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1. 发明申请

WO2004083197A2 INTERMEDIATES FOR THE PREPARATION OF CITALOPRAM AND ESCITALOPRAM 审中-公开
标题翻译：中间体用于编写CITALOPRAM和ESCITALOPRAM
公开(公告)号：WO2004083197A2
公开(公告)日：2004-09-30
申请号：PCT/DK2004/000177
申请日：2004-03-17
申请人： H. LUNDBECK A/S , PITTELKOW, Thomas , CASTELLIN, Andrea , SBROGIO, Federico , DAHLBERG, Nielsen, Poul , ZANON, Jacopo , SØGAARD, Steen , HUMBLE, Rikke, Eva
发明人： PITTELKOW, Thomas , CASTELLIN, Andrea , SBROGIO, Federico , DAHLBERG, Nielsen, Poul , ZANON, Jacopo , SØGAARD, Steen , HUMBLE, Rikke, Eva
IPC分类号： C07D307/88
CPC分类号： C07D307/88
摘要： Methods for manufacture of 5-alkoxycarbonylphthtalides are disclosed. The 5-alkoxycarbonylphthtalides are useful in syntheses of the well-known antidepresssants citalopram and escitalopram.
摘要翻译：公开了制备5-烷氧基羰基二硫化物的方法。 5-烷氧基羰基萘甲酸盐用于合成众所周知的抗抑郁药西酞普兰和依他普仑。

2. 发明申请

WO2011134724A2 METHOD FOR PREPARING RITODRINE HYDROCHLORIDE 审中-公开
标题翻译：制备盐酸氯吡格雷的方法
公开(公告)号：WO2011134724A2
公开(公告)日：2011-11-03
申请号：PCT/EP2011/054565
申请日：2011-03-24
申请人： LUNDBECK PHARMACEUTICALS ITALY S.P.A. , ZANON, Jacopo , LIBRALON, Giovanna , DE FAVERI, Carla , HUBER, Florian Anton Martin
发明人： ZANON, Jacopo , LIBRALON, Giovanna , DE FAVERI, Carla , HUBER, Florian Anton Martin
IPC分类号： C07C215/60
CPC分类号： C07C215/60 , C07C213/08 , C07C213/10
摘要： The present invention describes a new method for preparing Ritodrinehydrochloride.The invention also concerns non-hygroscopic crystalline polymorphic Ritodrine hydrochloride Form (I).
摘要翻译：本发明描述了一种制备盐酸利多替罗的新方法。本发明还涉及非吸湿结晶多晶型盐酸雷托方（I）。

3. 发明申请

WO2004083197A3 INTERMEDIATES FOR THE PREPARATION OF CITALOPRAM AND ESCITALOPRAM 审中-公开
标题翻译：用于准备CITALOPRAM和ESCITALOPRAM的中间件
公开(公告)号：WO2004083197A3
公开(公告)日：2004-10-28
申请号：PCT/DK2004000177
申请日：2004-03-17
申请人： LUNDBECK & CO AS H , PITTELKOW THOMAS , CASTELLIN ANDREA , SBROGIO FEDERICO , DAHLBERG NIELSEN POUL , ZANON JACOPO , SOEGAARD STEEN , HUMBLE RIKKE EVA
发明人： PITTELKOW THOMAS , CASTELLIN ANDREA , SBROGIO FEDERICO , DAHLBERG NIELSEN POUL , ZANON JACOPO , SOEGAARD STEEN , HUMBLE RIKKE EVA
IPC分类号： C07D307/88
CPC分类号： C07D307/88
摘要： Methods for manufacture of 5-alkoxycarbonylphthtalides are disclosed. The 5-alkoxycarbonylphthtalides are useful in syntheses of the well-known antidepressants citalopram and escitalopram. A method for preparing an alkoxycarbonylphtalide of formula (III) comprising: (a) reacting a compound of formula (VIIIa) with a formaldehyde and oleum; and (b) addition of an alcohol R -OH to the reaction of step (a); wherein X and Y of formula (VIIIa) may be selected independently from the group consisting of: OR , OR , a halogen (such as C1, Br, I), and NR; wherein R, R and R are independently h or a C1-6 alkyl or phenyl.
摘要翻译：公开了5-烷氧基羰基噻吩的制备方法。 5-烷氧基羰基甜菜碱可用于合成已知的抗抑郁药西酞普兰和依他普仑。制备式（III）的烷氧基羰基化合物的方法，包括：（a）使式（VIIIa）化合物与甲醛和发烟硫酸反应; 和（b）向步骤（a）的反应中加入醇R 3 -OH; 其中式（VIIIa）的X和Y可以独立地选自：OR 1，OR 2，卤素（例如C 1，Br，I）和NR; 其中R，R 1和R 2独立地为h或C 1-6 - 烷基或苯基。

4. 发明申请

WO2010010058A1 METHOD OF PREPARING ANHYDROUS ALFUSOZIN HYDROCHLORIDE 审中-公开
标题翻译：制备无机盐酸氢氯化物的方法
公开(公告)号：WO2010010058A1
公开(公告)日：2010-01-28
申请号：PCT/EP2009/059284
申请日：2009-07-20
申请人： LUNDBECK PHARMACEUTICALS ITALY S.P.A. , ZANON, Jacopo , PIOVESANA, Tiziana , NICOLE', Andrea
发明人： ZANON, Jacopo , PIOVESANA, Tiziana , NICOLE', Andrea
IPC分类号： C07D405/12
CPC分类号： C07D405/12
摘要： There is described a method of preparing anhydrous alfuzosin hydrochloride by means of a condensation reaction between N 1 -methyl- N 2 -(tetrahydrodrofuroyl-2)-propylenediamine and 4-amino-2-chloro-6,7-dimethoxyquinazoline. The obtained crude product is subsequently purified by further stages that include steps of preparing novel intermediates. The described alfuzosin synthesis and purification process allow to obtain this active ingredient with a high yield and purity, and therefore suitable to be employed as an active ingredient in medicaments.
摘要翻译：描述了通过N 1 - 甲基-N 2-（四氢呋喃甲酰基-2） - 丙二胺和4-氨基-2-氯-6,7-二甲氧基喹唑啉之间的缩合反应制备无水阿夫唑嗪盐酸盐的方法。随后通过包括制备新型中间体的步骤的进一步阶段纯化获得的粗产物。所述的阿夫唑嗪合成和纯化方法允许以高产率和纯度获得该活性成分，因此适合用作药物中的活性成分。

5. 发明申请

WO2009124906A3 A POLYMORPH OF ARGATROBAN MONOHYDRATE AND A PROCESS FOR ITS SYNTHESIS 审中-公开
公开(公告)号：WO2009124906A3
公开(公告)日：2009-10-15
申请号：PCT/EP2009/054085
申请日：2009-04-06
申请人： LUNDBECK PHARMACEUTICALS ITALY S.P.A. , ZANON, Jacopo , LIBRALON, Giovanna , NICOLE', Andrea
发明人： ZANON, Jacopo , LIBRALON, Giovanna , NICOLE', Andrea
IPC分类号： C07D401/12
摘要： A method is described for preparing argatroban monohydrate obtained from (2R,4R)-1-[N G -nitro-N 2 -(3-methyl-8-quinolinesulphonyl)-L-arginyl]-4-methyl-2- piperidine carboxylic acid by suitably treating crude argatroban. The method either comprises preparation of argatroban monohydrate in a continuous step or an intermediate step of isolating a purified argatroban. Also obtainable from argatroban monohydrate is anhydrous argatroban, shown to have new physico- chemical characteristics. The described argatroban synthesis and purification process hence enables three different forms of argatroban, not previously described, to be obtained, each with distinctive physico-chemical characteristics and in particular enables argatroban monohydrate to be obtained with high yield and with high purity, being therefore a product suitable for use as active principle in proprietary medicines.

6. 发明申请

WO2009124906A2 METHOD FOR PREPARING ARGATROBAN MONOHYDRATE 审中-公开
标题翻译：制备阿糖胞苷单硬脂酸酯的方法
公开(公告)号：WO2009124906A2
公开(公告)日：2009-10-15
申请号：PCT/EP2009054085
申请日：2009-04-06
申请人： LUNDBECK PHARMACEUTICALS ITALY , ZANON JACOPO , LIBRALON GIOVANNA , NICOLE ANDREA
发明人： ZANON JACOPO , LIBRALON GIOVANNA , NICOLE ANDREA
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： A method is described for preparing argatroban monohydrate obtained from (2R,4R)-1-[NG-nitro-N2-(3-methyl-8-quinolinesulphonyl)-L-arginyl]-4-methyl-2- piperidine carboxylic acid by suitably treating crude argatroban. The method either comprises preparation of argatroban monohydrate in a continuous step or an intermediate step of isolating a purified argatroban. Also obtainable from argatroban monohydrate is anhydrous argatroban, shown to have new physico- chemical characteristics. The described argatroban synthesis and purification process hence enables three different forms of argatroban, not previously described, to be obtained, each with distinctive physico-chemical characteristics and in particular enables argatroban monohydrate to be obtained with high yield and with high purity, being therefore a product suitable for use as active principle in proprietary medicines.
摘要翻译：描述了从（2R，4R）-1- [NG-硝基-N 2 - （3-甲基-8-喹啉磺酰基）-L-精氨酰基] -4-甲基-2-哌啶羧酸得到的制备阿格曲班一水合物的方法，适当处理粗制阿加曲班。该方法包括在连续步骤中制备阿加曲班一水合物或分离纯化的阿加曲班的中间步骤。也可从阿加曲班一水合物获得的是无水阿加曲班，显示具有新的物理化学特性。所述的阿加曲班合成和纯化方法因此能够获得三种不同形式的阿加曲班，没有以前描述，其具有独特的物理化学特性，特别是能够以高产率和高纯度获得阿格曲班一水合物，因此是一种适用于专利药物活性成分的产品。

7. 发明申请

WO2003080597A1 METHOD FOR MANUFACTURE OF SERTINDOLE 审中-公开
标题翻译：方法制造系列
公开(公告)号：WO2003080597A1
公开(公告)日：2003-10-02
申请号：PCT/DK2003/000208
申请日：2003-03-26
申请人： H. LUNDBECK A/S , ZANON, Jacopo , VILLA, Marco , CIARDELLA, Francesco
发明人： ZANON, Jacopo , VILLA, Marco , CIARDELLA, Francesco
IPC分类号： C07D401/14
CPC分类号： C07D209/08 , C07D401/14
摘要： The present invention relates to a novel method for manufacture of sertindole comprising manufacturing 5-chloro-1-(4-fluorophenyl)-indole and converting it to sertindole wherein the method for manufacture of 5-chloro-1-(4-fluorophenyl)-indole comprises reacting 5-chloro-indole with a 4-fluorophenylhalide in the presence of a base, a chelating ligand and catalytic amounts of a copper salt comprising copper(I) or copper(II) and an anion which does not interfere in an unfavourable way with the reaction.
摘要翻译：本发明涉及一种制造三氯吲哚的新方法，包括制备5-氯-1-（4-氟苯基） - 吲哚并将其转化成三氢吲哚，其中制备5-氯-1-（4-氟苯基） - 吲哚的方法，吲哚包括在碱，螯合配体和催化量的包含铜（I）或铜（II）的铜盐和不妨碍不利的阴离子的存在下，使5-氯 - 吲哚与4-氟苯基卤反应方式与反应。

8. 发明申请

WO2011134724A3 METHOD FOR PREPARING RITODRINE HYDROCHLORIDE 审中-公开
标题翻译：制备盐酸氯吡格雷的方法
公开(公告)号：WO2011134724A3
公开(公告)日：2012-03-15
申请号：PCT/EP2011054565
申请日：2011-03-24
申请人： LUNDBECK PHARMACEUTICALS ITALY S P A , ZANON JACOPO , LIBRALON GIOVANNA , DE FAVERI CARLA , HUBER FLORIAN ANTON MARTIN
发明人： ZANON JACOPO , LIBRALON GIOVANNA , DE FAVERI CARLA , HUBER FLORIAN ANTON MARTIN
IPC分类号： C07C215/60 , C07C213/08 , C07C213/10
CPC分类号： C07C215/60 , C07C213/08 , C07C213/10
摘要： The present invention describes a new method for preparing Ritodrinehydrochloride.The invention also concerns non-hygroscopic crystalline polymorphic Ritodrine hydrochloride Form (I).
摘要翻译：本发明描述了一种制备盐酸利多替罗的新方法。本发明还涉及非吸湿结晶多晶型盐酸雷托方（I）。

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