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1. 发明授权

US06586593B1 Efficient process for the preparation of lamotrigine and related 3,5-diamino-6-substituted-1,2,4-triazines 失效
标题翻译：制备拉莫三嗪及其相关的3,5-二氨基-6-取代-1,2,4-三嗪的高效方法
公开(公告)号：US06586593B1
公开(公告)日：2003-07-01
申请号：US10046383
申请日：2002-01-16
申请人： Bhaskar Reddy Guntoori , Daqing Che , K. S. Keshava Murthy
发明人： Bhaskar Reddy Guntoori , Daqing Che , K. S. Keshava Murthy
IPC分类号： C07D253075
CPC分类号： C07D253/075
摘要： A process for the manufacture of 3,5-diamino-6-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-6-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I的3,5-二氨基-6-取代-1,2,4-三嗪化合物或水合形式。

2. 发明授权

US06858747B2 Process to prepare, 1,4-dihydropyridine intermediates and derivatives thereof 失效
标题翻译：制备方法，1,4-二氢吡啶中间体及其衍生物
公开(公告)号：US06858747B2
公开(公告)日：2005-02-22
申请号：US10819910
申请日：2004-04-08
申请人： Daqing Che , Bhaskar Reddy Guntoori , K. S. Keshava Murthy
发明人： Daqing Che , Bhaskar Reddy Guntoori , K. S. Keshava Murthy
IPC分类号： C07D211/90 , C07C69/79 , C07C205/00
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。

3. 发明授权

US07193090B2 Preparation of atorvastatin 失效
标题翻译：阿托伐他汀的制备
公开(公告)号：US07193090B2
公开(公告)日：2007-03-20
申请号：US10800741
申请日：2004-03-16
申请人： Bhaskar Reddy Guntoori , Daqing Che , Fan Wang , Yajun Zhao , K. S. Keshava Murthy , Stephen E. Horne
发明人： Bhaskar Reddy Guntoori , Daqing Che , Fan Wang , Yajun Zhao , K. S. Keshava Murthy , Stephen E. Horne
IPC分类号： C07D207/00
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-1-heptanoic acid, tert-butylester comprising: (a) reduction of 5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-oxo-1-pentanoic acid, (R)-2-hydroxy-1,2,2-triphenylethyl ester; (b) hydrolysis of (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (R)-2-hydroxy-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)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-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 - 羟基-3-氧代-1-庚酸叔丁酯包括：（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] -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-1,2,2-三苯基乙基酯，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。

4. 发明授权

US06596866B2 Process for the preparation of nefazodone hydrochloride 失效
标题翻译：盐酸奈法唑嗪的制备方法
公开(公告)号：US06596866B2
公开(公告)日：2003-07-22
申请号：US09953167
申请日：2001-09-17
申请人： K. S. Keshava Murthy , Bhaskar Reddy Guntoori , Daqing Che
发明人： K. S. Keshava Murthy , Bhaskar Reddy Guntoori , Daqing Che
IPC分类号： C07D40306
CPC分类号： C07D249/12
摘要： A process for the preparation of Nefazodone hydrochloride comprising direct conversion of semicarbazide dihydrochloride 3 into Nefazodone hydrochloride which process involves a reaction of triethyl orthopropionate in the presence of trimethylsilylchloride and hydrochloric acid.
摘要翻译：制备盐酸奈法唑酮的方法包括将氨基脲二盐酸盐3直接转化为盐酸奈法唑嗪，该方法涉及在三甲基甲硅烷基氯和盐酸存在下原甲酸三乙酯的反应。

5. 发明授权

US5919931A Process for the manufacture of intermediates suitable to make doxazosin, terazosin, prazosin, tiodazosin and related antihypertensive medicines 失效
标题翻译：制造适合制造多沙唑嗪，特拉唑嗪，哌唑嗪，替沙星和相关抗高血压药物的中间体的方法
公开(公告)号：US5919931A
公开(公告)日：1999-07-06
申请号：US627454
申请日：1996-04-04
申请人： K. S. Keshava Murthy , Gamini Weeratunga , Tianhao Zhou , Bhaskar Reddy Guntoori
发明人： K. S. Keshava Murthy , Gamini Weeratunga , Tianhao Zhou , Bhaskar Reddy Guntoori
IPC分类号： C07D307/24 , C07D307/68 , C07D319/20 , C07D405/06 , C07D413/06
CPC分类号： C07D319/20 , C07D307/24 , C07D307/68
摘要： A process is provided for the manufacture of: where R is: ##STR1## comprising reacting: ##STR2## wherein R.sub.1 may be selected from H, Methyl, Ethyl and suitable lower alkyl groups, C.sub.n H.sub.2n+1 (where n is from 3 to 5) or any other suitable group and thereafter if desired converting the resultant product to a salt thereof.
摘要翻译：提供了制备以下方法的方法：其中R为：其中R 1可以选自H，甲基，乙基和合适的低级烷基，C n H 2n + 1（其中n为3至5）或任何其它合适的然后如果需要，将所得产物转化成其盐。

6. 发明申请

US20080319189A1 Processes for the synthesis of olanzapine 失效
标题翻译：奥氮平合成方法
公开(公告)号：US20080319189A1
公开(公告)日：2008-12-25
申请号：US11976978
申请日：2007-10-30
申请人： Kiran Kumar Kothakonda , Daqing Che , Bhaskar Reddy Guntoori
发明人： Kiran Kumar Kothakonda , Daqing Che , Bhaskar Reddy Guntoori
IPC分类号： C07D243/10
CPC分类号： C07D495/04
摘要： There is provided a process for the preparation of olanzapine comprising: i) reacting 4-amino-2-methyl-10H-thieno-[2,3-b][1,5]benzodiazepine and N-methylpiperazine in a C1 to C4 alcoholic solvent or mixture thereof at suitable temperature and for a suitable time, ii) cooling the reaction mixture, and iii) isolating the precipitated olanzapine.
摘要翻译：提供了一种制备奥氮平的方法，其包括：i）使4-氨基-2-甲基-10H-噻吩并[2,3-b] [1,5]苯并二氮杂和N-甲基哌嗪在C1至C4醇中反应溶剂或其混合物在合适的温度和合适的时间，ii）冷却反应混合物，和iii）分离沉淀的奥氮平。

7. 发明申请

US20090131683A1 Process for the preparation of atorvastatin and intermediates 失效
标题翻译：制备阿托伐他汀和中间体的方法
公开(公告)号：US20090131683A1
公开(公告)日：2009-05-21
申请号：US12222690
申请日：2008-08-14
申请人： Fan Wang , Daqing Che , Bhaskar Reddy Guntoori , Yajun Zhao , Aaron C. Kinsman , Jody Faught , Alan Chow
发明人： Fan Wang , Daqing Che , Bhaskar Reddy Guntoori , Yajun Zhao , Aaron C. Kinsman , Jody Faught , Alan Chow
IPC分类号： C07D207/333
CPC分类号： C07D207/34
摘要： A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 comprising: (a) reacting the aldehyde 1 with the enolate form of (S)-2-hydroxy-1,2,2-triphenylethyl acetate substituent in a chelating co-solvent; (b) hydrolysis of (R,S)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (S)-2-hydroxy-1,2,2-triphenylethyl ester (2a and 2b) using a base, preferably an alkali metal base, preferably in a solvent to form the carboxylic acid 7; (c) treating the acid 7 with a chiral base to form a salt and purifying the salt to obtain enantiomerically enriched (R)-7 chiral base salt; (d) alkylation of the (R)-7 chiral base salt or the free base derived from (R)-7, forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 and atorvastatin calcium 6, wherein R is a C1 to C6 alkyl, C6 to C9 aryl or C7 to C10 aralkyl.
摘要翻译：提供了制备（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-羟基-3-氧代-1-庚酸，R-取代的酯9，其包含：（a）使醛1与烯醇化形式的（S）-2-羟基-1,2,2-三苯基乙基乙酸酯取代基在螯合助溶剂中; （b）（R，S）-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，（S）-2-羟基-1,2,2-三苯基乙酯（2a和2b），使用碱，优选碱金属碱，优选在溶剂中形成羧酸酸7; （c）用手性碱处理酸7以形成盐并纯化该盐以获得对映体富集的（R）-7手性碱盐; （d）（R）-7手性碱盐或衍生自（R）-7的游离碱的烷基化，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] -5-羟基-3-氧代-1-庚酸，R-取代的酯9和阿托伐他汀钙6，其中R是C1 C6烷基，C6〜C9芳基或C7〜C10芳烷基。

8. 发明授权

US07863442B2 Processes for the synthesis of olanzapine 失效
标题翻译：奥氮平合成方法
公开(公告)号：US07863442B2
公开(公告)日：2011-01-04
申请号：US11976978
申请日：2007-10-30
申请人： Kiran Kumar Kothakonda , Daqing Che , Bhaskar Reddy Guntoori
发明人： Kiran Kumar Kothakonda , Daqing Che , Bhaskar Reddy Guntoori
IPC分类号： C07D495/02
CPC分类号： C07D495/04
摘要： There is provided a process for the preparation of olanzapine comprising: i) reacting 4-amino-2-methyl-10H-thieno-[2,3-b][1,5]benzodiazepine and N-methylpiperazine in a C1 to C4 alcoholic solvent or mixture thereof at suitable temperature and for a suitable time, ii) cooling the reaction mixture, and iii) isolating the precipitated olanzapine.
摘要翻译：提供了一种制备奥氮平的方法，其包括：i）使4-氨基-2-甲基-10H-噻吩并[2,3-b] [1,5]苯并二氮杂和N-甲基哌嗪在C1至C4醇中反应溶剂或其混合物在合适的温度和合适的时间，ii）冷却反应混合物，和iii）分离沉淀的奥氮平。

9. 发明授权

US07112604B2 Process for the preparation of Atorvastatin and intermediates 失效
标题翻译：阿托伐他汀和中间体的制备方法
公开(公告)号：US07112604B2
公开(公告)日：2006-09-26
申请号：US11099624
申请日：2005-04-06
申请人： Fan Wang , Daqing Che , Bhaskar Reddy Guntoori , Yajun Zhao , Aaron C. Kinsman , Jody Faught , Alan Chow
发明人： Fan Wang , Daqing Che , Bhaskar Reddy Guntoori , Yajun Zhao , Aaron C. Kinsman , Jody Faught , Alan Chow
IPC分类号： A61K31/4025 , C07D207/327
CPC分类号： C07D207/34
摘要： A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 comprising: (a) reacting the aldehyde 1 with the enolate form of (S)-2-hydroxy-1,2,2-triphenylethyl acetate substituent in a chelating co-solvent; (b) hydrolysis of (R,S)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (S)-2-hydroxy-1,2,2-triphenylethyl ester (2a and 2b) using a base, preferably an alkali metal base, preferably in a solvent to form the carboxylic acid 7; (c) treating the acid 7 with a chiral base to form a salt and purifying the salt to obtain enantiomerically enriched (R)-7 chiral base salt; (d) alkylation of the (R)-7 chiral base salt or the free base derived from (R)-7, forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 and atorvastatin calcium 6, wherein R is a C1 to C6 alkyl, C6 to C9 aryl or C7 to C10 aralkyl.
摘要翻译：提供了制备（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-羟基-3-氧代-1-庚酸，R-取代的酯9，其包含：（a）使醛1与烯醇化形式的（S）-2-羟基-1,2,2-三苯基乙基乙酸酯取代基在螯合助溶剂中; （b）（R，S）-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，（S）-2-羟基-1,2,2-三苯基乙酯（2a和2b），使用碱，优选碱金属碱，优选在溶剂中形成羧酸酸7; （c）用手性碱处理酸7以形成盐并纯化该盐，得到对映体富集的（R）-7手性碱盐; （d）（R）-7手性碱盐或衍生自（R）-7的游离碱的烷基化，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] -5-羟基-3-氧代-1-庚酸，R-取代的酯9和阿托伐他汀钙6，其中R是C1 C6烷基，C6〜C9芳基或C7〜C10芳烷基。

10. 发明授权

US07429613B2 Process for the preparation of atorvastatin and intermediates 失效
标题翻译：制备阿托伐他汀和中间体的方法
公开(公告)号：US07429613B2
公开(公告)日：2008-09-30
申请号：US11487500
申请日：2006-07-17
申请人： Fan Wang , Daqing Che , Bhaskar Reddy Guntoori , Yajun Zhao , Aaron C. Kinsman , Jody Faught , Alan Chow
发明人： Fan Wang , Daqing Che , Bhaskar Reddy Guntoori , Yajun Zhao , Aaron C. Kinsman , Jody Faught , Alan Chow
IPC分类号： A61K31/4025 , C07D207/327
CPC分类号： C07D207/34
摘要： A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 comprising: (a) reacting the aldehyde 1 with the enolate form of (S)-2-hydroxy-1,2,2-triphenylethyl acetate substituent in a chelating co-solvent; (b) hydrolysis of (R,S)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (S)-2-hydroxy-1,2,2-triphenylethyl ester (2a and 2b) using a base, preferably an alkali metal base, preferably in a solvent to form the carboxylic acid 7; (c) treating the acid 7 with a chiral base to form a salt and purifying the salt to obtain enantiomerically enriched (R)-7 chiral base salt; (d) alkylation of the (R)-7 chiral base salt or the free base derived from (R)-7, forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 and atorvastatin calcium 6, wherein R is a C1 to C6 alkyl, C6 to C9 aryl or C7 to C10 aralkyl.
摘要翻译：提供了制备（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-羟基-3-氧代-1-庚酸，R-取代的酯9，其包含：（a）使醛1与烯醇化形式的（S）-2-羟基-1,2,2-三苯基乙基乙酸酯取代基在螯合助溶剂中; （b）（R，S）-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，（S）-2-羟基-1,2,2-三苯基乙酯（2a和2b），使用碱，优选碱金属碱，优选在溶剂中形成羧酸酸7; （c）用手性碱处理酸7以形成盐并纯化该盐以获得对映体富集的（R）-7手性碱盐; （d）（R）-7手性碱盐或衍生自（R）-7的游离碱的烷基化，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] -5-羟基-3-氧代-1-庚酸，R-取代的酯9和阿托伐他汀钙6，其中R是C1 C6烷基，C6〜C9芳基或C7〜C10芳烷基。

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