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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

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。

5. 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。

6. 发明申请

US20060189670A1 Process for the preparation of anastrozole and intermediates thereof 审中-公开
标题翻译：制备阿那曲唑及其中间体的方法
公开(公告)号：US20060189670A1
公开(公告)日：2006-08-24
申请号：US11359248
申请日：2006-02-22
申请人： Anil Khile , Narendra Joshi , Shekhar Bhirud
发明人： Anil Khile , Narendra Joshi , Shekhar Bhirud
IPC分类号： C07D249/08 , A61K31/4196
CPC分类号： C07D249/08 , Y02P20/55
摘要： A process for the preparation of anastrozole is provided, the process comprising: (a) reacting 3,5-bis(1-cyano-1-methylethyl)benzyl halide with a 4-Z-1,2,4-triazole compound of the formula wherein Z is a protecting group to produce 2,2′-[5-(4-Z-1,2,4-triazolium-1-ylmethyl)-1,3-phenylene]di(2-methylpropionitrile) halide; and (b) deprotecting the 2,2′-[5-(4-Z-1,2,4-triazolium-1-ylmethyl)-1,3-phenylene]di(2-methylpropionitrile)halide to produce anastrozole. Also provided is anastrozole substantially free of its isomers.
摘要翻译：提供了一种制备阿那曲唑的方法，该方法包括：（a）使3,5-双（1-氰基-1-甲基乙基）苄基卤与4-Z-1,2,4-三唑化合物其中Z是产生2,2' - [5-（4-Z-1,2,4-三唑鎓-1-基甲基）-1,3-亚苯基]二（2-甲基丙腈）卤化物的保护基; 和（b）使2,2' - [5-（4-Z-1,2,4-三唑鎓-1-基甲基）-1,3-亚苯基]二（2-甲基丙腈）卤化物脱保护而制备阿那曲唑。还提供了基本上不含其异构体的阿那曲唑。

7. 发明申请

US20050124639A1 Process for the preparation of pyrimidine derivatives 失效
标题翻译：制备嘧啶衍生物的方法
公开(公告)号：US20050124639A1
公开(公告)日：2005-06-09
申请号：US11004755
申请日：2004-12-03
申请人： Narendra Joshi , Shekhar Bhirud , Batchu Chandrasekhar , K. Rao , Subhash Damle
发明人： Narendra Joshi , Shekhar Bhirud , Batchu Chandrasekhar , K. Rao , Subhash Damle
IPC分类号： C07D239/42 , A61K31/513 , A61K31/505 , C07D239/34
CPC分类号： C07D239/42 , Y02P20/55
摘要： An improved process for the preparation of pyrimidine derivatives is provided comprising reacting a Wittig reagent of the general formula wherein R is an alkyl of from 1 to 10 carbon atoms, aryl or arylalkyl, R1 is a substituted or unsubstituted hydrocarbon group, R2 and R3 are the same or different and are hydrogen or a substituted or unsubstituted hydrocarbon group; Z is sulfur, oxygen, sulfonyl, or imino which may be substituted by formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, amino substituted by sulfonyl or alkylsulfonyl, and sulfonyl substituted by alkyl, amino or alkylamino and X is a halogen; with an aldehyde of the general formula wherein R4 is hydrogen, a lower alkyl or a cation capable of forming a non-toxic pharmaceutically acceptable salt and each R5 are the same or different and are hydrogen or a hydrolyzable protecting group, or each R5, together with the oxygen atom to which each is bonded, form a hydrolyzable cyclic protecting group, or each R5 is bonded to the same substituent which is bonded to each oxygen atom to form a hydrolyzable protecting group; in the presence of a base.
摘要翻译：提供了制备嘧啶衍生物的改进方法，包括使通式为Wittig试剂反应其中R为1至10个碳原子的烷基，芳基或芳基烷基，R 1是被取代或未取代的烃基，R 2和R 3相同或不同，为氢或取代或未取代的烃基; Z可以被甲酰基，乙酰基，丙酰基，丁酰基，异丁酰基，戊酰基，异戊酰基，被磺酰基或烷基磺酰基取代的氨基，和被烷基，氨基或烷基氨基取代的磺酰基取代的硫，氧，磺酰基或亚氨基，X是卤素 ; 与其中R 4为氢的通式的醛，能够形成无毒的药学上可接受的盐的低级烷基或阳离子和每个R 5相同或不同的是氢或可水解保护基团，或每个R 5与每个键合的氧原子一起形成可水解的环保护基团，或每个R 5， SUP>键合到与每个氧原子键合的相同取代基以形成可水解保护基团; 在一个基地的存在。

8. 发明申请

US20150018578A1 PROCESS FOR PREPARATION OF FINGOLIMOD 有权
标题翻译：制备FINGOLIMOD的方法
公开(公告)号：US20150018578A1
公开(公告)日：2015-01-15
申请号：US14373214
申请日：2013-01-17
申请人： Milind Gharpure , Krishna Narawade , Prem Chand , Shekhar Bhirud
发明人： Milind Gharpure , Krishna Narawade , Prem Chand , Shekhar Bhirud
IPC分类号： C07C209/78 , C07C215/10 , C07C45/30 , C07C209/16 , C07C29/14
CPC分类号： C07C209/78 , C07C17/16 , C07C29/00 , C07C29/14 , C07C45/30 , C07C45/64 , C07C67/293 , C07C209/16 , C07C213/08 , C07C215/10 , C07C215/28 , C07C231/12 , C07C303/28 , C07C309/66 , C07C233/47 , C07C22/04 , C07C69/157 , C07C49/82 , C07C33/20
摘要： The present invention provides a process for preparation of fingolimod, a compound of Formula I or a pharmaceutically acceptable salt thereof, free of regioisomeric impurity compound of Formula IA
摘要翻译：本发明提供了一种制备芬戈莫德，式I化合物或其药学上可接受的盐的方法，其不含式IA的区域异构体杂质化合物

9. 发明申请

US20060106233A1 Process for the preparation of disubstituted acetylenes bearing heteroaromatic and heterobicyclic groups 审中-公开
公开(公告)号：US20060106233A1
公开(公告)日：2006-05-18
申请号：US11155847
申请日：2005-06-17
申请人： Bobba Kumar , Shekhar Bhirud , Batchu Chandrasekhar , Changdev Raut
发明人： Bobba Kumar , Shekhar Bhirud , Batchu Chandrasekhar , Changdev Raut
IPC分类号： C07D335/06 , C07D215/60
CPC分类号： C07D335/06
摘要： A process for the preparation of a disubstituted acetylene bearing heteroaromatic and heterobicyclic groups of formula I is provided wherein X is S, O, or NR1 wherein R1 is hydrogen or a C1-C6 straight or branched alkyl group; R is hydrogen or a C1-C6 straight or branched alkyl group; A is a substituted or unsubstituted pyridinyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl group; n is 0-4; and B is H, —COOH, —CH2OH, —CHO or a C1-C6 alkyl acetal derivative, —COR2 or a C1-C6 alkyl ketal derivative where R2 is —(CH2)mCH3 where m is 0-4 or COOR3 wherein R3 is a straight or branched C1-C30 alkyl group, a substituted or unsubstituted C6-C30 aromatic group, a substituted or unsubstituted C3-C30 cycloalkyl, a substituted or unsubstituted C3-C30 cycloalkylalkyl, a substituted or unsubstituted C3-C30 cycloalkenyl, a substituted or unsubstituted C5-C30 aryl, a substituted or unsubstituted C5-C30 arylalkyl, a substituted or unsubstituted C5-C30 heteroaryl, a substituted or unsubstituted C3-C30 heterocyclic ring, a substituted or unsubstituted C4-C30 heterocyclylalkyl, a substituted or unsubstituted C6-C30 heteroarylalkyl, the process comprising a Sonogashira coupling reaction between a compound of formula II wherein X and R have the aforestated meanings, with a compound of formula III X′-A-(CH2)n—B (III) wherein X′ is a halogen and A, n and B have the aforestated meanings, in the presence of a base and a transition metal catalyst and in a polar aprotic solvent.

10. 发明申请

US20050240029A1 Process for the preparation of 4,4-dimethyl-6-ethynylthiochroman 失效
标题翻译：制备4,4-二甲基-6-乙炔基二氢苯并噻喃的方法
公开(公告)号：US20050240029A1
公开(公告)日：2005-10-27
申请号：US11158856
申请日：2005-06-22
申请人： Bobba Venkata Kumar , Vishvas Patil , Changdev Raut , Shekhar Bhirud , Batchu Chandrasekhar
发明人： Bobba Venkata Kumar , Vishvas Patil , Changdev Raut , Shekhar Bhirud , Batchu Chandrasekhar
IPC分类号： C07D335/06 , C07D335/04 , A61K31/382
CPC分类号： C07D335/06
摘要： An improved process for the preparation of key intermediates for tazarotene, 4,4-dimethyl-6-ethynylthiochroman, is provided comprising (a) reacting 4,4-dimethyl-6-acetylthiochroman of the formula with an acid chloride and an amido-group containing compound of the general formula wherein R is hydrogen or a hydrocarbyl of from 1 to 15 carbon atoms and R1 and R2 can be the same or different and are hydrocarbyls of from 1 to 15 carbon atoms or R1 and R2 together with the nitrogen atom to which they are bonded are joined together to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms, or one of R1 and R2 together with the nitrogen atom to which it bonded are joined together with the carbonyl radical to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms to form a chloro vinyl carbonyl compound intermediate of the general formula wherein R has the aforestated meanings; and (b) reacting the β-chloro vinyl carbonyl compound intermediate with an alkali metal to provide the 4,4-dimethyl-6-ethynylthiochroman.
摘要翻译：提供了一种用于制备他扎罗汀4,4-二甲基-6-乙炔基二氢苯并噻喃的关键中间体的改进方法，其包括（a）使下式的4,4-二甲基-6-乙酰基二氢苯并二氢吡喃与酰氯和酰氨基其中R是氢或1至15个碳原子的烃基，R 1和R 2可以相同或不同，并且是烃基的通式 1至15个碳原子或R 1和R 2与它们所键合的氮原子一起连接在一起形成杂环基，任选地含有一个或多个另外的杂环原子或R 1和R 2中的一个与其键合的氮原子一起与羰基连接在一起形成杂环基，任选地含有一个或多个另外的杂环原子以形成通式的氯乙烯基羰基化合物中间体，其中R具有af ;意和（b）使β-氯乙烯基羰基化合物中间体与碱金属反应，得到4,4-二甲基-6-乙炔基二氢苯并噻喃。

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