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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

US20060079698A1 Process for the preparation of intermediates of trandolapril and use thereof for the preparation of trandolapril 审中-公开
标题翻译：制备群多普利中间体的方法及其用于制备群多普利的方法
公开(公告)号：US20060079698A1
公开(公告)日：2006-04-13
申请号：US11245871
申请日：2005-10-07
申请人： Narendra Joshi , Shekhar Bhirud , Buddhavarapu Ramam , Arjun Bodkhe
发明人： Narendra Joshi , Shekhar Bhirud , Buddhavarapu Ramam , Arjun Bodkhe
IPC分类号： C07D209/42
CPC分类号： C07D209/42
摘要： A process for the preparation of an intermediate of trandolapril, (2S,3aR,7aS)-perhydroindole-2-carboxylic acid of Formula II is provided. Also provided are processes for preparing trandolapril.
摘要翻译：提供了制备式II的（2S，3aR，7aS） - 二氢吲哚-2-羧酸的中间体的方法。还提供了制备群多普利的方法。

4. 发明申请

US20070032661A1 Process for the preparation of intermediates of perindopril 审中-公开
标题翻译：培哚普利中间体的制备方法
公开(公告)号：US20070032661A1
公开(公告)日：2007-02-08
申请号：US11495102
申请日：2006-07-28
申请人： Narendra Joshi , Buddhavarapu Ramam , Arjun Bodkhe
发明人： Narendra Joshi , Buddhavarapu Ramam , Arjun Bodkhe
IPC分类号： C07D209/42
CPC分类号： C07D209/42
摘要： A process for the preparation of (2S, 3aS, 7aS)perhydroindole-2-carboxylic acid is provided comprising (a) esterifying a cis-perhydroindole-2-carboxylic acid with a first alcohol of the formula ROH and a suitable free acid to provide the acid salt (AS) of Formula V: (b) reacting the acid salt of Formula V with a first base to provide a compound of Formula VI: (c) treating the product of step (b) with an L-tartaric containing acid in a second alcohol of the formula ROH to precipitate a compound of Formula VII: (d) reacting the compound of Formula VII with a second base to provide a compound of Formula II (e) hydrolyzing the compound of Formula II to provide the (2S, 3aS, 7aS)perhydroindole-2-carboxylic acid.
摘要翻译：提供了制备（2S，3aS，7aS）全氢吲哚-2-羧酸的方法，其包括（a）使顺式 - 全氢吲哚-2-羧酸与式ROH的第一醇和合适的游离酸酯化，以提供式Ⅴ的酸性盐（AS）：（b）使式Ⅴ的酸式盐与第一碱反应以提供式Ⅵ化合物：（ⅲ）用含L-酒石酸的酸处理步骤（b）的产物在式ROH的第二个醇中，使式VII化合物沉淀：（d）使式VII化合物与第二碱反应，得到式II化合物（e）水解式II化合物，得到（2S ，3aS，7aS）全氢吲哚-2-羧酸。

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