated from the mother Liquor and optionally become a Salt thereof by the addition of an Acid, where the mixture of R - and S - citalopram with more than 50% of the s-enantiomer is prepared from a mixture of R - and S - 4 - [4 - (dimethylamino) - 1 - (4 - fluorofeni L) - 1 - hidroxibutil] - 3 - (hydroxymethyl) - Benzonitrile with more than 50% of the S - enantiomer by TrainingN a labile Ester Group, after which closes the ring in a basic environment; or the mixture of R - and S - citalopram with more than 50% of the R enantiomer is prepared from a mixture of R - and S - 4 - [4 - (dimethylamino) - 1 - (4-fluorophenyl) - 1 - hidroxibutil] - 3 - (h
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