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1. 发明申请

WO2007054978A2 PROCESS FOR PREPARING PAROXETINE HYDROCHLORIDE HEMIHYDRATE 审中-公开
标题翻译：制备环氧氯丙烷硫酸氢盐的方法
公开(公告)号：WO2007054978A2
公开(公告)日：2007-05-18
申请号：PCT/IN2006000446
申请日：2006-11-10
申请人： JUBILANT ORGANOSYS LTD , DUBEY SHAILENDRA KUMAR , KUMAR PRAMOD , DUBEY SUSHIL KUMAR
发明人： DUBEY SHAILENDRA KUMAR , KUMAR PRAMOD , DUBEY SUSHIL KUMAR
IPC分类号： C07D405/02
CPC分类号： C07D405/12
摘要： Disclosed herein a process for the preparation of crystalline paroxetine hydrochloride in hemihydrate form employing a selective solvent system to achieve stable and non- hygroscopic form which is easy to prepare and convenient to operate on commercial scale.
摘要翻译：本文公开了以半水合物形式制备结晶帕罗西汀盐酸盐的方法，其采用选择性溶剂体系以实现易于制备和方便在商业规模下操作的稳定和非吸湿性形式。

2. 发明申请

WO2009013764A3 PROCESS FOR PRODUCING 6(R)-[2-(8'(S)-2 ",2 "-DIMETHYLBUTYRYLOXY-2'(S),6'(R)-DIMETHYL-1,2,6,7', 8',8A'(R)- HEXAHYDRONAPHTHYL-L'(S))ETHYL]-4(R)-HYDROXY-3,4,5,6- TETRAHYDRO-2H-PYRAN-2-ONE 审中-公开
标题翻译：制备6（R） - [2-（8'（S）-2“，2” - 二甲基丁酰氧基-2'（S），6'（R） - 二甲基-1,2,6,7'，8 '，8A'（R） - 十六氢萘基-L'（S））乙基] -4（R） - 羟基-3,4,5,6-四氢-2H-吡喃-2-酮
公开(公告)号：WO2009013764A3
公开(公告)日：2009-03-19
申请号：PCT/IN2008000467
申请日：2008-07-24
申请人： JUBILANT ORGANOSYS LTD , SINGH HARNAM , DUBEY SHAILENDRA KUMAR , GUPTA NITIN , DUBEY SUSHIL KUMAR
发明人： SINGH HARNAM , DUBEY SHAILENDRA KUMAR , GUPTA NITIN , DUBEY SUSHIL KUMAR
IPC分类号： C07D309/30
CPC分类号： C07D309/30
摘要： Disclosed herein is an improved process for producing HMG-CoA reductase inhibitor, 6(R)-[2-(8 '(S)-2 ",2 ''-dimethylbutyryloxy-2'(S),6 '(R)-dimethyl- 1', 2', 6', 7', 8',8a'(R)-hexahydronaphthyl-r(S))ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H- pyran-2-one, the process comprising hydrolyzing (lS,3R,7S,8S,8aR)-8-{2-[(2R,4R)- 4-hydroxy-6-oxotetrahydro-2H-?yran-2-yl]ethyl}-3,7-dimethyl-l,2,3,7,8,8a- hexahydronaphthalen-1-yl (2S)-2-methylbutanoate in presence of a base and antioxidant, lactonizing and selectively protecting the hydroxyl group of the resultant compound, followed by acylation with an acylating agent to obtain 6(R)-[2-(8'(S)- 2",2''-dimethylbutyryloxy-2 '(S),6 '(R)-dimethyl- 1',2',6',7',8',8a'(R)- hexahydronaphthyl-r(S))ethyl]-4(R)-substituted)-3,4,5,6-tetrahydro-2H-pyran-2-one and further deprotection to obtain 6(R)-[2-(8'(S)-2",2"-dimethylbutyryloxy- 2'(S),6'(R)-dimethyl-1',2',6',7',8',8a'(R)-hexahydronaphthyl-1'(S))ethyl]-4(R)- hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one.
摘要翻译：本文公开了一种生产HMG-CoA还原酶抑制剂，6（R） - [2-（8'（S）-2“，2” - 二甲基丁酰氧基-2'（S），6'（R） - （R） - 六氢萘基-r（S））乙基] -4（R） - 羟基-3,4,5,6-四氢 - （1S，3R，7S，8S，8aR）-8- {2 - [（2R，4R）-4-羟基-6-氧代四氢-2H-哒嗪-2 - 基]乙基} -3,7-二甲基-1,2,3,7,8,8a-六氢萘-1-基（2S）-2-甲基丁酸酯在碱和抗氧化剂存在下，内酯化和选择性保护羟基然后用酰化剂酰化，得到6（R） - [2-（8'（S）-2“，2” - 二甲基丁酰氧基-2'（S），6'（R） - 二甲基-1'，2'，6'，7'，8'，8a'（R） - 六氢萘基-r（S））乙基] -4（R） - 取代的）四氢-2H-吡喃-2-酮，进一步脱保护，得到6（R） - [2-（8'（S）-2“，2” - 二甲基丁酰氧基-2'（S），6'（R） -1'，2'，6'，7'，8'，8a'（R） - 六氢萘基-1'（S））乙基] -4（R） - 羟基-3,4,5,6-四氢 - -2H-吡喃-2-酮。

3. 发明申请

WO2006111983A2 NOVEL POLYMORPHIC FORM OF (l-BENZYL-4-[(5,6-DIMETHOXY-l- INDANONE)-2-YL]METHYL PIPERIDINE HYDROCHLORIDE AND PROCESS FOR PREPARING THE SAME 审中-公开
标题翻译：（1-苄基-4 - [（5,6-二甲氧基-1-吲哚酮）-2-基]甲基哌啶盐酸氢盐的新型多晶型及其制备方法
公开(公告)号：WO2006111983A2
公开(公告)日：2006-10-26
申请号：PCT/IN2006000136
申请日：2006-04-21
申请人： JUBILANT ORGANOSYS LTD , DUBEY SHAILENDRA KUMAR , GUPTH POORVI , THAPER RAJESH KUMAR , DUBEY SUSHIL KUMAR
发明人： DUBEY SHAILENDRA KUMAR , GUPTH POORVI , THAPER RAJESH KUMAR , DUBEY SUSHIL KUMAR
CPC分类号： C07D211/32
摘要： Disclosed herein are novel and stable polymorphic form of Donepezil Hydrochloride, wherein said polymorphic form is designated as J and are characterized by their powder X-ray diffraction patterns, Infrared absorption spectrums, thermo gravimetric analysis and differential scanning calorimetry. The processes for preparing said polymorphic form and use thereof to prepare another forms is also disclosed.
摘要翻译：本文公开了多奈哌齐盐酸盐的新颖且稳定的多晶型物，其中所述多晶型物称为J，其特征在于它们的粉末X射线衍射图，红外吸收光谱，热重分析和差示扫描量热法。还公开了制备所述多晶形式及其用途以制备另一种形式的方法。

4. 发明申请

WO2005076749A3 A NOVEL PROCESS FOR THE PREPARATION OF 1-BENZYL-4-[(5,6-DIMETHOXY-1-INDANON-2-YL)METHYL]PIPERIDINE 审中-公开
标题翻译：制备1-苄基-4 - [（5,6-二甲氧基-1-吲哚-2-基）甲基]哌嗪的新工艺
公开(公告)号：WO2005076749A3
公开(公告)日：2006-06-08
申请号：PCT/IN2005000044
申请日：2005-02-11
申请人： JUBILANT ORGANOSYS LTD , DUBEY SHAILENDRA KUMAR , CHAVHAN BHAUSAHEB , SHARMA AMIT KUMAR , PAUL SOUMENDU , THAPER RAJESH KUMAR , DUBEY SUSHIL KUMAR , KHANNA JAG MOHAN
发明人： DUBEY SHAILENDRA KUMAR , CHAVHAN BHAUSAHEB , SHARMA AMIT KUMAR , PAUL SOUMENDU , THAPER RAJESH KUMAR , DUBEY SUSHIL KUMAR , KHANNA JAG MOHAN
IPC分类号： C07D211/02 , C07D211/32 , C07D211/70
CPC分类号： C07D211/02 , C07D211/32 , C07D211/70
摘要： Disclosed herein is the novel process for producing 1-benzyl-4-(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine (donepezil) of formula [I] by treating novel starting compound 1,2,3,6-tetrahydropyridine derivative of formula [V] with 5,6-dimethoxy-1-indanone of formula [IV] to obtain an intermediate 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2yl)methyl]-1,2,3,6-tetrahydro pyridine of formula [II] and reducing the same to produce 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine of formula [I]. The invention further comprising the process for preparation of the novel compound of formula [V].
摘要翻译：本文公开了通过处理新的起始化合物1,2,3（1）的新型制备式[I]的1-苄基-4-（5,6-二甲氧基-1-茚满酮-2-基）甲基]哌啶（多奈哌齐）式[Ⅴ]的6-四氢吡啶衍生物与式[Ⅳ]的5,6-二甲氧基-1-二氢茚酮得到中间体1-苄基-4 - [（5,6-二甲氧基-1-茚满酮基）甲基 ] -1,2,3,6-四氢吡啶并将其还原，得到式（I）的1-苄基-4 - [（5,6-二甲氧基-1-茚满-2-基）甲基]哌啶 [一世]。本发明还包括制备式[Ⅴ]新化合物的方法。

5. 发明申请

WO2008012837A8 PROCESS FOR PRODUCING 10-OXO-L10, 11-DIHYDR0-5H-DIBENZ [B, F] AZEPINE-5-CARBOXAMIDE STARTING FROM 5-CYANOIMINOSTILBENE 审中-公开
标题翻译：用于生产从5-氰基氨基甲酸酯起始的10-OXO-L10,11-二氢吲哚-5H-二苯并[B，F]亚胺-5-羧酰胺的方法
公开(公告)号：WO2008012837A8
公开(公告)日：2008-05-08
申请号：PCT/IN2007000307
申请日：2007-07-24
申请人： JUBILANT ORGANOSYS LTD , SINGH HARNAM , GUPTA NITIN , KUMAR PRAMOD , DUBEY SUSHIL KUMAR
发明人： SINGH HARNAM , GUPTA NITIN , KUMAR PRAMOD , DUBEY SUSHIL KUMAR
IPC分类号： C07D223/26 , C07D223/28
CPC分类号： C07D223/26 , C07D223/28
摘要： Disclosed herein is a process for producing 10-oxo-10,11-dihydro-5H-dibenz[bf] azepine-5-carboxamide of formula I via novel intermediates 11-alkoxy-10-halo-10,11-dihydro-5H-dibenzo [b,f ] azepine-5-carbonitrile [XIX] or 10-alkoxy-5H-dibenz [b,f] azepine -5-carbonitrile [XX]. Further the present invention also provides a process for preparation of said intermediates.
摘要翻译：本文公开了通过新的中间体11-烷氧基-10-卤代-10,11-二氢-5H-咪唑并[1,2-a]所示的式I的10-氧代-10,11-二氢-5H-二苯并[bf]吖庚因-5-甲酰胺的制备方法，二苯并[b，f]吖庚因-5-甲腈[XIX]或10-烷氧基-5H-二苯并[b，f]吖庚因-5-甲腈[XX]。此外，本发明还提供了制备所述中间体的方法。

6. 发明申请

WO2006067795A3 NOVEL POLYMORPHIC FORMS OF ATORVASTATIN LACTONE AND PROCESS FOR PREPARING THE SAME 审中-公开
标题翻译：异烟肼的新型多形态及其制备方法
公开(公告)号：WO2006067795A3
公开(公告)日：2009-04-16
申请号：PCT/IN2004000401
申请日：2004-12-23
申请人： JUBILANT ORGANOSYS LTD , BHATRAJU SREENIVAS RAO , DUA ANNU , KAUSHIK GEETESH , THAPER RAJESH KUMAR , DUBEY SUSHIL KUMAR
发明人： BHATRAJU SREENIVAS RAO , DUA ANNU , KAUSHIK GEETESH , THAPER RAJESH KUMAR , DUBEY SUSHIL KUMAR
IPC分类号： C07D207/36
CPC分类号： C07D405/06
摘要： The present invention provides novel crystalline polymorphic Forms and amorphous Form of atorvastatin lactone, characterized by powder X-ray diffraction pattern and Infrared absorption spectrum. The novel processes for their preparation are also disclosed.
摘要翻译：本发明提供了阿托伐他汀内酯的新型结晶多晶型和无定形形式，其特征在于粉末X射线衍射图和红外吸收光谱。还公开了其制备的新方法。

7. 发明申请

WO2006085338A3 NOVEL POLYMORPHIC FORMS OF FLUVASTATIN SODIUM AND PROCESS FOR PREPARING THE SAME 审中-公开
标题翻译：氟维沙星钠的新型多晶型及其制备方法
公开(公告)号：WO2006085338A3
公开(公告)日：2009-04-09
申请号：PCT/IN2006000045
申请日：2006-02-10
申请人： JUBILANT ORGANOSYS LTD , CHAVHAN BHAUSAHEB , AWASTHI ARUN KUMAR , AGGARWAL RICHA , BEENA RANI S , SOUMENDU PAUL , THAPER RAJESH KUMAR , DUBEY SUSHIL KUMAR
发明人： CHAVHAN BHAUSAHEB , AWASTHI ARUN KUMAR , AGGARWAL RICHA , BEENA RANI S , SOUMENDU PAUL , THAPER RAJESH KUMAR , DUBEY SUSHIL KUMAR
IPC分类号： C07D209/12
CPC分类号： C07D209/10
摘要： Disclosed herein are novel polymorphic forms of Fluvastatin sodium, wherein said polymorphic forms are designated as JF, JF1, JF2, JF3 and are characterized by their powder X-ray diffraction patterns, Infrared absorption spectrums, thermo gravimetric analysis and differential scanning calorimetry. The processes for preparing said polymorphic forms are also disclosed. , The present invention also relates to process for preparing amorphous form of Fluvastatin sodium.
摘要翻译：本文公开了氟伐他汀钠的新型多晶型物，其中所述多晶型物质命名为JF，JF1，JF2，JF3，其特征在于它们的粉末X射线衍射图，红外吸收光谱，热重分析和差示扫描量热法。还公开了制备所述多晶型物的方法。本发明还涉及制备氟伐他汀钠无定形形式的方法。

8. 发明申请

WO2005069741A3 PROCESS FOR PRODUCING SIMVASTATIN USING NOVEL HYDRAZIDE INTERMEDIATES 审中-公开
标题翻译：使用新的肼基中间体生产辛伐他汀的方法
公开(公告)号：WO2005069741A3
公开(公告)日：2005-12-22
申请号：PCT/IN2004000302
申请日：2004-09-28
申请人： JUBILANT ORGANOSYS LTD , PANCHASARA DINESH R , JAISWAL SANJAY , SINGH GOVIND , BHADWAL PARAMVIR , THAPER RAJESH KUMAR , DUBEY SUSHIL KUMAR , KHANNA JAG MOHAN
发明人： PANCHASARA DINESH R , JAISWAL SANJAY , SINGH GOVIND , BHADWAL PARAMVIR , THAPER RAJESH KUMAR , DUBEY SUSHIL KUMAR , KHANNA JAG MOHAN
IPC分类号： C07C67/28 , C07C243/24 , C07C243/32 , C07D309/30 , C07F7/18
CPC分类号： C07C243/32 , C07C2602/02 , C07D309/30 , C07F7/1856 , C07F7/1892
摘要： This invention relates to an industrially feasible process for producing HMG-CoA reductase inhibitor, simvastatin via novel intermediates, wherein the process comprises treating lovastatin [2] or lovastatin ammonium salt [2'] with hydrazine or hydrazine derivatives to obtain lovastatin hydrazide [3], optionally protecting the hydroxyl groups of hydrazide intermediate [3] to obtain protected lovastatin hydrazide intermediate [4] which is further used in the process for producing simvastatin [1].
摘要翻译：本发明涉及一种工业上可行的通过新中间体制备HMG-CoA还原酶抑制剂辛伐他汀的方法，其中该方法包括用肼或肼衍生物处理洛伐他汀[2]或洛伐他汀铵盐[2']以获得洛伐他汀酰肼[3] ，任选地保护酰肼中间体[3]的羟基以获得被保护的洛伐他汀酰肼中间体[4]，其进一步用于生产辛伐他汀[1]的方法中。

9. 发明申请

WO2011092564A3 PROCESS FOR THE PREPARATION OF TEMSIROLIMUS AND ITS INTERMEDIATES 审中-公开
标题翻译：制备纤维素及其中间体的方法
公开(公告)号：WO2011092564A3
公开(公告)日：2011-12-01
申请号：PCT/IB2011000084
申请日：2011-01-20
申请人： FRESENIUS KABI ONCOLOGY LTD , GUPTA NITIN , HANDA VISHAL , PAL ABIR KUMAR , SINGH HEMAT KUMAR , LAHIRI SASWATA , DUBEY SUSHIL KUMAR
发明人： GUPTA NITIN , HANDA VISHAL , PAL ABIR KUMAR , SINGH HEMAT KUMAR , LAHIRI SASWATA , DUBEY SUSHIL KUMAR
IPC分类号： C07D319/06 , C07D498/18
CPC分类号： C07D498/18 , C07D319/06
摘要： Intermediates, process for their preparation and their use in the preparation of therapeutically effective antineoplastic agents, in particular Temsirolimus of formula (I).
摘要翻译：中间体，其制备方法及其在制备治疗有效的抗肿瘤药物中的用途，特别是式（I）的替西罗莫司。

10. 发明申请

WO02088149A3 A PROCESS FOR MANUFACTURE OF FOSINOPRIL SODIUM 审中-公开
标题翻译：一种制造FOSINOPRIL SODIUM的方法
公开(公告)号：WO02088149A3
公开(公告)日：2003-06-05
申请号：PCT/IN0100144
申请日：2001-08-17
申请人： LUPIN LAB LTD , DUBEY SUSHIL KUMAR , LAHIRI SASWATA , SINGH ANIL VIR
发明人： DUBEY SUSHIL KUMAR , LAHIRI SASWATA , SINGH ANIL VIR
IPC分类号： C07B57/00 , C07B61/00 , C07F9/572
CPC分类号： C07F9/5721
摘要： The present invention discloses a process for the synthesis of fosinopril as a single desired isomer of high purity in two steps comprising of (a) preparation of fosinopril as a mixture of four diastereomers and (b) separation of the desired isomer from the mixture through formation of alkali metal salts followed by crystallisation.
摘要翻译：本发明公开了一种在两个步骤中合成作为高纯度的单一所需异构体的福辛普利的方法，包括（a）以四种非对映异构体的混合物制备福辛普利，和（b）通过形成从所述混合物中分离所需的异构体的碱金属盐，随后结晶。

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