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1. 发明申请

US20060194867A1 PROCESS FOR THE PREPARATION OF ATORVASTATIN AND INTERMEDIATES 失效
标题翻译：制备ATORVASTATIN和中间体的方法
公开(公告)号：US20060194867A1
公开(公告)日：2006-08-31
申请号：US11099624
申请日：2005-04-06
申请人： Fan Wang , Daqing Che , Bhaskar Guntoori , Yajun Zhao , Aaron Kinsman , Jody Faught , Alan Chow
发明人： Fan Wang , Daqing Che , Bhaskar Guntoori , Yajun Zhao , Aaron Kinsman , Jody Faught , Alan Chow
IPC分类号： A61K31/401 , C07D207/34
CPC分类号： C07D207/34
摘要： A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 comprising: (a) reacting the aldehyde 1 with the enolate form of (S)-2-hydroxy-1,2,2-triphenylethyl acetate substituent in a chelating co-solvent; (b) hydrolysis of (R,S)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (S)-2-hydroxy-1,2,2-triphenylethyl ester (2a and 2b) using a base, preferably an alkali metal base, preferably in a solvent to form the carboxylic acid 7; (c) treating the acid 7 with a chiral base to form a salt and purifying the salt to obtain enantiomerically enriched (R)-7 chiral base salt; (d) alkylation of the (R)-7 chiral base salt or the free base derived from (R)-7, forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 and atorvastatin calcium 6, wherein R is a C1 to C6 alkyl, C6 to C9 aryl or C7 to C10 aralkyl.
摘要翻译：提供了制备（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -5-羟基-3-氧代-1-庚酸，R-取代的酯9，其包含：（a）使醛1与烯醇化形式的（S）-2-羟基-1,2,2-三苯基乙基乙酸酯取代基在螯合助溶剂中; （b）（R，S）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基 ] -3-羟基-1-戊酸，（S）-2-羟基-1,2,2-三苯基乙酯（2a和2b），使用碱，优选碱金属碱，优选在溶剂中形成羧酸酸7; （c）用手性碱处理酸7以形成盐并纯化该盐以获得对映体富集的（R）-7手性碱盐; （d）（R）-7手性碱盐或衍生自（R）-7的游离碱的烷基化，形成（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基） 3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -5-羟基-3-氧代-1-庚酸，R-取代的酯9和阿托伐他汀钙6，其中R是C1 C6烷基，C6〜C9芳基或C7〜C10芳烷基。

2. 发明申请

US20060252816A1 Process for the preparation of atorvastatin and intermediates 失效
公开(公告)号：US20060252816A1
公开(公告)日：2006-11-09
申请号：US11487500
申请日：2006-07-17
申请人： Fan Wang , Daqing Che , Bhaskar Guntoori , Yajun Zhao , Aaron Kinsman , Jody Faught , Alan Chow
发明人： Fan Wang , Daqing Che , Bhaskar Guntoori , Yajun Zhao , Aaron Kinsman , Jody Faught , Alan Chow
IPC分类号： A61K31/401
CPC分类号： C07D207/34
摘要： A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 comprising: (a) reacting the aldehyde 1 with the enolate form of (S)-2-hydroxy-1,2,2-triphenylethyl acetate substituent in a chelating co-solvent; (b) hydrolysis of (R,S)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (S)-2-hydroxy-1,2,2-triphenylethyl ester (2a and 2b) using a base, preferably an alkali metal base, preferably in a solvent to form the carboxylic acid 7; (c) treating the acid 7 with a chiral base to form a salt and purifying the salt to obtain enantiomerically enriched (R)-7 chiral base salt; (d) alkylation of the (R)-7 chiral base salt or the free base derived from (R)-7, forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 and atorvastatin calcium 6, wherein R is a C1 to C6 alkyl, C6 to C9 aryl or C7 to C10 aralkyl.

3. 发明申请

US20050203302A1 Preparation of atorvastatin 失效
标题翻译：阿托伐他汀的制备
公开(公告)号：US20050203302A1
公开(公告)日：2005-09-15
申请号：US10800741
申请日：2004-03-16
申请人： Bhaskar Guntoori , Daqing Che , Fan Wang , Yajun Zhao , K.S. Murthy , Stephen Horne
发明人： Bhaskar Guntoori , Daqing Che , Fan Wang , Yajun Zhao , K.S. Murthy , Stephen Horne
IPC分类号： C07D207/34 , C07D207/416 , C07D27/36
CPC分类号： C07D207/416 , C07D207/34
摘要： A process for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, tert-butylester comprising: (a) reduction of 5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-oxo-1-pentanoic acid, (R)-2-hydroxy-1,2,2-triphenylethyl ester; (b) hydrolysis of (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (R)-2-hydroxy-1,2,2-triphenylethyl ester using an alkali base in a solvent to form the acid; (c) alkylation of the acid forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, tert-butylester.
摘要翻译：制备（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] 包括：（a）还原5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -3-氧代-1-戊酸，（R）-2-羟基-1,2,2-三苯乙基酯; （b）（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -3-羟基-1-戊酸，（R）-2-羟基-1,2,2-三苯基乙基酯，使用碱在溶剂中形成酸; （c）酸形成（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1 - 基] -5-羟基-3-氧代-1-庚酸叔丁酯。

4. 发明申请

US20050165242A1 Process for the preparation of amorphous atorvastatin calcium 审中-公开
标题翻译：制备无定形阿托伐他汀钙的方法
公开(公告)号：US20050165242A1
公开(公告)日：2005-07-28
申请号：US10771383
申请日：2004-02-05
申请人： Daqing Che , Aaron Kinsman , Bhaskar Guntoori , K.S. Murthy
发明人： Daqing Che , Aaron Kinsman , Bhaskar Guntoori , K.S. Murthy
IPC分类号： A61K31/40 , A61P3/06 , C07D207/34 , C07D405/06 , C07D27/333
CPC分类号： C07D207/34 , C07D405/06
摘要： A process for the preparation of amorphous atorvastatin calcium and hydrates thereof, which comprises: (a) hydrolysis of the precursor lactone using sodium hydroxide to form atorvastatin sodium salt solution; (b) addition of the atorvastatin sodium salt solution to a calcium chloride or calcium acetate solution in the absence or presence of seeds of amorphous atorvastatin calcium; and (c) isolation of the resultant amorphous atorvastatin calcium salt by filtration and drying.
摘要翻译：一种制备无定形阿托伐他汀钙及其水合物的方法，其包括：（a）使用氢氧化钠水解前体内酯以形成阿托伐他汀钠盐溶液; （b）在不存在或存在无定形阿托伐他汀钙的种子的情况下将阿托伐他汀钠盐溶液加入到氯化钙或乙酸钙溶液中; 和（c）通过过滤和干燥分离得到的无定形阿托伐他汀钙盐。

5. 发明申请

US20050209460A1 Process for the preparation of torsemide and related intermediates 失效
标题翻译：制备托塞米及相关中间体的方法
公开(公告)号：US20050209460A1
公开(公告)日：2005-09-22
申请号：US10800740
申请日：2004-03-16
申请人： Daqing Che , Bhaskar Guntoori , Sammy Duncan
发明人： Daqing Che , Bhaskar Guntoori , Sammy Duncan
IPC分类号： C07D213/70 , C07D213/74
CPC分类号： C07D213/74
摘要： A process for preparing torsemide or salts thereof comprising: a) reacting II with isopropyl isocyanate in the presence of an alkali carbonate or bicarbonate and an organic solvent to form an alkali torsemide mixture, b) recovering the alkali torsemide mixture, and c) if desired, recovering the torsemide by acidification of the alkali torsemide mixture.
摘要翻译：一种制备托塞米或其盐的方法，其包括：a）在碱金属碳酸盐或碳酸氢盐和有机溶剂的存在下使II与异氰酸异丙酯反应以形成碱式载体混合物，b）回收碱式托塞米混合物，和c）如果需要，通过碱性托塞米特混合物的酸化来回收托塞米姆。

6. 发明申请

US20050282797A1 Process for the preparation of oxcarbazepine and related intermediates 失效
标题翻译：奥卡西平及相关中间体的制备方法
公开(公告)号：US20050282797A1
公开(公告)日：2005-12-22
申请号：US11153370
申请日：2005-06-16
申请人： Daqing Che , Nadia Corelli-Rennie , Bhaskar Guntoori , Jodi Faught
发明人： Daqing Che , Nadia Corelli-Rennie , Bhaskar Guntoori , Jodi Faught
IPC分类号： A61K31/55 , C07D223/18 , C07D223/22 , C07D223/26 , C07D223/28 , C07D223/30
CPC分类号： C07D223/26 , C07D223/28
摘要： A process for preparing Oxcarbazepine III comprising: a) reacting oximinostilbene IV with chlorosulfonyl isocyanate in an inert organic solvent and isolating compound V b) hydrolyzing compound V to form crude Oxcarbazepine III c) purifying oxcarbazepine.
摘要翻译：一种制备奥卡西平III的方法，包括：a）使肟基芪Ⅳ与氯代磺酰基异氰酸酯在惰性有机溶剂中反应并分离化合物Ⅴb）水解化合物V以形成粗制的奥卡西平III，c）纯化奥卡西平。

7. 发明申请

US20050059825A1 Novel process for the preparation of flecainide, its pharmaceutically acceptable salts and important intermediates thereof 失效
标题翻译：氟卡尼苷的制备方法，其药学上可接受的盐和重要的中间体
公开(公告)号：US20050059825A1
公开(公告)日：2005-03-17
申请号：US10663836
申请日：2003-09-17
申请人： Zhi-Xian Wang , Yuanqiang Li , Bhaskar Guntoori
发明人： Zhi-Xian Wang , Yuanqiang Li , Bhaskar Guntoori
IPC分类号： C07C51/363 , C07C51/367 , C07C65/21 , C07C67/14 , C07D211/26 , C07D211/32
CPC分类号： C07D211/26 , C07C51/363 , C07C51/367 , C07C65/21 , C07C67/14 , C07C69/92
摘要： Process for the preparation of Flecainide, its pharmaceutically acceptable salts and important intermediates thereof that involves the use of the 2-halobenzoic acid and its derivatives as a starting material. The use of this process also allows for the synthesis of a novel intermediate useful in the production of Flecainide. This new process is an inexpensive and efficient process for the manufacture of these compounds.
摘要翻译：制备涉及使用2-卤代苯甲酸及其衍生物作为起始原料的氟卡尼苷及其药学上可接受的盐和重要的中间体的方法。使用该方法还可以合成可用于生产氟卡尼的新型中间体。这种新方法是制造这些化合物的廉价和有效的方法。

8. 发明申请

US20070142644A1 Process for the preparation of zonisamide and the intermediates thereof 失效
标题翻译：制备唑尼沙胺及其中间体的方法
公开(公告)号：US20070142644A1
公开(公告)日：2007-06-21
申请号：US11304563
申请日：2005-12-16
申请人： Gamini Weeratunga , Eckardt Wolf , Nageib Mohamed , Allan Rey , Bhaskar Guntoori
发明人： Gamini Weeratunga , Eckardt Wolf , Nageib Mohamed , Allan Rey , Bhaskar Guntoori
IPC分类号： C07D261/20
CPC分类号： C07D261/20
摘要： The present invention provides a novel and improved process for the preparation of Zonisamide and the intermediates thereof. In one aspect of the present invention, the process provides for: the preparation and isolation of a novel crystalline form of anhydrous 1,2-benzisoxazole-3-methanesulfonic acid of formula 1; the direct chlorination of the acid of formula 1 into its acid chloride of formula 2; and the in situ conversion of the intermediate acid chloride of formula 2 into Zonisamide.
摘要翻译：本发明提供了制备唑尼沙胺及其中间体的新颖和改进的方法。在本发明的一个方面，该方法提供：制备和分离式1的无水1,2-苯并异恶唑-3-甲磺酸的新结晶形式; 将式1的酸直接氯化成式2的酰氯; 并将式2的中间体酰氯原位转化成唑尼沙胺。

9. 发明申请

US20070010678A1 Efficient method for preparing 3-aryloxy-3-arylpropylamines and their optical stereoisomers 有权
标题翻译：制备3-芳氧基-3-芳基丙胺及其光学立体异构体的有效方法
公开(公告)号：US20070010678A1
公开(公告)日：2007-01-11
申请号：US11176361
申请日：2005-07-08
申请人： Zhi-Xian Wang , Mohammed Raheem , Gamini Weeratunga , Bhaskar Guntoori
发明人： Zhi-Xian Wang , Mohammed Raheem , Gamini Weeratunga , Bhaskar Guntoori
IPC分类号： C07D333/20
CPC分类号： C07D333/20
摘要： Provided is an efficient method for the preparation of 3-aryloxy-3-arylpropylamines, their optical stereoisomers, and pharmaceutically acceptable salts thereof. The process allows for the isolation of 3-aryloxy-3-arylpropylamines in high yield and purity. The present invention further relates to a process for producing fluoxetine, tomoxetine, norfluoxetine, duloxetine, nisoxetine, and their optically enriched (R)— and (S)-enantiomers.
摘要翻译：提供了制备3-芳氧基-3-芳基丙胺，其光学立体异构体及其药学上可接受的盐的有效方法。该方法允许以高产率和纯度分离3-芳氧基-3-芳基丙胺。本发明还涉及氟西汀，托莫西汀，诺氟西汀，度洛西汀，尼索西汀及其光学富集的（R） - 和（S） - 对映异构体的制备方法。

10. 发明申请

US20080033181A1 Process for the preparation of Zonisamide and the intermediates thereof 审中-公开
标题翻译：制备唑尼沙胺及其中间体的方法
公开(公告)号：US20080033181A1
公开(公告)日：2008-02-07
申请号：US11806090
申请日：2007-05-30
申请人： Gamini Weeratunga , Eckardt Wolf , Nageib Mohamed , Allan Rey , Bhaskar Guntoori
发明人： Gamini Weeratunga , Eckardt Wolf , Nageib Mohamed , Allan Rey , Bhaskar Guntoori
IPC分类号： C07D261/20
CPC分类号： C07D261/20
摘要： The present invention provides a novel and improved process for the preparation of Zonisamide and the intermediates thereof. In one aspect of the present invention, the process provides for: the preparation and isolation of a novel crystalline form of anhydrous 1,2-benzisoxazole-3-methanesulfonic acid of formula 1; the direct chlorination of the acid of formula 1 into its acid chloride of formula 2; and the in situ conversion of the intermediate acid chloride of formula 2 into Zonisamide.
摘要翻译：本发明提供了制备唑尼沙胺及其中间体的新颖和改进的方法。在本发明的一个方面，该方法提供：制备和分离式1的无水1,2-苯并异恶唑-3-甲磺酸的新结晶形式; 将式1的酸直接氯化成式2的酰氯; 并将式2的中间体酰氯原位转化成唑尼沙胺。

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