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1. 发明申请

US20060211867A1 Process for the preparation of perindopril 失效
标题翻译：培哚普利的制备方法
公开(公告)号：US20060211867A1
公开(公告)日：2006-09-21
申请号：US11386011
申请日：2006-03-21
申请人： Narendra Joshi , Shekhar Bhirud , Kodali Rao , Buddhavarapu Ramam , Vijay Soni
发明人： Narendra Joshi , Shekhar Bhirud , Kodali Rao , Buddhavarapu Ramam , Vijay Soni
IPC分类号： C07D209/42
CPC分类号： C07D209/42 , Y02P20/55
摘要： A process for preparing perindopril is provided comprising condensing an N-[(S)-1-carbethoxybutyl]-(S)-alanyl halide of formula II: wherein X is a halide with an (2S,3aS,7aS)-2-carboxyperhydroindole of formula III: wherein R is hydrogen or a protecting group.
摘要翻译：提供了一种制备培哚普利的方法，包括将式II的N - [（S）-1-乙酯基） - （S） - 丙氨酰卤进行缩合：其中X是卤素与（2S，3aS，7aS）-2-羧基全氢吲哚其中R是氢或保护基。

2. 发明申请

US20060211866A1 Process for the preparation of angiotensin receptor blockers and intermediates thereof 审中-公开
标题翻译：制备血管紧张素受体阻滞剂及其中间体的方法
公开(公告)号：US20060211866A1
公开(公告)日：2006-09-21
申请号：US11386010
申请日：2006-03-21
申请人： Narendra Joshi , Kodali Rao , Buddhavarapu Ramam , Shekhar Bhirud
发明人： Narendra Joshi , Kodali Rao , Buddhavarapu Ramam , Shekhar Bhirud
IPC分类号： C07D403/02 , C07D235/04
CPC分类号： C07D257/04 , C07D235/20 , C07D403/10
摘要： A process for the preparation of a biphenyl-containing compound of general formula I: wherein R1 is a C3-6 carbonyl containing compound; R2 is a substituted or unsubstituted, straight or branched C3-6 alkyl group, or R1 and R2 together with the nitrogen atom to which they are bonded are joined together to form a substituted heterocyclic group selected from the group consisting of substituted or unsubstituted imidazoles, substituted or unsubstituted benzimidazoles and substituted or unsubstituted 1,3-diazaspiro[4,4]non-1-en-4-one; and R3 is a carboxylic acid ester, cyano, a substituted or unsubstituted 1H-tetrazolyl group or a substituted or unsubstituted group which may be converted in vivo into a carboxy group is provided, the process comprising reacting a compound of general formula II: wherein R1 and R2 have the aforestated meanings with a compound of general formula III: wherein Z is a leaving group and R3 has the aforestated meaning in a biphasic solvent system in the presence of a phase transfer catalyst.
摘要翻译：一种制备含联苯的通式I化合物的方法：其中R 1是含3-6个碳原子的化合物; R 2是取代或未取代的直链或支链C 3-6 - 烷基，或R 1和R 2， SUP与它们所键合的氮原子一起连接在一起形成选自取代或未取代的咪唑，取代或未取代的苯并咪唑和取代或未取代的1,3-二氮杂螺[4,4] 非1-烯-4-酮; R 3是可以在体内转化为羧基的羧酸酯，氰基，取代或未取代的1H-四唑基或取代或未取代的基团，该方法包括使通式II的化合物：其中R 1和R 2具有通式III的化合物的前述含义：其中Z是离去基团，R 3 在相转移催化剂存在下，在双相溶剂体系中具有上述含义。

3. 发明申请

US20050250706A1 Processes for the preparation of alpha polymorph of perindopril erbumine 审中-公开
标题翻译：培哚普林卵白素α多晶型物的制备方法
公开(公告)号：US20050250706A1
公开(公告)日：2005-11-10
申请号：US11122731
申请日：2005-05-05
申请人： Narendra Joshi , Shekhar Bhirud , Kodali Rao
发明人： Narendra Joshi , Shekhar Bhirud , Kodali Rao
IPC分类号： A61K31/405 , A61K38/04 , C07D209/42 , C07K5/02
CPC分类号： C07K5/022 , C07D209/42
摘要： Processes for the preparation of an alpha polymorph of perindopril erbumine is provided comprising (a) forming a solution comprising perindopril erbumine in one or more ketones; (b) heating the solution to reflux; and (c) cooling the solution to a temperature sufficient to form the alpha polymorph of perindopril erbumine. The alpha polymorphs of perindopril erbumine obtained herein have a high purity level.
摘要翻译：提供了用于制备培哚普利埃尔本辛的α多晶型物的方法，包括（a）在一种或多种酮中形成包含培哚普利埃尔本辛的溶液; （b）将溶液加热回流; 和（c）将溶液冷却到足以形成培哚普利埃尔本的α多晶型物的温度。本文获得的培哚普利埃尔本的α多晶型物具有高纯度水平。

4. 发明申请

US20080071094A1 Process for the preparation of perindopril 审中-公开
标题翻译：培哚普利的制备方法
公开(公告)号：US20080071094A1
公开(公告)日：2008-03-20
申请号：US11903352
申请日：2007-09-21
申请人： Narendra JOSHI , Shekhar BHIRUD , Kodali RAO , Buddhavarapu RAMAM , Vijay SONI
发明人： Narendra JOSHI , Shekhar BHIRUD , Kodali RAO , Buddhavarapu RAMAM , Vijay SONI
IPC分类号： C07D209/42
CPC分类号： C07D209/42 , Y02P20/55
摘要： A process for preparing perindopril is provided comprising condensing an N-[(S)-1-carbethoxybutyl]-(S)-alanyl halide of formula II: wherein X is a halide with an (2S,3aS,7aS)-2-carboxyperhydroindole of formula III: wherein R is hydrogen or a protecting group.
摘要翻译：提供了一种制备培哚普利的方法，包括将式II的N - [（S）-1-乙酯基） - （S） - 丙氨酰卤进行缩合：其中X是卤素与（2S，3aS，7aS）-2-羧基全氢吲哚其中R是氢或保护基。

5. 发明申请

US20050239885A1 Processes for the preparation of simvastatin 审中-公开
标题翻译：辛伐他汀的制备方法
公开(公告)号：US20050239885A1
公开(公告)日：2005-10-27
申请号：US11112893
申请日：2005-04-22
申请人： Narendra Joshi , Shekhar Bhirud , Kodali Rao
发明人： Narendra Joshi , Shekhar Bhirud , Kodali Rao
IPC分类号： A61K31/225 , C07C67/02 , C07C211/63
CPC分类号： C07D309/30 , C07C211/63
摘要： Improved processes for the preparation of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) inhibitors, e.g., simvastatin, and their intermediates are provided. In one embodiment, a process for the preparation of a carboxylic acid amine salt of formula I is provided wherein R1 and R2 are as defined herein, the process comprising reacting lovastatin with an amine of formula III: in an aqueous medium to provide the carboxylic acid amine salt of formula I. The process further includes the steps of lithiating the carboxylic acid amine salt of formula I to form the corresponding 2,2-dimethylbutyrate intermediate of formula IIa lactonizing the 2,2-dimethylbutyrate intermediate (IIa) to provide simvastatin and pharmaceutically acceptable salts thereof. Also provided is an improved process for lactonization of the intermediates herein using peptide coupling reagents.
摘要翻译：提供了制备3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）抑制剂，例如辛伐他汀及其中间体的改进方法。在一个实施方案中，提供了制备式I的羧酸胺盐的方法，其中R 1和R 2如本文所定义，所述方法包括使洛伐他汀与式III的胺在水性介质中反应，得到式I的羧酸胺盐。该方法还包括将式I的羧酸胺盐锂化以形成相应的2,2-二甲基丁酸酯中间体 IIa将2,2-二甲基丁酸中间体（IIa）内酯化以提供辛伐他汀及其药学上可接受的盐。还提供了使用肽偶联试剂使本文中间体内酯化的改进方法。

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