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1. 发明授权

US07812179B2 Process for the preparation of atorvastatin and intermediates 失效
标题翻译：制备阿托伐他汀和中间体的方法
公开(公告)号：US07812179B2
公开(公告)日：2010-10-12
申请号：US12222690
申请日：2008-08-14
申请人： Fan Wang , Daqing Che , Bhaskar Reddy Guntoori , Yajun Zhao , Aaron C. Kinsman , Jody Faught , Alan Chow
发明人： Fan Wang , Daqing Che , Bhaskar Reddy Guntoori , Yajun Zhao , Aaron C. Kinsman , Jody Faught , Alan Chow
IPC分类号： C07D207/333
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. 发明授权

US07615647B2 Process for producing atorvastatin hemicalcium 失效
标题翻译：生产阿托伐他汀半钙的方法
公开(公告)号：US07615647B2
公开(公告)日：2009-11-10
申请号：US11197413
申请日：2005-08-05
申请人： K.S. Keshava Murthy , Yajun Zhao , Daqing Che , Bhaskar Reddy Guntoori , Sammy Chris Duncan , Stephen E. Horne
发明人： K.S. Keshava Murthy , Yajun Zhao , Daqing Che , Bhaskar Reddy Guntoori , Sammy Chris Duncan , Stephen E. Horne
IPC分类号： C07D207/30
CPC分类号： C07D207/34 , C07D405/06 , Y02P20/55
摘要： A process is provided for preparing pharmaceutical grade atorvastatin hemicalcium salt comprising: (a) deesterifying, wherein R is an ester protecting group to (b) extracting R(R*,R*)-3 into an organic solvent or mixture of solvents, (c) adding a base of formula NR1R2R3 wherein R1, R2 and R3 are independently selected from H, substituted or non-substituted C1 to C7 alkyl, C6 to C9 aryl, C8 to C10 aralkyl or aminoalkyl to form atorvastatin base salt, (d) isolating by precipitation of the above atorvastatin base salt and purifying when necessary, (e) converting atorvastatin base salt to atorvastatin hemicalcium salt by treatment with a calcium salt solution, and (f) isolating the atorvastatin hemicalcium salt.
摘要翻译：提供用于制备药物级阿托伐他汀半钙盐的方法，其包括：（a）脱酯化，其中R是酯保护基团，以（b）将R（R *，R *） - 3提取到有机溶剂或溶剂混合物中 c）加入式NR1R2R3的碱，其中R1，R2和R3独立地选自H，取代或未取代的C1至C7烷基，C6至C9芳基，C8至C10芳烷基或氨基烷基以形成阿托伐他汀碱盐，（d）通过上述阿托伐他汀碱盐的沉淀分离并在需要时进行纯化，（e）通过用钙盐溶液处理将阿托伐他汀碱盐转化成阿托伐他汀半钙盐，和（f）分离阿托伐他汀半钙盐。

3. 发明授权

US07834195B2 Atorvastatin calcium propylene glycol solvates 有权
标题翻译：阿托伐他汀钙丙二醇溶剂化物
公开(公告)号：US07834195B2
公开(公告)日：2010-11-16
申请号：US11808942
申请日：2007-06-14
申请人： K. S. Keshava Murthy , Yajun Zhao , Allan W. Rey , Daqing Che , David A. Stradiotto , Uma Kotipalli
发明人： K. S. Keshava Murthy , Yajun Zhao , Allan W. Rey , Daqing Che , David A. Stradiotto , Uma Kotipalli
IPC分类号： C07D207/00
CPC分类号： C07D207/34
摘要： Atorvastatin calcium propylene glycol solvates and processes to prepare these novel solvates which are particularly useful and suitable for pharmaceutical applications.
摘要翻译：阿托伐他汀钙丙二醇溶剂化物并制备这些新的溶剂化物，这些新的溶剂合物特别有用并适用于药物应用。

4. 发明授权

US07745624B2 Preparation of acid addition salts of ziprasidone and intermediates thereof by solid phase-gas phase reactions 失效
标题翻译：通过固相 - 气相反应制备齐拉西酮的酸加成盐及其中间体
公开(公告)号：US07745624B2
公开(公告)日：2010-06-29
申请号：US11168524
申请日：2005-06-29
申请人： Allan W. Rey , Lotfi Derdour , K.S. Keshava Murthy , Probal Kanti Datta , Martin Ehlert , Stephen E. Home
发明人： Allan W. Rey , Lotfi Derdour , K.S. Keshava Murthy , Probal Kanti Datta , Martin Ehlert , Stephen E. Home
IPC分类号： C07D241/00 , C07D241/02
CPC分类号： C07D417/14
摘要： A process for the preparation of an acid addition salt of ziprasidone base and intermediates thereof comprising exposing the ziprasidone base in solid form to a gaseous acid in a substantially dry environment.
摘要翻译：一种制备齐拉西酮碱的酸加成盐的方法及其中间体，其包括将固体形式的齐拉西酮碱在基本干燥的环境中暴露于气态酸。

5. 发明授权

US07816355B1 Processes for the preparation of rivaroxaban and intermediates thereof 有权
标题翻译：制备利伐沙班及其中间体的方法
公开(公告)号：US07816355B1
公开(公告)日：2010-10-19
申请号：US12431272
申请日：2009-04-28
申请人： Prabhudas Bodhuri , Gamini Weeratunga
发明人： Prabhudas Bodhuri , Gamini Weeratunga
IPC分类号： A61K31/5377 , C07D413/14 , C07D413/10 , C07D295/155
CPC分类号： A61K31/5377 , C07D265/32 , C07D413/10 , C07D413/14
摘要： This invention provides a process for the preparation of S-Rivaroxaban and/or R-Rivaroxaban comprising reacting, in the presence of a first base, a compound of Formula 9: with a compound of Formula 8:
摘要翻译：本发明提供了一种制备S-里瓦罗沙班和/或R-里瓦沙班的方法，包括在第一碱的存在下使式9的化合物与式8的化合物反应：

6. 发明授权

US07485754B2 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：US07485754B2
公开(公告)日：2009-02-03
申请号：US11176361
申请日：2005-07-08
申请人： Zhi-Xian Wang , Mohammed Abdul Raheem , Gamini Weeratunga , Bhaskar Reddy Guntoori
发明人： Zhi-Xian Wang , Mohammed Abdul Raheem , Gamini Weeratunga , Bhaskar Reddy Guntoori
IPC分类号： C07C215/08
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。

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