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1. 发明授权

US5939564A Process of lactonization in the preparation of statins 失效
标题翻译：内酯化制备他汀类药物的过程
公开(公告)号：US5939564A
公开(公告)日：1999-08-17
申请号：US055572
申请日：1998-04-06
申请人： Yatendra Kumar , Rajesh Kumar Thaper , S. M. Dileep Kumar , Jag Mohan Khanna
发明人： Yatendra Kumar , Rajesh Kumar Thaper , S. M. Dileep Kumar , Jag Mohan Khanna
IPC分类号： C07D309/30
CPC分类号： C07D309/30
摘要： A novel process of lactonizaton in the preparation of statins (e.g., the HMG--CoA reductase inhibitors lovastatin and simvastatin) employs very mild reaction conditions. The improved process comprises dissolving the open ring hydroxy acid form of the statins in an organic solvent by heating at a temperature, which ranges from ambient to reflux of the solvent, under anhydrous conditions to produce a solution, treating the solution with a mild catalyst at a temperature from about ambient to 50.degree. C., and adding water to the solution to cause the statins in lactone form to crystalize from the reaction mixture. The mild catalyst used in the reaction is a salt of an organic base with an organic or inorganic acid, such as pyridine hydrobromide, pyridine hydrochloride, or pyridinium, p-toluene sulfonate. The organic solvent comprises a lower alkanol, a non-alcoholic polar solvent, or a mixture of the two.
摘要翻译：在制备他汀类药物（例如，HMG-CoA还原酶抑制剂洛伐他汀和辛伐他汀）中的新方法使用非常温和的反应条件。改进的方法包括通过在无水条件下从环境温度至溶剂回流的温度加热，将开环羟基酸形式的他汀类药物溶解在有机溶剂中，以产生溶液，用温和的催化剂处理溶液温度为约环境温度至50℃，并向溶液中加入水，使得内酯形式的他汀类从反应混合物中结晶。反应中使用的温和催化剂是有机碱与有机或无机酸的盐，例如吡啶氢溴酸盐，吡啶盐酸盐或吡啶鎓对甲苯磺酸盐。有机溶剂包括低级链烷醇，非醇极性溶剂或两者的混合物。

2. 发明授权

US5763646A Process for manufacturing simvastatin from lovastatin or mevinolinic acid 失效
标题翻译：从洛伐他汀或甲维林酸生产辛伐他汀的方法
公开(公告)号：US5763646A
公开(公告)日：1998-06-09
申请号：US816573
申请日：1997-03-13
申请人： Yatendra Kumar , Rajesh Kumar Thaper , Satyananda Misra , S. M. Dileep Kumar , Jag Mohan Khanna
发明人： Yatendra Kumar , Rajesh Kumar Thaper , Satyananda Misra , S. M. Dileep Kumar , Jag Mohan Khanna
IPC分类号： C07D309/30 , C07C67/02
CPC分类号： C07D309/30
摘要： A process for preparing simvastatin from lovastatin or mevinolinic acid in salt form comprises treating either starting material with cyclopropyl or butyl amine, the pyranone ring thereby being opened when lovastatin is the starting material, adding a methyl group to the 2-methylbutyrate side chain, and thereafter closing the open pyranone ring to produce simvastatin. The process is performed without protecting and deprotecting the two hydroxy groups of the open pyranone ring. In a preferred embodiment, the starting material is treated with cyclopropyl amine which produces simvastatin via the novel intermediate lovastatin cyclopropyl amide.
摘要翻译：以盐形式从洛伐他汀或甲维林酸制备辛伐他汀的方法包括用环丙基或丁胺处理起始原料，当洛伐他汀为原料时，吡喃酮环由此开放，向2-甲基丁酸酯侧链加入甲基，然后关闭开放的吡喃酮环以产生辛伐他汀。在不保护和去保护开放式吡喃酮环的两个羟基的情况下进行该方法。在优选的实施方案中，用环丙胺处理起始物质，其通过新的中间体洛伐他汀环丙基酰胺产生辛伐他汀。

3. 发明授权

US5756729A Process for the manufacture of 8-chloro-6 (2-fluorophenyl)-1 methyl-4H-imidazo �1,5a! �1,4! benzodiazepine (midazolam) 失效
标题翻译：制备8-氯-6（2-氟苯基）-1甲基-4H-咪唑并[1,5a] [1,4]苯并二氮杂卓（咪达唑仑）的方法
公开(公告)号：US5756729A
公开(公告)日：1998-05-26
申请号：US728808
申请日：1996-10-09
申请人： Jag Mohan Khanna , Naresh Kumar , Chandrahas Khanduri , Mukesh Kumar Sharma , Pankaj Sharma , Swargam Sathyanarayan , Girij Pal Singh
发明人： Jag Mohan Khanna , Naresh Kumar , Chandrahas Khanduri , Mukesh Kumar Sharma , Pankaj Sharma , Swargam Sathyanarayan , Girij Pal Singh
IPC分类号： C07D339/06 , C07D339/08 , C07D409/10 , C07D487/04 , C07D243/10 , A61K31/55 , C07D243/14
CPC分类号： C07D409/10 , C07D339/06 , C07D339/08 , C07D487/04
摘要： A multistep process for producing 8-chloro-6-(2-fluorophenyl)-1-methyl-4-H-imidazo�1,5a!�1,4! benzodiazepine (midazolam) comprises treating a compound of Formula II with a lower alkyl dithiol to produce a compound of Formula III, wherein n=2 or 3, converting the compound of Formula III to a compound of Formula VII, and then treating the compound of Formula VII with a deprotecting agent, thereby producing midazolam. Novel intermediate compounds are also disclosed.
摘要翻译：用于制备8-氯-6-（2-氟苯基）-1-甲基-4H-咪唑并[1,5a] [1,4]苯并二氮杂（咪达唑仑）的多步方法包括用较低的制备式III化合物，其中n = 2或3，将式III化合物转化为式VII化合物，然后用脱保护剂处理式VII化合物，从而产生咪达唑仑。还公开了新的中间体化合物。

4. 发明授权

US07678927B2 Process for lactonization in the preparation of statins 失效
标题翻译：内酯化制备他汀类药物的方法
公开(公告)号：US07678927B2
公开(公告)日：2010-03-16
申请号：US11574872
申请日：2004-09-08
申请人： Govind Singh , Paramvir Bhadwal , Sanjay Jaiswal , Dinesh R. Panchasara , Rajesh Kumar Thaper , Sushil Kumar Dubey , Jag Mohan Khanna
发明人： Govind Singh , Paramvir Bhadwal , Sanjay Jaiswal , Dinesh R. Panchasara , Rajesh Kumar Thaper , Sushil Kumar Dubey , Jag Mohan Khanna
IPC分类号： C07D309/30
CPC分类号： C07D309/30
摘要： The present invention relates to an improved and industrial friendly process for lactonization to produce compound of the Formula [I], from compound of the Formula [II] in presence of an inorganic compound as a suitable lactonizing agent, preferably alkali metal hydrogen sulfate, and crystallizing the obtained lactone product in a solvent; or treating compound of the Formula [II] in the presence of an inorganic compound preferably alkali metal hydrogen sulfate using phase transfer catalyst in heterogeneous phase followed by crystallizing the obtained lactone product in a solvent.
摘要翻译：本发明涉及在无机化合物作为合适的内酯化剂，优选碱金属硫酸氢盐的存在下，通过式[II]的化合物制备式[I]的化合物的内酯化的改进和工业友好的方法，以及将所得内酯产物在溶剂中结晶; 或在无机化合物（优选碱金属硫酸氢盐）存在下处理式[II]化合物，使用非均相相转移催化剂，然后将所得内酯产物在溶剂中结晶。

5. 发明授权

US08124783B2 Process for producing 1-benzyl-4-[5,6-dimethoxy-1-indanon-2-yl)methyl] piperidine or its salt thereof via novel intermediate 有权
标题翻译：通过新中间体制备1-苄基-4- [5,6-二甲氧基-1-茚满酮-2-基）甲基]哌啶或其盐的方法
公开(公告)号：US08124783B2
公开(公告)日：2012-02-28
申请号：US11813093
申请日：2004-12-30
申请人： Shailendra Kumar Dubey , Amit Kumar Sharma , Beena S. Rani , Soumendu Paul , Rajesh Kumar Thaper , Dubey Sushil Kumar , Jag Mohan Khanna
发明人： Shailendra Kumar Dubey , Amit Kumar Sharma , Beena S. Rani , Soumendu Paul , Rajesh Kumar Thaper , Dubey Sushil Kumar , Jag Mohan Khanna
IPC分类号： C07D211/82 , C07D211/70
CPC分类号： C07D213/89 , C07D211/22
摘要： Disclosed herein the process for producing 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2yl)methyl]piperidine or its salt thereof employing novel intermediates.
摘要翻译：本文公开了使用新型中间体生产1-苄基-4 - [（5,6-二甲氧基-1-茚满酮-2-基）甲基]哌啶或其盐的方法。

6. 发明授权

US06235896B1 Process for the preparation of cefuroxime 失效
标题翻译：头孢呋辛的制备方法
公开(公告)号：US06235896B1
公开(公告)日：2001-05-22
申请号：US09264977
申请日：1999-03-09
申请人： Vijay Kumar Handa , Ramesh Dandala , Jag Mohan Khanna
发明人： Vijay Kumar Handa , Ramesh Dandala , Jag Mohan Khanna
IPC分类号： C07D50134
CPC分类号： C07D501/00
摘要： There is described a process for the preparation of cefuroxime from predominantly S-cefuroxime axetil, R, S mixture of cefuroxime axetil or R-cefuroxime axetil not meeting the purity criteria. This comprises treating cefuroxime axetil with alkoxides in the presence of a suitable solvent or solvent mixture and isolating cefuroxime from the reaction mixture.
摘要翻译：描述了头孢呋辛主要由头孢呋辛酯，头孢呋辛酯或R-头孢呋辛酯的R，S混合物制成的方法，该方法不符合纯度标准。这包括在合适的溶剂或溶剂混合物存在下用醇盐处理头孢呋辛酯，并从反应混合物中分离头孢呋辛。

7. 发明授权

US5792874A Process for the manufacture of 8-chloro-6-(2-flourophenyl)-1-methyl-4H-imidazo�1,5A!�1,4!benzodiazepine (midazolam) 失效
标题翻译：制备8-氯-6-（2-氟苯基）-1-甲基-4H-咪唑并[1,5A] [1,4]苯并二氮杂（咪达唑仑）的方法
公开(公告)号：US5792874A
公开(公告)日：1998-08-11
申请号：US918393
申请日：1997-08-26
申请人： Jag Mohan Khanna , Naresh Kumar , Chandrahas Khanduri , Mukesh Kumar Sharma , Pankaj Sharma , Swargam Sathyanarayan , Girij Pal Singh
发明人： Jag Mohan Khanna , Naresh Kumar , Chandrahas Khanduri , Mukesh Kumar Sharma , Pankaj Sharma , Swargam Sathyanarayan , Girij Pal Singh
IPC分类号： A61K31/55 , A61P21/02 , A61P23/00 , A61P25/20 , C07D339/06 , C07D339/08 , C07D409/10 , C07D487/04 , C07D204/04
CPC分类号： C07D339/08 , C07D339/06 , C07D409/10 , C07D487/04
摘要： A multistep process for producing 8-chloro-6-(2-fluorophenyl)-1-methyl-4-H-imidazo�1,5a!�1,4!benzodiazepine (midazolam) comprises treating a compound of Formula II with a lower alkyl dithiol to produce a compound of Formula III, wherein n=2 or 3, converting the compound of Formula III to a compound of Formula VII, and then treating the compound of Formula VII with a deprotecting agent, thereby producing midazolam. Novel intermediate compounds are also disclosed.
摘要翻译：用于制备8-氯-6-（2-氟苯基）-1-甲基-4H-咪唑并[1,5a] [1,4]苯并二氮杂（咪达唑仑）的多步方法包括用较低的制备式III化合物，其中n = 2或3，将式III化合物转化为式VII化合物，然后用脱保护剂处理式VII化合物，从而产生咪达唑仑。还公开了新的中间体化合物。

8. 发明授权

US5917058A Process of lactonization in the preparation of statins 失效
标题翻译：内酯化制备他汀类药物的过程
公开(公告)号：US5917058A
公开(公告)日：1999-06-29
申请号：US64285
申请日：1998-04-22
申请人： Yatendra Kumar , Rajesh Kumar Thaper , S. M. Dileep Kumar , Jag Mohan Khanna
发明人： Yatendra Kumar , Rajesh Kumar Thaper , S. M. Dileep Kumar , Jag Mohan Khanna
IPC分类号： C07D309/30
CPC分类号： C07D309/30
摘要： An improved process of lactonization in the preparation of statins (e.g., the HMG--CoA reductase inhibitors lovastatin and simvastatin) employs very mild reaction conditions. The improved process comprises treating the open ring hydroxy acid form of the statins with an excess of acetic acid and in the absence of a strong acid catalyst under mild heating conditions (e.g., ambient to 55.degree. C.), and adding an anti-solvent to the reaction mixture, thereby causing the statins in lactone form to crystalize from the reaction mixture. The acetic acid serves as both a solvent and a catalyst for the lactonization reaction.
摘要翻译：在制备他汀类药物（例如，HMG-CoA还原酶抑制剂洛伐他汀和辛伐他汀）中改进的内酯化方法采用非常温和的反应条件。改进的方法包括用温和的加热条件（例如，环境温度至55℃）用过量的乙酸处理开环羟基酸形式的他汀类和不存在强酸催化剂的情况下，加入抗溶剂反应混合物，从而使内酯形式的他汀类从反应混合物中结晶。乙酸既用作内酯化反应的溶剂和催化剂。

9. 发明申请

US20090137812A1 PROCESS FOR PRODUCING 1-BENZYL-4-[5,6-DIMETHOXY-1-INDANON-2-YL)METHYL]PIPERIDINE OR ITS SALT THEREOF VIA NOVEL INTERMEDIATE 有权
标题翻译：通过新型中间体生产1-苄基-4- [5,6-二甲氧基-1-吲哚-2-基]甲基]哌啶或其盐的方法
公开(公告)号：US20090137812A1
公开(公告)日：2009-05-28
申请号：US11813093
申请日：2004-12-30
申请人： Shailendra Kumar Dubey , Amit Kumar Sharma , Beena S. Rani , Soumendu Paul , Rajesh Kumar Thaper , Dubey Sushil Kumar , Jag Mohan Khanna
发明人： Shailendra Kumar Dubey , Amit Kumar Sharma , Beena S. Rani , Soumendu Paul , Rajesh Kumar Thaper , Dubey Sushil Kumar , Jag Mohan Khanna
IPC分类号： C07D211/06
CPC分类号： C07D213/89 , C07D211/22
摘要： Disclosed herein the process for producing 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2yl)methyl]piperidine or its salt thereof employing novel intermediates.
摘要翻译：本文公开了使用新型中间体生产1-苄基-4 - [（5,6-二甲氧基-1-茚满酮-2-基）甲基]哌啶或其盐的方法。

10. 发明授权

US5869649A Process for producing cephalosporin antibiotics 失效
标题翻译：生产头孢菌素抗生素的方法
公开(公告)号：US5869649A
公开(公告)日：1999-02-09
申请号：US641954
申请日：1996-05-01
申请人： Jag Mohan Khanna , Vijay Kumar Handa , Ramesh Dandala , Ram Chander Aryan
发明人： Jag Mohan Khanna , Vijay Kumar Handa , Ramesh Dandala , Ram Chander Aryan
IPC分类号： C07D501/00 , C07D501/06
CPC分类号： C07D501/00
摘要： A process for preparing certain cephalosporin antibiotics, namely, cefotaxime, cefetemet, and ceftriaxone sodium comprising acylation of 7-amino-3-cephem-4-carboxylic acid derivatives with 2-mercapto-5-methyl-1,3,4-thiadiazolyl-(Z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetate having the formula: ##STR1##
摘要翻译：包括头孢噻肟，头孢曲松和头孢曲松钠的某些头孢菌素类抗生素的制备方法，包括用2-巯基-5-甲基-1,3,4-噻二唑基-4-羧酸衍生物酰化7-氨基-3-头孢烯-4-羧酸衍生物，（Z）-2-（2-氨基噻唑-4-基）-2-甲氧基亚氨基乙酸酯，具有下式：

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