专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 发明申请

WO2011000539A1 METHOD OF PREPARING NERAMEXANE 审中-公开
标题翻译：制备NERAMEXANE的方法
公开(公告)号：WO2011000539A1
公开(公告)日：2011-01-06
申请号：PCT/EP2010/003922
申请日：2010-06-28
申请人： MERZ PHARMA GMBH & CO. KGAA , KOLLER, Herbert , PYERIN, Michael , SBROGIO, Federico
发明人： KOLLER, Herbert , PYERIN, Michael , SBROGIO, Federico
IPC分类号： C07C209/62 , C07C209/16 , C07C211/35
CPC分类号： C07C211/35 , C07C209/62 , C07C2601/14
摘要： Method of preparing 1-amino-1,3,3,5,5-pentamethylcyclohexane or a pharmaceutically acceptable salt thereof, comprising at least two steps selected from the following steps (i) to (iv): (i) converting isophorone to 3,3,5,5-tetramethylcyclohexanone in the presence of methylmagnesium chloride; (N) converting 3,3,5,5-tetramethylcyclohexanone to 1-hydroxy-1,3,3,5,5- pentamethylcyclohexane in the presence of methylmagnesium chloride; (iii) converting 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane to 1-chloroacetamido- 1,3,3,5,5-pentamethylcyclohexane in the presence of chloroacetonitrile in acidic solution; (iv) converting 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane to 1-amino- 1,3,3,5,5-pentamethylcyclohexane in the presence of thiourea in water.
摘要翻译：制备1-氨基-1,3,3,5,5-五甲基环己烷或其药学上可接受的盐的方法，其包含选自以下步骤（i）至（iv）中的至少两个步骤：（i）将异佛尔酮转化为3 ，3,5,5-四甲基环己酮在甲基氯化镁存在下反应; （N）在甲基氯化镁存在下将3,3,5,5-四甲基环己酮转化成1-羟基-1,3,3,5,5-五甲基环己烷; （iii）在氯乙腈存在下，在酸性溶液中将1-羟基-1,3,3,5,5-五甲基环己烷转化为1-氯乙酰氨基-1,3,3,5,5-五甲基环己烷; （iv）在硫脲在水存在下将1-氯乙酰氨基-1,3,3,5,5-五甲基环己烷转化为1-氨基-1,3,3,5,5-五甲基环己烷。

3. 发明申请

WO2010118889A1 SYNTHESIS OF 1-AMINO-1,3,3,5,5-PENTAMETHYLCYCLOHEXANE MESYLATE 审中-公开
标题翻译： 1-氨基-1,3,3,5,5-三甲氧基环己烷甲酸酯的合成
公开(公告)号：WO2010118889A1
公开(公告)日：2010-10-21
申请号：PCT/EP2010/002361
申请日：2010-04-16
申请人： MERZ PHARMA GMBH & CO. KGAA , HENRICH, Markus , NEGURA, Simona , TASI, Gergely , KOCSÁN, Pál , SBROGIO, Federico , PYERIN, Michael , KOLLER, Herbert
发明人： HENRICH, Markus , NEGURA, Simona , TASI, Gergely , KOCSÁN, Pál , SBROGIO, Federico , PYERIN, Michael , KOLLER, Herbert
IPC分类号： C07C303/32 , C07C211/35 , C07C309/04 , A61K31/13
CPC分类号： C07C303/32 , C07C29/40 , C07C209/16 , C07C209/68 , C07C209/84 , C07C209/86 , C07C211/35 , C07C2601/14 , Y10T428/2982 , C07C35/08 , C07C309/04
摘要： Process for manufacturing 1-amino-1,3,3, 5, 5-pentamethylcyclohexane mesylate comprising step (i): (i) reacting 1-amino-1, 3, 3, 5, 5-pentamethylcyclohexane with methane sulfonic acid in a solvent or a mixture of two or more solvents selected among anisole, cumene; pentane, hexane, heptane, isooctane; methyl acetate, propyl acetate, isopropyl acetate, n-butyl acetate, isobutyl acetate; methyl ethyl ketone, methyl isopropylketone, methyl isobutyl ketone; dimethyl sulphoxide; tetrahydrofurane, methyltetrahydrofurane, 1,1-diethoxypropane, 1,1-dimethoxymethane, and 2,2-dimethoxypropane.
摘要翻译：包括步骤（i）的1-氨基-1,3,3,5,5-五甲基环己烷甲磺酸酯的制备方法：（i）使1-氨基-1,3,3,5,5-五甲基环己烷与甲磺酸反应，溶剂或两种或更多种选自苯甲醚，异丙基苯的溶剂的混合物; 戊烷，己烷，庚烷，异辛烷; 乙酸甲酯，乙酸丙酯，乙酸异丙酯，乙酸正丁酯，乙酸异丁酯; 甲基乙基酮，甲基异丙基酮，甲基异丁基酮; 二甲基亚砜四氢呋喃，甲基四氢呋喃，1,1-二乙氧基丙烷，1,1-二甲氧基甲烷和2,2-二甲氧基丙烷。

4. 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。

5. 发明申请

WO0147877A3 PROCESS FOR THE PREPARATION OF PURE CITALOPRAM 审中-公开
标题翻译：制备纯CITALOPRAM的工艺
公开(公告)号：WO0147877A3
公开(公告)日：2001-12-27
申请号：PCT/DK0100148
申请日：2001-03-07
申请人： LUNDBECK & CO AS H , CASTELLIN ANDREA , VOLPE GIULIO , SBROGIO FEDERICO
发明人： CASTELLIN ANDREA , VOLPE GIULIO , SBROGIO FEDERICO
IPC分类号： A61P25/24 , C07D307/87
CPC分类号： C07D307/87
摘要： A process for the preparation of citalopram of formula (I) in which a compound of formula (II) wherein Z is iodo, bromo, chloro or CF3-(CF2)n-SO2-O- n being 0, 1, 2, 3, 4, 5, 6, 7 or 8, is subjected to a cyanide exchange reaction in which the group Z is exchanged with cyanide by reaction with a cyanide source; the resultant crude citalopram product is optionally subjected to some initial purification and the crude citalopram base is subsequently subjected to a film distillation process; the resulting citalopram product is then optionally further purified and worked up and isolated as the base or a pharmaceutically acceptable salt thereof.
摘要翻译：制备式（I）的西酞普兰的方法，其中Z为碘，溴，氯或CF 3 - （CF 2）n -SO 2 -O-的式（II）化合物为0,1,2,3 ，4，5，6，7或8进行氰化物交换反应，其中基团Z与氰化物通过与氰化物源反应而与氰化物进行交换; 所得粗制西酞普兰产品任选进行一些初步纯化，随后对粗制西酞普兰碱进行膜蒸馏处理; 然后任选地将所得西酞普兰产物进一步纯化和处理并分离为碱或其药学上可接受的盐。

6. 发明申请

WO2007054105A2 METHOD FOR THE PREPARATION OF ESCITALOPRAM 审中-公开
标题翻译：用于制备ESCITALOPRAM的方法
公开(公告)号：WO2007054105A2
公开(公告)日：2007-05-18
申请号：PCT/DK2006050067
申请日：2006-11-14
申请人： LUNDBECK & CO AS H , PAULON ANTONIO , DE LUCCI OTTORINO , CASTELLIN ANDREA , FABRIS FABRIZIO , SBROGIO FEDERICO , CERON EMANUELE , PETERSEN HANS , DANCER ROBERT
发明人： PAULON ANTONIO , DE LUCCI OTTORINO , CASTELLIN ANDREA , FABRIS FABRIZIO , SBROGIO FEDERICO , CERON EMANUELE , PETERSEN HANS , DANCER ROBERT
IPC分类号： C07D493/18 , C07D307/87 , C07D407/04
CPC分类号： C07D307/87 , C07D407/04
摘要： The invention relates to novel intermediates and the use thereof in a novel method for the preparation of escitalopram.
摘要翻译：本发明涉及新型中间体及其在制备艾司西酞普兰的新方法中的应用。

7. 发明申请

WO0145483A3 METHOD FOR THE PREPARATION OF PURE CITALOPRAM 审中-公开
标题翻译：制备纯立方厘米的方法
公开(公告)号：WO0145483A3
公开(公告)日：2001-12-27
申请号：PCT/DK0100147
申请日：2001-03-07
申请人： LUNDBECK & CO AS H , VILLA MARCO , SBROGIO FEDERICO , DANCER ROBERT
发明人： VILLA MARCO , SBROGIO FEDERICO , DANCER ROBERT
IPC分类号： A61P25/24 , C07B61/00 , C07D307/87 , H01L21/00
CPC分类号： C07D307/87
摘要： The present invention relates to a process for the preparation and purification of citalopram (I) in which a compound of Formula (II) wherein Z is iodo, bromo, chloro or CF3-(CF2)n-SO2-O-, n being 0, 1, 2, 3, 4, 5, 6, 7 or 8, is subjected to a cyanide exchange reaction with a cyanide source; the resultant crude citalopram product is optionally subjected to some initial purification and subsequently treated with an amide or an amide-like group forming agent; the reaction mixture is then subjected to an acid/base wash and/or crystallisation and recrystallisation of citalopram in order to remove the amides formed from the crude citalopram mixture; and the resulting citalopram product is optionally further purified, worked up and isolated as the base or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及西酞普兰（I）的制备和纯化方法，其中Z为碘，溴，氯或CF 3 - （CF 2）n -SO 2 -O-的式（II）化合物，n为0 ，1，2，3，4，5，6，7或8，与氰化物源进行氰化物交换反应; 所得粗制西酞普兰产品任选进行一些初始纯化，随后用酰胺或类酰胺形成剂处理; 然后将反应混合物进行酸/碱洗涤和/或结晶并重结晶西酞普兰以除去由西酞普兰粗制混合物形成的酰胺; 任选地进一步纯化，后处理和分离得到的西酞普兰产物作为碱或其药学上可接受的盐。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式