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1. 发明申请

WO2008151430A1 NOVEL PROCESSES TO FORM-I OF OLANZAPINE 审中-公开
标题翻译： OLANZAPINE的新方法
公开(公告)号：WO2008151430A1
公开(公告)日：2008-12-18
申请号：PCT/CA2008/001124
申请日：2008-06-12
申请人： APOTEX PHARMACHEM INC. , CHE, Daqing , KOTHAKONDA, Kiran Kumar , MCPHAIL, Cameron , GUNTOORI, Bhaskar Reddy
发明人： CHE, Daqing , KOTHAKONDA, Kiran Kumar , MCPHAIL, Cameron , GUNTOORI, Bhaskar Reddy
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。

2. 发明申请

WO2007140608A1 A NOVEL PROCESS FOR THE PREPARATION OF ESOMEPRAZOLE AND SALTS THEREOF 审中-公开
标题翻译：用于制备异喹诺酮和其盐的新方法
公开(公告)号：WO2007140608A1
公开(公告)日：2007-12-13
申请号：PCT/CA2007/001005
申请日：2007-06-08
申请人： APOTEX PHARMACHEM INC. , WANG, Fan , MONTEMAYOR, Laura, Kaye , CHE, Daqing , HORNE, Stephen, E.
发明人： WANG, Fan , MONTEMAYOR, Laura, Kaye , CHE, Daqing , HORNE, Stephen, E.
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , Y02P20/55
摘要： A novel process for the preparation of omeprazole and its enantiomers, such as esomeprazole, as well as the preparation of related 2-(2-pyridinylmethyl-sulphinyl)-1H-benzimidazoles, including pantoprazole, lansoprazole and rabeprazole, as recemates or single enantiomers, and their alkali or alkaline salts has been developed. The novel process involves the surprising discovery that protection of the free-base benzimidazole sulfoxide (e.g. omeprazole or esomeprazole), by reaction with an alkyl, aryl or aralkyl chloroformate following oxidation of the corresponding sulfide, eliminates the need for its direct isolation. Subsequent removal of the protecting group with a solution of alkali or alkaline earth alkoxide in a C1-C4 alcohol directly provides the corresponding salt. By eliminating the need to handle the free-base benzimidazole sulfoxide, this advantageous procedure provides increased chemical yields over processes described in the art.
摘要翻译：一种用于制备奥美拉唑及其对映异构体的新方法，例如艾美拉唑，以及相关的2-（2-吡啶基甲基 - 亚磺酰基）-1H-苯并咪唑（包括泮托拉唑，兰索拉唑和雷贝拉唑）作为受体或单一对映异构体的制备，并开发了它们的碱金属盐或碱金属盐。该新方法涉及令人惊奇的发现：在相应的硫化物氧化后，通过与烷基，芳基或氯甲酸烷基酯反应来保护游离碱性苯并咪唑亚砜（例如奥美拉唑或埃索美拉唑）消除了对其直接分离的需要。随后用碱金属或碱土金属醇溶液在C1-C4醇中除去保护基团直接提供相应的盐。通过消除处理游离碱性苯并咪唑亚砜的需要，与本领域中描述的方法相比，该有利的方法提供了增加的化学产率。

3. 发明申请

WO2006089401A1 AN IMPROVED PROCESS FOR THE PREPARATION OF ATORVASTATIN AND INTERMEDIATES 审中-公开
标题翻译：改进ATORVASTATIN和中间体的制备方法
公开(公告)号：WO2006089401A1
公开(公告)日：2006-08-31
申请号：PCT/CA2006/000243
申请日：2006-02-21
申请人： APOTEX PHARMACHEM INC. , WANG, Fan , CHE, Daqing , GUNTOORI, Bhaskar Reddy , ZHAO, Yajun , KINSMAN, Aaron, C. , FAUGHT, Jody , CHOW, Alan
发明人： WANG, Fan , CHE, Daqing , GUNTOORI, Bhaskar Reddy , ZHAO, Yajun , KINSMAN, Aaron, C. , FAUGHT, Jody , CHOW, Alan
IPC分类号： C07D207/34
CPC分类号： C07D207/34
摘要： A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(l- methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-lH-pyrrol-l-yl]-5-hydroxy-3-oxo- 1-heptanoic acid, R-substituted ester 9 comprising: (a) reacting 5-(4-fluorophenyl)-2-(l -methylethyl)-l -(3-oxopropyl)-N,4- diphenyl-lH-pyrrole-3-carboxamide, 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-(l -methylethyl)-3-phenyl- 4-[(phenylamino)carbonyl]- 1 H-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 (R,S)-5-[2-(4-fluorophenyl)-5-(l -methylethyl)-3-phenyl-4- [(phenylamino)carbonyl]- 1 H-pyrrol- 1 -yl]-3 -hydroxy- 1 -pentanoic acid, 7; (c) treating the carboxylic 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 acid derived from (R)-7, forming (R)-5-[2-(4-fluorophenyl)-5-(l-methylethyl)-3-phenyl- 4-[(phenylamino)carbonyl]-lH-pyrrol-l-yl]-5-hydroxy-3-oxo-l- heptanoic acid, R-substituted ester 9, wherein the R substituent is a Cl to C6 alkyl, C6 to C9 aryl or C7 to Cl0 aralkyl. Subsequently, R-substituted ester 9 may be converted into atorvastatin calcium 6 based on procedures known in the art.
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5-（4-氟苯基）-2-（1-甲基乙基）-1-（3-氧代丙基）-N ，4-二苯基-1H-吡咯-3-甲酰胺，1，在螯合助溶剂中具有（S）-2-羟基-1,2-二苯基乙基乙酸酯取代基的烯醇化物形式; （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-基吡啶-3-基] -3-羟基-1-戊酸，（S）-2-羟基-1,2-二苯基乙酯（2a和2b），使用碱，优选碱金属碱，优选在溶剂中形成（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] 羟基-1-戊酸，7; （c）用手性碱处理羧酸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的游离酸的烷基化，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，其中R取代基是C1至C6 烷基，C 6至C 9芳基或C 7至C 10芳烷基。随后，基于本领域已知的方法，R取代的酯9可以转化成阿托伐他汀钙6。

4. 发明申请

WO2005122671A3 AN IMPROVED PROCESS FOR THE PREPARATION OF OXCARBAZEPINE AND RELATED INTERMEDIATES 审中-公开
标题翻译：改进奥沙利铂及相关中间体的制备方法
公开(公告)号：WO2005122671A3
公开(公告)日：2007-11-08
申请号：PCT/CA2005000932
申请日：2005-06-16
申请人： APOTEX PHARMACHEM INC , CHE DAQING , CORELLI-RENNIE NADIA , GUNTOORI BHASKAR REDDY , FAUGHT JODY
发明人： CHE DAQING , CORELLI-RENNIE NADIA , GUNTOORI BHASKAR REDDY , FAUGHT JODY
IPC分类号： C07D223/22 , A61K31/55 , C07D223/18 , 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与氯磺酰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。

5. 发明申请

WO2006092037A1 PROCESS FOR PRODUCING ATORVASTATIN HEMICALCIUM 审中-公开
标题翻译：生产ATORVASTATIN HEMICALCIUM的方法
公开(公告)号：WO2006092037A1
公开(公告)日：2006-09-08
申请号：PCT/CA2006/000190
申请日：2006-02-14
申请人： APOTEX PHARMACHEM INC. , MURTHY, K.S. Keshava , ZHAO, Yajun , CHE, Daqing , GUNTOORI, Bhaskar Reddy , DUNCAN, Sammy Chris , HORNE, Stephen, E.
发明人： MURTHY, K.S. Keshava , ZHAO, Yajun , CHE, Daqing , GUNTOORI, Bhaskar Reddy , DUNCAN, Sammy Chris , HORNE, Stephen, E.
IPC分类号： C07D207/34 , C07D405/06
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, (Formula I), wherein R is an ester protecting group to (Formula II), (b) extracting R(R*,R*)-3 into an organic solvent or mixture of solvents, (c) adding a base of formula NR 1 R 2 R 3 wherein R 1 , R 2 and R 3 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：提供了制备药物级阿托伐他汀半钙盐的方法，其包括：（a）脱酯化（式I），其中R是（式II）的酯保护基，（b）提取R（R *，R *） - 加入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）通过沉淀上述阿托伐他汀碱盐进行分离并在必要时进行纯化，（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。

6. 发明申请

WO2005087723A1 AN IMPROVED PREPARATION OF ATORVASTATIN 审中-公开
标题翻译：改进ATORVASTATIN的制备
公开(公告)号：WO2005087723A1
公开(公告)日：2005-09-22
申请号：PCT/CA2005/000368
申请日：2005-03-11
申请人： APOTEX PHARMACHEM INC. , GUNTOORI, Bhaskar, Reddy , CHE, Daqing , WANG, Fan , ZHAO, Yajun , MURTHY, Keshava, K.S. , HORNE, Stephen, E.
发明人： GUNTOORI, Bhaskar, Reddy , CHE, Daqing , WANG, Fan , ZHAO, Yajun , MURTHY, Keshava, K.S. , HORNE, Stephen, E.
IPC分类号： C07D207/416
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-l-heptanoic acid, tert-butylester comprising: (a) reduction of 5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4[(phenylamino)carbonyl]-1H-pyrrol-l-yl]-3-oxo-l-pentanoic acid, (R)-2-hydroxy1,2,2-triphenylethyl ester; (b) hydrolysis of (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-l-pentanoic acid, (R)-2hydroxy-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)-3phenyl-4-[(phenylamino)carbonyl]-1 H-pyrrol-1-yl]-5-hydroxy-3-oxo- l -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] -5- 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）-2-羟基-3-氧代-1-庚酸 ] -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-基吡啶-3-基] -5-羟基-3-氧代-1-庚酸叔丁酯。

7. 发明申请

WO2003078407A1 A NEW AND EFFICIENT PROCESS FOR THE PREPARATION OF LAMOTRIGINE AND RELATED 3,5-DIAMINO-6-SUBSTITUTED-1,2,4-TRIAZINES 审中-公开
标题翻译：制备拉莫曲宁及其相关的3,5-二氨基-6-取代的1,2,4-三唑的新的和有效的方法
公开(公告)号：WO2003078407A1
公开(公告)日：2003-09-25
申请号：PCT/CA2002/001926
申请日：2002-12-18
申请人： BRANTFORD CHEMICALS INC. , GUNTOORI, Bhaskar, Reddy , CHE, Daqing , MURTHY, Keshava, K., S.
发明人： GUNTOORI, Bhaskar, Reddy , CHE, Daqing , MURTHY, Keshava, K., S.
IPC分类号： C07D253/06
CPC分类号： C07D253/075
摘要： A process for the manufacture of 3,5-diamino-kgg6-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-kgg6-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（IV）的3,5-二氨基-6-取代-1,2,4-三嗪化合物 I）或其水合形式。

8. 发明申请

WO2009000067A1 IMPROVED PROCESSES FOR THE SYNTHESIS OF OLANZAPINE 审中-公开
标题翻译：改进奥兰治泊合成方法
公开(公告)号：WO2009000067A1
公开(公告)日：2008-12-31
申请号：PCT/CA2008/001123
申请日：2008-06-12
申请人： APOTEX PHARMACHEM INC. , KOTHAKONDA, Kiran Kumar , CHE, Daqing , GUNTOORI, Bhaskar Reddy
发明人： KOTHAKONDA, Kiran Kumar , CHE, Daqing , GUNTOORI, Bhaskar Reddy
IPC分类号： C07D495/04
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-10 H -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[2,3b] [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。

9. 发明申请

WO2005122671A2 AN IMPROVED PROCESS FOR THE PREPARATION OF OXCARBAZEPINE AND RELATED INTERMEDIATES 审中-公开
标题翻译：改进奥沙利铂及相关中间体的制备方法
公开(公告)号：WO2005122671A2
公开(公告)日：2005-12-29
申请号：PCT/CA2005/000932
申请日：2005-06-16
申请人： APOTEX PHARMACHEM INC. , CHE, Daqing , CORELLI-RENNIE, Nadia , GUNTOORI, Bhaskar, Reddy , FAUGHT, Jody
发明人： CHE, Daqing , CORELLI-RENNIE, Nadia , GUNTOORI, Bhaskar, Reddy , FAUGHT, Jody
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。

10. 发明申请

WO2005073187A1 IMPROVED PROCESS FOR THE PREPARATION OF AMORPHOUS ATORVASTATIN CALCIUM 审中-公开
标题翻译：用于制备不定形ATORVASTATIN钙的改进方法
公开(公告)号：WO2005073187A1
公开(公告)日：2005-08-11
申请号：PCT/CA2004/002161
申请日：2004-12-20
申请人： APOTEX PHARMACHEM INC. , CHE, Daqing , KINSMAN, Aaron, C. , GUNTOORI, Bhaskar, Reddy , MURTHY, Keshava, K.S. , ZHAO, Yajun , HORNE, Stephen, E.
发明人： CHE, Daqing , KINSMAN, Aaron, C. , GUNTOORI, Bhaskar, Reddy , MURTHY, Keshava, K.S. , ZHAO, Yajun , HORNE, Stephen, E.
IPC分类号： C07D207/34
CPC分类号： C07D207/34
摘要： A process for the preparation of amorphous atorvastatin calcium which comprises: (a) hydrolysis of the atorvastatin lactone of formula II to form atorvastatin sodium salt solution; (b) addition of the atorvastatin sodium salt solution to an aqueous calcium chloride or calcium acetate solution; (c) isolation of the product; and (d) drying to afford amorphous atorvastatin calcium salt.
摘要翻译：一种制备无定形阿托伐他汀钙的方法，其包括：（a）水解式II的阿托伐他汀内酯以形成阿托伐他汀钠盐溶液; （b）将阿托伐他汀钠盐溶液加入到氯化钙水溶液或乙酸钙溶液中; （c）产品的隔离; 和（d）干燥以得到无定形的阿托伐他汀钙盐。

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