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1. 发明申请

WO2010038124A1 AN IMPROVED PROCESS FOR PREPARING PYRIMIDINE PROPENALDEHYDE 审中-公开
标题翻译：制备吡咯烷丙炔的改进方法
公开(公告)号：WO2010038124A1
公开(公告)日：2010-04-08
申请号：PCT/IB2009/006935
申请日：2009-09-23
申请人： AUROBINDO PHARMA LIMITED , MALLELA, Sambhu Prasad Sarma , NANDI, Sukumar , NANGI, Gangadhara Bhima Shankar , ANANTA, Rani , MEENAKSHISUNDERAM, Sivakumaran
发明人： MALLELA, Sambhu Prasad Sarma , NANDI, Sukumar , NANGI, Gangadhara Bhima Shankar , ANANTA, Rani , MEENAKSHISUNDERAM, Sivakumaran
IPC分类号： C07D239/42
CPC分类号： C07D239/42
摘要： The present invention relates to an improved process for preparing (2E)-3-[4-(4- fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidin-5-yl]- propenal of formula (I), which is an useful intermediate in the preparation of Rosuvastatin.
摘要翻译：本发明涉及制备式（2E）-3- [4-（4-氟苯基）-6-异丙基-2-（N-甲基-N-甲磺酰氨基）嘧啶-5-基] - 丙烯醛的改进方法，式（I），其是制备罗苏伐他汀的有用中间体。

2. 发明申请

WO2011021058A1 PROCESS FOR THE MANUFACTURE OF ROSUVASTATIN CALCIUM USING CRYSTALLINE ROSUVASTATIN ETHYL ESTER 审中-公开
标题翻译：用ROSUVASTATIN ETHYL ESTER制造ROSUVASTATIN钙的方法
公开(公告)号：WO2011021058A1
公开(公告)日：2011-02-24
申请号：PCT/IB2009/006580
申请日：2009-08-17
申请人： AUROBINDO PHARMA LIMITED , MALLELA, Sambhu, Prasad, Sarma , NANDI, Sukumar , NANGI, Gangadhara, Bhima, Shankar , DANDALA, Ramesh , MEENAKSHISUNDERAM, Sivakumaran
发明人： MALLELA, Sambhu, Prasad, Sarma , NANDI, Sukumar , NANGI, Gangadhara, Bhima, Shankar , DANDALA, Ramesh , MEENAKSHISUNDERAM, Sivakumaran
IPC分类号： C07D239/42
CPC分类号： C07D239/42
摘要： The present invention relates to an improved process to prepare Rosuvastatin calcium of Formula (I), with good quality. Further, the present invention also relates to a crystalline polymorphic form of Rosuvastatin ethyl ester.
摘要翻译：本发明涉及具有良好质量的制备式（I）的罗苏伐他汀钙的改进方法。此外，本发明还涉及罗苏伐他汀乙酯的结晶多晶型物。

3. 发明申请

WO2009118598A1 PROCESS FOR THE MANUFACTURE OF ROSUVASTATIN CALCIUM WITH HIGH PURITY 审中-公开
标题翻译：具有高纯度的罗司他汀钙的制备方法
公开(公告)号：WO2009118598A1
公开(公告)日：2009-10-01
申请号：PCT/IB2009/000570
申请日：2009-03-16
申请人： AUROBINDO PHARMA LIMITED , NANGI, Gangadhara, Bhima, Shankar , NANDI, Sukumar , MALLELA, Sambhu, Prasad, Sarma , DANDALA, Ramesh , MEENAKSHISUNDERAM, Sivakumaran
发明人： NANGI, Gangadhara, Bhima, Shankar , NANDI, Sukumar , MALLELA, Sambhu, Prasad, Sarma , DANDALA, Ramesh , MEENAKSHISUNDERAM, Sivakumaran
IPC分类号： C07D239/42
CPC分类号： C07D239/42
摘要： The present invention relates to an improved process to prepare Rosuvastatin calcium of Formula (I), with good quality, which comprises a) reducing Rosuvastatin keto ester of Formula (III) with a hydride ion source and dialkylalkoxyborane at law temperature in a mixture of three or more organic solvents.
摘要翻译：本发明涉及一种制备具有良好质量的式（I）的罗苏伐他汀钙的改进方法，该方法包括：a）在法定温度下，用三价混合物在氢化物离子源和二烷基烷氧基硼烷中还原式（III）的罗苏伐他汀酮酯或更多的有机溶剂。

4. 发明申请

WO2011004242A3 AN IMPROVED PROCESS FOR THE PREPARATION OF DUTASTERIDE 审中-公开
公开(公告)号：WO2011004242A3
公开(公告)日：2011-01-13
申请号：PCT/IB2010/001661
申请日：2010-07-07
申请人： AUROBINDO PHARMA LIMITED , MALLELA, Sambhu, Prasad, Sarma , NANDI, Sukumar , GONA, Balanarasimha, Reddy , AKKINA, Naresh , ANANTA, Rani , AMINUL, Islam , MEENAKSHISUNDERAM, Sivakumaran
发明人： MALLELA, Sambhu, Prasad, Sarma , NANDI, Sukumar , GONA, Balanarasimha, Reddy , AKKINA, Naresh , ANANTA, Rani , AMINUL, Islam , MEENAKSHISUNDERAM, Sivakumaran
IPC分类号： C07J73/00
摘要： The present invention provides an improved process for the preparation of Dutasteride (I) which comprises: (i) reacting 4-aza-5α-androst-l -en-3-one-17β-carboxylic acid (VII), Formula VII with sulfonic acid anhydride (RSO 2 ) 2 O in presence of base to produce an intermediate compound of Formula (XIII), wherein R represents C 1-6 alkyl, C 1-6 halo alkyl, C 6-10 aryl, halo aryl; (ii) condensing compound of Formula (XIII) with 2,5-bis(trifluoromethyl)aniline (III), Formule (III) in the presence or absence of a base to produce Dutasteride (I).

5. 发明申请

WO2008072078A1 AN IMPROVED PROCESS FOR PREPARING ROSUVASTATIN CACLIUM 审中-公开
标题翻译：改进罗斯伐他汀的制备方法
公开(公告)号：WO2008072078A1
公开(公告)日：2008-06-19
申请号：PCT/IB2007/003936
申请日：2007-12-11
申请人： AUROBINDO PHARMA LIMITED , DANDALA, Ramesh , MALLELA, Sambhu Prasad Sarma , NANDI, Sukumar , NANGI, Gangadhar Bhima Shankar , BURIDIPADU, Sunil Kumar , MEENAKSHISUNDERAM, Sivakumaran
发明人： DANDALA, Ramesh , MALLELA, Sambhu Prasad Sarma , NANDI, Sukumar , NANGI, Gangadhar Bhima Shankar , BURIDIPADU, Sunil Kumar , MEENAKSHISUNDERAM, Sivakumaran
IPC分类号： C07D239/42
CPC分类号： C07D239/42
摘要： The present invention relates to an improved process for preparing (2E)-3-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidin-5-yl]-propenal of Formula I which is an intermediate useful in the preparation of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoicacid] calcium salt of Formula II
摘要翻译：本发明涉及制备式（2E）-3- [4-（4-氟苯基）-6-异丙基-2-（N-甲基-N-甲磺酰氨基）嘧啶-5-基] - 丙酸的方法，其是可用于制备双[（E）-7- [4-（4-氟苯基）-6-异丙基-2- [甲基（甲基磺酰基）氨基]嘧啶-5-基]（3R，5S ）-3,5-二羟基庚-6-烯酸]钙盐

6. 发明申请

WO2008038132A1 CRYSTALLINE DIAMINE SALTS OF ROSUVASTATIN 审中-公开
标题翻译： ROSUVASTATIN的结晶二胺盐
公开(公告)号：WO2008038132A1
公开(公告)日：2008-04-03
申请号：PCT/IB2007/002880
申请日：2007-09-24
申请人： AUROBINDO PHARMA LIMITED , DANDALA, Ramesh , MALLELA, Sambhu Prasad Sarma , NANDI, Sukumar , NANGI, Gangadhar Bhima Shankar , MEENAKSHISUNDERAM, Sivakumaran
发明人： DANDALA, Ramesh , MALLELA, Sambhu Prasad Sarma , NANDI, Sukumar , NANGI, Gangadhar Bhima Shankar , MEENAKSHISUNDERAM, Sivakumaran
IPC分类号： C07D239/42
CPC分类号： C07D239/42
摘要： The present invention relates to crystalline rosuvastatin amine salts represented by Formula (I) wherein R 1 , R 2 , R 3 , R 4 independently represent hydrogen, straight or branched chain C 1-15 alkyl, cycloalkyl, optionally substituted aryl, aralkyl, heterocycloalkyl, a heterocyclic residue containing one or more hetero atoms.
摘要翻译：本发明涉及由式（I）表示的结晶瑞舒伐他汀胺盐，其中R 1，R 2，R 3，R 3， 4个独立地表示氢，直链或支链C 1-15烷基，环烷基，任选取代的芳基，芳烷基，杂环烷基，含有一个或多个杂原子的杂环残基。

7. 发明申请

WO2008096257A1 AN IMPROVED PROCESS FOR PREPARATION OF ROSUVASTATIN CALCIUM 审中-公开
标题翻译：改进罗司伐他汀钙的方法
公开(公告)号：WO2008096257A1
公开(公告)日：2008-08-14
申请号：PCT/IB2008/000290
申请日：2008-02-04
申请人： AUROBINDO PHARMA LIMITED , DANDALA, Ramesh , MALLELA, Sambhu Prasad Sarma , NANDI, Sukumar , NANGI, Gangadhar Bhima Shankar , BURIDIPADU, Sunil Kumar , MEENAKSHISUNDERAM, Sivakumaran
发明人： DANDALA, Ramesh , MALLELA, Sambhu Prasad Sarma , NANDI, Sukumar , NANGI, Gangadhar Bhima Shankar , BURIDIPADU, Sunil Kumar , MEENAKSHISUNDERAM, Sivakumaran
IPC分类号： C07D239/42
CPC分类号： C07D239/42
摘要： The present invention relates to an improved process for preparing (E)-7-[4-(4-fluorophenyl)- 6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6- enoic acid calcium of Formula (I).
摘要翻译：本发明涉及制备（E）-7- [4-（4-氟苯基）-6-异丙基-2- [甲基（甲基磺酰基）氨基]嘧啶-5-基]（3R，5S） - 式（I）的3,5-二羟基庚-6-烯酸钙。

8. 发明申请

WO2008053334A3 AN IMPROVED PROCESS FOR PREPARING ROSUVASTATIN CALCIUM 审中-公开
公开(公告)号：WO2008053334A3
公开(公告)日：2008-05-08
申请号：PCT/IB2007/003312
申请日：2007-10-29
申请人： AUROBINDO PHARMA LIMITED , DANDALA, Ramesh , MALLELA, Sambhu Prasad Sarma , GARIMELLA, Narayan K A S S , NANDI, Sukumar , BURIDIPAD, Sunil Kumar , NANGI, Gangadhar Bhima Shankar , MEENAKSHISUNDERAM, Sivakumaran
发明人： DANDALA, Ramesh , MALLELA, Sambhu Prasad Sarma , GARIMELLA, Narayan K A S S , NANDI, Sukumar , BURIDIPAD, Sunil Kumar , NANGI, Gangadhar Bhima Shankar , MEENAKSHISUNDERAM, Sivakumaran
IPC分类号： C07D239/42
摘要： The present invention relates to an improved process for preparing Rosuvastatin calcium of Formula I.

9. 发明申请

WO2012001484A2 AN IMPROVED PROCESS FOR THE PREPARATION OF VALSARTAN 审中-公开
标题翻译：一种改进的缬沙坦制备方法
公开(公告)号：WO2012001484A2
公开(公告)日：2012-01-05
申请号：PCT/IB2011/001483
申请日：2011-06-24
申请人： AUROBINDO PHARMA LIMITED , CHINTA, Raveendra Reddy , NANGI, Gangadhara Bhima Shankar , NAYINI, Mahendar Reddy , YALLAPPA, Somappa Somannavar , BUDIDET, Shankar Reddy , AMINUL, Islam , MEENAKSHISUNDERAM, Sivakumaran
发明人： CHINTA, Raveendra Reddy , NANGI, Gangadhara Bhima Shankar , NAYINI, Mahendar Reddy , YALLAPPA, Somappa Somannavar , BUDIDET, Shankar Reddy , AMINUL, Islam , MEENAKSHISUNDERAM, Sivakumaran
IPC分类号： C07D257/04
CPC分类号： C07D257/04
摘要： The present invention relates to a process for the preparation of pure Valsartan (I) substantially free from impurities of formulae (la), (lb), and (Ic), which comprises: (i) condensing 2-(4'-bromomethylphenyl)benzonitrile of formula (II) with L-valine methyl ester hydrochloride of formula (V) in the presence of a base in a solvent to produce N-[(2'-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester of formula (VI); (ii) treating the compound VI of step (i) with acid followed by treating with base to produce pure compound VI substantially free from dimeric impurity of formula (Via); (iii) reacting the pure compound of formula (VI) with n-valeryl chloride in the presence of a base to produce pure N-valeryl-N-[(2'-cyanobiphenyl-4-yl)methyl]- (L)-valine methyl ester (VII) substantially free from alkene impurity of formula (Vila); (iv) reacting the compound of formula (VII) with trialkyltin chloride and a metal azide in a solvent at a reflux temperature to produce N-(l-oxopentyl)-N-[[2'-(2- tributyltintetrazol-5-yl)-(l, l '-biphenyl)-4-yl]methyl]-(L)-valine methyl ester of formula (VHIb) free from thermal degradation impurity (Villa); (v) hydrolyzing the compound of formula (VHIb) in the presence of alkaline conditions to produce Valsartan (I).
摘要翻译：本发明涉及制备基本上不含式（Ia），（Ib）和（Ic）杂质的纯缬沙坦（I）的方法，其包括：（i）（II）的2-（4'-溴甲基苯基）苄腈与式（V）的L-缬氨酸甲酯盐酸盐在碱的存在下在溶剂中反应，生成N - [（2'-氰基联苯-4-基）（Ⅵ）的甲基] - （L） - 缬氨酸甲酯; （ii）用酸处理步骤（i）的化合物VI，随后用碱处理以产生基本上不含式（VIa）的二聚杂质的纯化合物VI; （iii）使纯的式（VI）化合物与正戊酰氯在碱的存在下反应，生成纯的N-戊酰基-N - [（2'-氰基联苯-4-基）甲基] - （L） - 缬氨酸甲酯（VII）基本上不含式（VIIa）的烯烃杂质; （iv）在回流温度下使式（VII）化合物与氯化三烷基锡和金属叠氮化物在溶剂中反应，生成N-（1-氧代戊基）-N - [[2' - （2-三丁基锡四唑-5-基） - 不含热降解杂质（Villa）的式（VIIIa） - （1,1'-联苯）-4-基]甲基] - （L） - 缬氨酸甲酯; （v）在碱性条件下水解式（VIIIa）化合物以产生缬沙坦（I）。

10. 发明申请

WO2010095024A2 AN IMPROVED PROCESS FOR THE PREPARATION OF CELECOXIB 审中-公开
标题翻译：改进CELECOXIB的制备方法
公开(公告)号：WO2010095024A2
公开(公告)日：2010-08-26
申请号：PCT/IB2010/000325
申请日：2010-02-18
申请人： AUROBINDO PHARMA LIMITED , AMBATI, V Raghava Reddy , GARAGA, Srinivas , MALLELA, Sambhu Prasad Sarma , MEENAKSHISUNDERAM, Sivakumaran
发明人： AMBATI, V Raghava Reddy , GARAGA, Srinivas , MALLELA, Sambhu Prasad Sarma , MEENAKSHISUNDERAM, Sivakumaran
IPC分类号： C07D231/12
CPC分类号： C07D231/12
摘要： The present invention relates to an improved process for the preparation of 4-[5-(4- methy lphenyl)-3-(trifluoromethyl)-1H-pyrazol- 1-yl]benzenesulfonamide of Formula (I), by condensing 1-(4-methylphenyl)-4,4,4-trifluorobutane-1,3-dione (IV), Formula (IV) with 4-hydrazinophenylsulfonamide (V) or its acid addition salt Formula (V) in a solvent selected from water and in presence of acid. The present invention also relates to the process for the purification of Celecoxib in a solvent mixture.
摘要翻译：本发明涉及一种制备式（I）的4- [5-（4-甲基苯基）-3-（三氟甲基）-1H-吡唑-1-基]苯磺酰胺的改进方法，将1-（ 4-氨基苯基磺酰胺（V）或其酸加成盐式（V）的溶剂在选自水和存在酸。本发明还涉及在溶剂混合物中净化塞来昔布的方法。

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