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1. 发明授权

US07863442B2 Processes for the synthesis of olanzapine 失效
标题翻译：奥氮平合成方法
公开(公告)号：US07863442B2
公开(公告)日：2011-01-04
申请号：US11976978
申请日：2007-10-30
申请人： Kiran Kumar Kothakonda , Daqing Che , Bhaskar Reddy Guntoori
发明人： Kiran Kumar Kothakonda , Daqing Che , Bhaskar Reddy Guntoori
IPC分类号： C07D495/02
CPC分类号： C07D495/04
摘要： There is provided a process for the preparation of olanzapine comprising: i) reacting 4-amino-2-methyl-10H-thieno-[2,3-b][1,5]benzodiazepine and N-methylpiperazine in a C1 to C4 alcoholic solvent or mixture thereof at suitable temperature and for a suitable time, ii) cooling the reaction mixture, and iii) isolating the precipitated olanzapine.
摘要翻译：提供了一种制备奥氮平的方法，其包括：i）使4-氨基-2-甲基-10H-噻吩并[2,3-b] [1,5]苯并二氮杂和N-甲基哌嗪在C1至C4醇中反应溶剂或其混合物在合适的温度和合适的时间，ii）冷却反应混合物，和iii）分离沉淀的奥氮平。

2. 发明申请

US20080319189A1 Processes for the synthesis of olanzapine 失效
标题翻译：奥氮平合成方法
公开(公告)号：US20080319189A1
公开(公告)日：2008-12-25
申请号：US11976978
申请日：2007-10-30
申请人： Kiran Kumar Kothakonda , Daqing Che , Bhaskar Reddy Guntoori
发明人： Kiran Kumar Kothakonda , Daqing Che , Bhaskar Reddy Guntoori
IPC分类号： C07D243/10
CPC分类号： C07D495/04
摘要： There is provided a process for the preparation of olanzapine comprising: i) reacting 4-amino-2-methyl-10H-thieno-[2,3-b][1,5]benzodiazepine and N-methylpiperazine in a C1 to C4 alcoholic solvent or mixture thereof at suitable temperature and for a suitable time, ii) cooling the reaction mixture, and iii) isolating the precipitated olanzapine.
摘要翻译：提供了一种制备奥氮平的方法，其包括：i）使4-氨基-2-甲基-10H-噻吩并[2,3-b] [1,5]苯并二氮杂和N-甲基哌嗪在C1至C4醇中反应溶剂或其混合物在合适的温度和合适的时间，ii）冷却反应混合物，和iii）分离沉淀的奥氮平。

3. 发明申请

US20080312433A1 Novel process to Form-I of olanzapine 审中-公开
标题翻译：奥氮平的一种新方法
公开(公告)号：US20080312433A1
公开(公告)日：2008-12-18
申请号：US11976944
申请日：2007-10-30
申请人： Daqing Che , Kiran Kumar Kothakonda , Cameron L. McPhail , Bhaskar Reddy Guntoori
发明人： Daqing Che , Kiran Kumar Kothakonda , Cameron L. McPhail , Bhaskar Reddy Guntoori
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： A process for obtaining crystalline Form-I olanzapine comprising the following: a) dissolving crude olanzapine in a solvent to form a solution, b) optionally drying by azeotropic distillation to remove water, c) precipitating by adding the solution of step (a) to an antisolvent, and d) isolating the precipitated crystalline Form-I olanzapine by filtration and drying at ambient temperature.
摘要翻译：一种获得结晶形式的奥氮平的方法，包括以下步骤：a）将粗奥氮平溶于溶剂中以形成溶液，b）任选地通过共沸蒸馏干燥除去水，c）通过将步骤（a）的溶液加入到反溶剂，以及d）通过过滤并在环境温度下干燥分离析出的结晶的形式I奥氮平。

4. 发明申请

US20090131683A1 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：US20090131683A1
公开(公告)日：2009-05-21
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。

5. 发明授权

US06586593B1 Efficient process for the preparation of lamotrigine and related 3,5-diamino-6-substituted-1,2,4-triazines 失效
标题翻译：制备拉莫三嗪及其相关的3,5-二氨基-6-取代-1,2,4-三嗪的高效方法
公开(公告)号：US06586593B1
公开(公告)日：2003-07-01
申请号：US10046383
申请日：2002-01-16
申请人： Bhaskar Reddy Guntoori , Daqing Che , K. S. Keshava Murthy
发明人： Bhaskar Reddy Guntoori , Daqing Che , K. S. Keshava Murthy
IPC分类号： C07D253075
CPC分类号： C07D253/075
摘要： A process for the manufacture of 3,5-diamino-6-substituted-1,2,4-triazines is disclosed which comprises the steps of: (a) reacting a compound of formula (II): with aminoguanidine salts, (b) dehydrating the compound obtained to form a compound of formula IV, and (c) cyclization of the compound of formula IV into a 3,5-diamino-6-substituted-1,2,4-triazine compound of formula I or into a hydrated form thereof.
摘要翻译：公开了制备3,5-二氨基-6-取代-1,2,4-三嗪的方法，其包括以下步骤：（a）使式（II）化合物与氨基胍盐反应，（b）使获得的化合物脱水以形成式IV化合物，和（c）将式IV化合物环化为式I的3,5-二氨基-6-取代-1,2,4-三嗪化合物或水合形式。

6. 发明授权

US07112604B2 Process for the preparation of Atorvastatin and intermediates 失效
标题翻译：阿托伐他汀和中间体的制备方法
公开(公告)号：US07112604B2
公开(公告)日：2006-09-26
申请号：US11099624
申请日：2005-04-06
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： A61K31/4025 , C07D207/327
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，得到对映体富集的（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。

7. 发明授权

US06858747B2 Process to prepare, 1,4-dihydropyridine intermediates and derivatives thereof 失效
标题翻译：制备方法，1,4-二氢吡啶中间体及其衍生物
公开(公告)号：US06858747B2
公开(公告)日：2005-02-22
申请号：US10819910
申请日：2004-04-08
申请人： Daqing Che , Bhaskar Reddy Guntoori , K. S. Keshava Murthy
发明人： Daqing Che , Bhaskar Reddy Guntoori , K. S. Keshava Murthy
IPC分类号： C07D211/90 , C07C69/79 , C07C205/00
CPC分类号： C07D211/90
摘要： An improved catalyst is disclosed for a process involving the preparation of benzylidene intermediates useful in the preparation of 1,4-dihydropyridine compounds and derivatives thereof useful as medicines such as for example felodipine. This is accomplished by the condensation of an aldehyde and an acetoacetate in the presence of a novel catalyst system that includes a pyridyl carboxylic acid and a secondary amine. It has been found that through the use of the present invention the purity and yield of the desired isomer of the benzylidene intermediate can be maximized, thus avoiding the requirement of additional purification steps. The use of these intermediates can then be further reacted to form the required dihydropyridines, again having a very high purity and yield compared with the prior art.
摘要翻译：公开了一种改进的催化剂，其用于制备可用作制备1,4-二氢吡啶化合物及其衍生物的亚苄基中间体的方法，其用作药物，例如非洛地平。这可以通过醛和乙酰乙酸酯在包含吡啶羧酸和仲胺的新型催化剂体系的存在下缩合来实现。已经发现，通过使用本发明，可以使亚苄基中间体的所需异构体的纯度和产率最大化，从而避免了额外的纯化步骤的需要。然后可以将这些中间体的使用进一步反应以形成所需的二氢吡啶，与现有技术相比，再次具有非常高的纯度和产率。

8. 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。

9. 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。

10. 发明申请

US20060199855A1 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：US20060199855A1
公开(公告)日：2006-09-07
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 Horne
发明人： K.S. Keshava Murthy , Yajun Zhao , Daqing Che , Bhaskar Reddy Guntoori , Sammy Chris Duncan , Stephen Horne
IPC分类号： A61K31/401 , C07D207/34
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,
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NR 1 R 2 R 3 R 3的碱，其中R 1，R 2， R 3和R 3独立地选自H，取代或未取代的C 1 -C 7烷基，C 6至C 9芳基，C 8至C 10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，必要时进行纯化，

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