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1. 发明申请

WO2004089902A1 PROCESS TO PREPARE 1,4-DIHYDROPYRIDINE INTERMEDIATES AND DERIVATIVES THEREOF 审中-公开
标题翻译：制备1,4-二氢吡啶中间体及其衍生物的方法
公开(公告)号：WO2004089902A1
公开(公告)日：2004-10-21
申请号：PCT/CA2004/000545
申请日：2004-04-13
申请人： APOTEX PHARMACHEM INC. , CHE, Daqing , GUNTOORI, Bhaskar, Reddy , MURTHY, K., S., Keshava
发明人： CHE, Daqing , GUNTOORI, Bhaskar, Reddy , MURTHY, K., S., Keshava
IPC分类号： C07D211/02
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。

2. 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。

3. 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。

4. 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。

5. 发明申请

WO2011072383A1 PROCESSES FOR THE PURIFICATION OF LUBIPROSTONE 审中-公开
标题翻译： LUBIPROSTONE的纯化方法
公开(公告)号：WO2011072383A1
公开(公告)日：2011-06-23
申请号：PCT/CA2010/001987
申请日：2010-12-17
申请人： APOTEX PHARMACHEM INC. , WEERATUNGA, Gamini , KOTHAKONDA, Kiran Kumar , CECCARELLI, Alfredo, Paul , GUNTOORI, Bhaskar, Reddy , WANG, Fan
发明人： WEERATUNGA, Gamini , KOTHAKONDA, Kiran Kumar , CECCARELLI, Alfredo, Paul , GUNTOORI, Bhaskar, Reddy , WANG, Fan
IPC分类号： C07D311/94 , A61K31/558
CPC分类号： C07D311/94 , C07C405/00 , C07C2601/08
摘要： There is provided processes for purification of Lubiprostone by formation of amine salts. Also provided are compounds of the Lubiprostone amine salt. Also provided are compositions comprising Lubiprostone and amines.
摘要翻译：提供了通过形成胺盐来纯化卢比石的方法。还提供了卢比石盐胺的化合物。还提供了包含柳普鲁石和胺的组合物。

6. 发明申请

WO2010083597A1 METHODS OF MAKING LUBIPROSTONE AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备LUBIPROSTONE及其中间体的方法
公开(公告)号：WO2010083597A1
公开(公告)日：2010-07-29
申请号：PCT/CA2010/000083
申请日：2010-01-22
申请人： APOTEX PHARMACHEM INC. , KOTHAKONDA, Kiran, Kumar , WANG, Fan , GUNTOORI, Bhaskar, Reddy , NGUYEN, Minh, T.N. , CECCARELLI, Alfredo, Paul , ZHAO, Yajun , KOTIPALLI, Uma , DUNCAN, Sammy, Chris , MILNEE, Kaarina, K. , KELLS, Kevin, W. , MONTEMAYOR, Laura, Kaye
发明人： KOTHAKONDA, Kiran, Kumar , WANG, Fan , GUNTOORI, Bhaskar, Reddy , NGUYEN, Minh, T.N. , CECCARELLI, Alfredo, Paul , ZHAO, Yajun , KOTIPALLI, Uma , DUNCAN, Sammy, Chris , MILNEE, Kaarina, K. , KELLS, Kevin, W. , MONTEMAYOR, Laura, Kaye
IPC分类号： C07C69/734 , C07C59/66 , C07C69/738 , C07D307/935 , C07D311/94 , C07F7/18
CPC分类号： C07F7/1892 , C07C69/734 , C07C69/738 , C07C405/00 , C07C2601/08 , C07D307/935
摘要： There is provided processes for preparing Lubiprostone and intermediates thereof. Also provided are compounds, including intermediates for preparing Lubiprostone as well as compositions comprising Lubiprostone and other compounds, including intermediates for preparing Lubiprostone and other compounds. (I)
摘要翻译：提供了用于制备柳普罗石及其中间体的方法。还提供了化合物，包括用于制备兰比罗石的中间体以及包含卢比石和其它化合物的组合物，包括用于制备兰普罗石和其他化合物的中间体。（一世）

7. 发明申请

WO2006053441A1 IMPROVED PROCESS FOR THE PREPARATION OF (S)-ALPHA-ETYL-2-OXO-1-PYRROLIDINEACETAMIDE AND (R)-ALPHA-ETHYL-2-OXO-1-PYRROLIDINEACETAMIDE 审中-公开
标题翻译：（S）-ALPHA-ETYL-2-氧代-1-吡咯烷胺乙酰胺和（R）-ALPHA-乙基-2-氧代-1-吡咯烷胺乙酰胺的改进方法
公开(公告)号：WO2006053441A1
公开(公告)日：2006-05-26
申请号：PCT/CA2005/001758
申请日：2005-11-21
申请人： APOTEX PHARMACHEM INC. , LI, Yuan, Qiang , WANG, Zhi-Xian , GUNTOORI, Bhaskar, Reddy
发明人： LI, Yuan, Qiang , WANG, Zhi-Xian , GUNTOORI, Bhaskar, Reddy
IPC分类号： C07D207/277
CPC分类号： C07D207/27
摘要： A process provided for the preparation of the (S)- and (R)- alpha- ethyl-2-oxo-1- pyrrolidineacetamide of formula:(1) from (RS)-alpha-ethyl-2-oxo-l-pyrrolidineacetic acid of formula: (2) comprising: i) combining the (RS)-2 with a chiral base (resolving agent) in a resolution solvent and crystallizing from the said mixture the diastereomeric salt of (S)- or (R)-2 and chiral base; ii) regenerating (S)- or (R)-2 from the crystallized diastereomeric salt by treating with a suitable acid or acidic ion-exchange resin; iii) optionally regenerating (R)- or (S)-2 or their mixture (predominantly one enantiomer) from the crystallization mother liquor by treating with a suitable acid or acidic ion-exchange resin; iv) optionally epimerizing (RS)-2 by treating (R)- or (S)-2 or their mixture (predominantly one enantiomer) of step iii with an acid anhydride; V) optionally converting (RS)-2 of step iv into enantiomerically enriched (S)- or (R)-2 through steps i and ii; vi) formation of the mixed anhydride by reacting (R)- or (S)-2 with an alkyl or aryl sulfonyl halogen compound RSO2X in the presence of a suitable base; and vii) reacting the mixed anhydride with ammonia; wherein R represents C 1 to C 15 alkyl or aryl groups such as methyl, ethyl, p-toluenyl, 2,4,6-trimethylbenzyl, 2,4,6-trichloribenzyl, and X represents a halogen atom such as F, Cl and Br atoms.
摘要翻译：（S） - （R）-α-乙基-2-氧代-1-吡咯烷乙酰胺由（RS）-α-乙基-2-氧代-1-吡咯烷乙酸制备的（S） - 和（R）-α-乙基-2-氧代-1-吡咯烷乙酰胺式（2）的酸包括：i）将（RS）-2与分解溶剂中的手性碱（拆分剂）组合并从所述混合物中结晶出（S） - 或（R）-2的非对映体盐和手性基; ii）通过用合适的酸或酸性离子交换树脂处理从结晶的非对映体盐再生（S） - 或（R）-2） iii）通过用合适的酸或酸性离子交换树脂处理任选地从结晶母液中再生（R） - 或（S）-2或它们的混合物（主要是一种对映异构体） iv）通过用酸酐处理（R） - 或（S）-2或它们的步骤iii的混合物（主要是一个对映异构体）任选差向异构化（RS）-2; V）任选地通过步骤i和ii将步骤iv的（RS）-2转化成对映异构体富集的（S） - 或（R） vi）通过使（R） - 或（S）-2与烷基或芳基磺酰基卤化合物RSO 2 X在合适的碱存在下反应形成混合酸酐; 和vii）使混合酸酐与氨反应; 其中R表示C 1至C 15烷基或芳基如甲基，乙基，对甲苯基，2,4,6-三甲基苄基，2,4,6-三氯苄基，X表示卤素原子如F，Cl和 Br原子。

8. 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。

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