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1. 发明申请

US20060020140A1 Process for the preparation of racemic citalopram diol and/or s-or r-citalopram diols and the use of such diols for the preparation o racemic citalopram, r-citalopram and/or s-citalopram 失效
标题翻译：用于制备外消旋西酞普兰二醇和/或s-或r-西酞普兰二醇的方法和使用这种二醇制备外消旋西酞普兰，西酞普兰和/或西酞普兰
公开(公告)号：US20060020140A1
公开(公告)日：2006-01-26
申请号：US10540300
申请日：2003-12-18
申请人： Hans Petersen , Brian Christiansen , Robert dancer , Rikke Humble
发明人： Hans Petersen , Brian Christiansen , Robert dancer , Rikke Humble
IPC分类号： C07D307/78
CPC分类号： C07D307/87 , C07C253/34
摘要： In the following, citalopram diol means 4-(4-(dimethylamino)-1-(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.
摘要翻译：在下文中，西酞普兰二醇是指作为游离碱和/或酸加成盐的4-（4-（二甲基氨基）-1-（4-氟苯基）-1-羟基丁基）-3-（羟甲基） - 苄腈。本发明涉及一种制备外消旋西酞普兰二醇和/或R-或S-西酞普兰二醇的方法，包括将R-和S-西酞普兰二醇的非外消旋混合物与50％以上的对映体转化成富含S-或R-西酞普兰二醇的级分和包含RS-西酞普兰二醇的级分，其中R-西酞普兰二醇：西西酞普兰二醇的比例等于1:1或比1:1 初始混合物。该方法的特征在于（i）RS-西酞普兰二醇从初始非外消旋混合物的溶液中沉淀，或将R-或S-西酞普兰二醇从初始非外消旋混合物中溶解到溶剂中，留下残余物的RS-西酞普兰二醇，并且（ii）所形成的残余物/沉淀物与最终溶液相分离，随后重复，重结晶，纯化，分离和转化游离碱和盐之间的任选步骤。本发明还涉及一种制备RS-西酞普兰，西酞普兰或R-西酞普兰（均为游离碱和/或酸加成盐）的方法，包括上述方法，然后闭环。

2. 发明申请

US20050196453A1 Crystalline composition containing escitalopram 审中-公开
标题翻译：含有依他普仑的结晶组合物
公开(公告)号：US20050196453A1
公开(公告)日：2005-09-08
申请号：US10851763
申请日：2004-05-21
申请人： Kim Jensen , Rikke Humble , Ken Liljegren , Troels Christensen
发明人： Kim Jensen , Rikke Humble , Ken Liljegren , Troels Christensen
IPC分类号： A61K9/14 , A61K31/343 , C07D307/87
CPC分类号： A61K9/2054 , A61K31/343 , C07D307/87
摘要： The present invention discloses crystalline particles of escitalopram oxalate which either have a broad particle size distribution or comprise at least 0.01% (w/w) of Z-4-(4-dimethylamino-1-(4-fluorophenyl)-but-1-enyl)-3-hydroxymethyl-benzonitrile, said particles being suitable for use in direct compression. Furthermore, the invention discloses a novel pharmaceutical unit dosage form containing such crystalline particles of escitalopram oxalate as well as methods for manufacture of such crystalline particles of escitalopram oxalate Finally, the invention provides a method for reduction of the amount of hydroxyl containing impurities in a solution of citalopram or escitalopram.
摘要翻译：本发明公开了具有宽粒度分布或包含至少0.01％（w / w）的Z-4-（4-二甲基氨基-1-（4-氟苯基） - 丁-1-醇的结晶颗粒草酸依他酰丙酸盐，烯基）-3-羟甲基 - 苄腈，所述颗粒适用于直接压缩。此外，本发明公开了含有草酸艾司西酞普兰的结晶性颗粒的新颖的药物单位剂型，以及用于制造草酸艾司西酞普兰的结晶性颗粒的方法。最后，本发明提供一种减少溶液中含羟基杂质的量的方法的西酞普兰或依他普仑。

3. 发明申请

US20050197388A1 Crystalline composition containing escitalopram 失效
公开(公告)号：US20050197388A1
公开(公告)日：2005-09-08
申请号：US10948594
申请日：2004-09-23
申请人： Kim Jensen , Rikke Humble , Ken Liljegren , Troels Christensen
发明人： Kim Jensen , Rikke Humble , Ken Liljegren , Troels Christensen
IPC分类号： A61K9/14 , A61K31/343 , C07D307/87
CPC分类号： A61K9/2054 , A61K31/343 , C07D307/87
摘要： The present invention discloses crystalline particles of escitalopram oxalate which either have a broad particle size distribution or comprise at least 0.01% (w/w) of Z-4-(4-dimethylamino-1-(4-fluorophenyl)-but-1-enyl)-3-hydroxymethyl-benzonitrile, said particles being suitable for use in direct compression. Furthermore, the invention discloses a novel pharmaceutical unit dosage form containing such crystalline particles of escitalopram oxalate as well as methods for manufacture of such crystalline particles of escitalopram oxalate Finally, the invention provides a method for reduction of the amount of hydroxyl containing impurities in a solution of citalopram or escitalopram.

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