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1. 发明申请

WO2011141805A3 PROCESS FOR THE MANUFACTURE OF LAMIVUDINE 审中-公开
标题翻译：制造拉米夫定的方法
公开(公告)号：WO2011141805A3
公开(公告)日：2012-03-22
申请号：PCT/IB2011001013
申请日：2011-05-12
申请人： LUPIN LTD , ROY BHAIRAB NATH , SINGH GIRIJ PAL , SHRIVASTAVA DHANANJAI , JADHAV HARISHCHANDRA SAMBHAJI , AHER UMESH PARASHRAM , DEOKAR SHARAD CHANDRABHAN
发明人： ROY BHAIRAB NATH , SINGH GIRIJ PAL , SHRIVASTAVA DHANANJAI , JADHAV HARISHCHANDRA SAMBHAJI , AHER UMESH PARASHRAM , DEOKAR SHARAD CHANDRABHAN
IPC分类号： C07D411/04
CPC分类号： C07D411/04
摘要： The present invention relates to an improved process for the Manufacture of Lamivudine. A process for the preparation of essentially enantiomerically pure (-)-[2R, 5S]-4-amino-1-[2- (hydroxymethyl)-1,3-oxathiolan-5-y1]-2(1H)-pyrimidin-2-one of formula (I), from L-menthyl glyoxylate is described. Also provided is a process for preparation of (+)-1- (2R/S-Cis)-4-amino-1-[(2-hydroxymethyl)-1,3-oxathiolan-5-y1]-2(1H)-pyrimidin-2-one of formula (XII), from L-menthyl glyoxylate.
摘要翻译：本发明涉及拉米夫定的制造方法。制备基本上对映体纯的（ - ） - [2R，5S] -4-氨基-1- [2-（羟甲基）-1,3-氧硫杂环戊烷-5-基] -2（1H） - 嘧啶-2-基 - 描述了式（I）的2-酮，乙醛酸L-薄荷酯。还提供了制备（+） - 1-（2R / S-顺式）-4-氨基-1 - [（2-羟甲基）-1,3-氧硫杂环戊烷-5-基] -2（1H）（XII）的嘧啶-2-酮，由乙醛酸L-薄荷酯。

2. 发明申请

WO2012007814A3 THREE COMPONENT CO-CRYSTAL FORMATION BETWEEN DIASTEREOMERIC MIXTURES OF 3-ALKYL-4-((S)-1'PHENYLETHYLAMINO) BUTANOIC ACID AND OPTICALLY PURE 1, 1'-BI-2-NAPHTHOL 审中-公开
标题翻译： 3-ALKYL-4 - （（S）-1'-苯基氨基甲酸）二油酸和光学纯度1'-BI-2-NAPHTHOL的二元醇混合物之间的三种组分共晶形成
公开(公告)号：WO2012007814A3
公开(公告)日：2012-03-08
申请号：PCT/IB2011001605
申请日：2011-07-11
申请人： LUPIN LTD , ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , MITRA RANGAN
发明人： ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , MITRA RANGAN
IPC分类号： C07C37/84 , C07C39/14 , C07C229/14
CPC分类号： C07C229/14 , C07B2200/07 , C07B2200/13 , C07C37/84 , C07C39/14
摘要： A ternary co-crystal consisting of 1 :0.5:0.5 molar proportion of (S)-1,1'-bi-2-naphthol, 3(S)-propyl-4-[(S)1 '-phenyl-ethylamino]-butanoic acid and 3(R)-propyl-4-[(S)1'- phenyl-ethylamino]-butanoic acid having characteristic powder X-ray diffraction pattern with 2T values of 8.41, 9.38, 10.32, 12.16, 15.52, 15.51, 17.84, 17.95, 19.16, 20.37, 21.74, 22.55, 24.44, 25.65, 28.40, 29.15, 29.69, 31.31, 33.54, 34.40, 35.43 (±0.2) and having differential scanning calorimetric peak at about 189.23 ° C when analyzed at the rate of heating of 10°C per minute and process for preparing the same. A process for resolution of (S)-1,1'-bi-2-naphthol from RS-1,1'-bi-2-naphthol.
摘要翻译：由（S）-1,1'-双-2-萘酚，3（S） - 丙基-4 - [（S）-1'-苯基 - 乙基氨基] - 丁酸和具有特征性粉末X射线衍射图的3（R） - 丙基-4 - [（S）1'-苯基 - 乙基氨基] - 丁酸，其中2T值为8.41,9.38,10.32,12.16,15.52,15.51 ，17.84,17.95,19.16,20.37,21.74,22.55,24.44,25.65,2840,29.15,29.69,31.31,33.54,34.40,35.43（±0.2），并且当以速率分析时在约189.23℃下具有差示扫描量热峰每分钟加热10℃，其制备方法。从RS-1,1'-双-2-萘酚中分离出（S）-1,1'-双-2-萘酚的方法。

3. 发明申请

WO2012153162A1 NOVEL METHOD FOR PREPARATION OF ATOVAQUONE 审中-公开
标题翻译：用于制备大田的新方法
公开(公告)号：WO2012153162A1
公开(公告)日：2012-11-15
申请号：PCT/IB2011/001507
申请日：2011-06-28
申请人： LUPIN LIMITED , ROY, Bhairab, Nath , SINGH, Girij, Pal , LATHI, Piyush, Suresh , AGRAWAL, Manoj, Kunjabihari , MITRA, Rangan , TRIVEDI, Anurag
发明人： ROY, Bhairab, Nath , SINGH, Girij, Pal , LATHI, Piyush, Suresh , AGRAWAL, Manoj, Kunjabihari , MITRA, Rangan , TRIVEDI, Anurag
IPC分类号： C07C46/00 , C07C49/403 , C07C49/427 , C07C50/24 , C07C50/26 , C07C50/34
CPC分类号： C07C46/00 , C07C37/07 , C07C39/42 , C07C45/513 , C07C45/62 , C07C45/63 , C07C45/66 , C07C46/06 , C07C49/697 , C07C50/32 , C07C2601/14 , C07C2601/16 , C07C2602/10 , C07F7/1852 , C07C49/747 , C07C50/24
摘要： Provided is a process of preparation of 2-[ trans ,-4-(4'-chlorophenyl)cyclohexyl]-3-hydroxy- 1,4-naphthoquinone, i.e. Atovaquone [I] which is cost effective, green, and eco-friendly process, without separation of any diastereomers or geometric isomers of intermediates obtained during the reactions. Also provided is separation of ' cis ' and ' trans ' isomer of intermediates VI, VII and VIII through selective crystallization in an appropriate solvent. A method for converting 2-[ cis ,-4-(4'-chlorophenyl)cyclohexyl]-3-hydroxy-1,4-naphthoquinone to 2-[ trans -4-(4'-chlorophenyl)cyclohexyl]-3-hydroxy-l,4-naphthoquinone in presence of Lewis/ Bronsted acid is also provided. A process for preparation of compound 2-(4-(4- chlorophenyl)- 1 -hydroxy cyclohexyl)-3,4-dihydronaphthalen- 1 (2H)-one [IV] comprising condensation of (1,2-dihydronaphthalen-4-yloxy)trimethylsilane [II] with 4-(4- chlorophenyl)cyclohexanone [III] in presence of Lewis acid in organic solvent. The invention also encompasses a highly efficient and atomeconomic process for synthesis of compound [III] i.e. 4-(4-chlorophenyl)cyclohexanone as well as a process for synthesis of 2-[ cis -4-(4'- chlorophenyl)cyclohexyl]-3-hydroxy-l,4-naphthoquinone. Further provided is a process for isomerization of cis- Atovaquone i.e. 2-[ cis -4-(4'-chlorophenyl)cyclohexyl]-3-hydroxy-l,4- naphthoquinone to tnms-Atovaquone i.e. 2-[ trans -4-(4'-chlorophenyl)cyclohexyl]-3- hydroxy- 1,4-naphthoquinone in presence of Lewis acid.
摘要翻译：提供制备2- [反式，4-（4'-氯苯基）环己基] -3-羟基-1,4-萘醌的方法，即具有成本效益，绿色和环保的Atovaquone [I] 方法，而不分离在反应期间获得的中间体的任何非对映异构体或几何异构体。还提供了通过在合适的溶剂中选择性结晶来分离中间体VI，VII和VIII的“顺式”和“反式”异构体。将2- [顺式，4-（4'-氯苯基）环己基] -3-羟基-1,4-萘醌转化为2- [反式-4-（4'-氯苯基）环己基] -3-羟基还提供了路易斯/布朗斯台德酸存在下的1,4-萘醌。制备化合物2-（4-（4-氯苯基）-1-羟基环己基）-3,4-二氢萘-1（2H） - 酮[Ⅳ]的方法，包括（1,2-二氢萘-4-基）氧基）三甲基硅烷[II]与4-（4-氯苯基）环己酮[III]在路易斯酸存在下在有机溶剂中反应。本发明还包括用于合成化合物[III]即4-（4-氯苯基）环己酮的高效和原子经济方法，以及合成2- [顺式-4-（4'-氯苯基）环己基] - 3-羟基-1,4-萘醌。还提供了顺式 - 阿托瓦醌异构化方法，即2- [顺式-4-（4'-氯苯基）环己基] -3-羟基-1,4-萘醌与叔 - 阿托喹醌即2- [反式-4-（ 4'-氯苯基）环己基] -3-羟基-1,4-萘醌在路易斯酸存在下进行。

4. 发明申请

WO2012059798A3 NOVEL METHOD FOR RACEMIZATION OF OPTICALLY PURE ß-CYANO ESTER TO CORRESPONDING RACEMIC ß-CYANO ACID 审中-公开
标题翻译：光学纯β-氰基酯相应的反应性β-氰基酸的新方法
公开(公告)号：WO2012059798A3
公开(公告)日：2012-07-19
申请号：PCT/IB2011000485
申请日：2011-03-07
申请人： LUPIN LTD , ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , AGRAWAL MANOJ KUNJABIHARI , MITRA RANGAN , RUPNAWAR MANOJ DATTATRAYA
发明人： ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , AGRAWAL MANOJ KUNJABIHARI , MITRA RANGAN , RUPNAWAR MANOJ DATTATRAYA
IPC分类号： C07C253/30 , C07C255/18
CPC分类号： C07C253/30 , C07C255/19
摘要： A novel process for racemization of (R)-3-cyano-5 -methyl hexanoic acid ethyl ester directly to (RS)-3-cyano-5 -methyl hexanoic acid has been developed through a base catalyzed mechanism in a specific solvent system.
摘要翻译：（R）-3-氰基-5-甲基己酸乙酯直接向（RS）-3-氰基-5-甲基己酸外消旋的新方法已经通过在特定溶剂体系中的碱催化机理开发出来。

5. 发明申请

WO2012007814A2 THREE COMPONENT CO-CRYSTAL FORMATION BETWEEN DIASTEREOMERIC MIXTURES OF 3-ALKYL-4-((S)-1'PHENYLETHYLAMINO) BUTANOIC ACID AND OPTICALLY PURE 1, 1'-BI-2-NAPHTHOL 审中-公开
标题翻译： 3-烷基-4 - （（S）-1'苯基乙基氨基）丁酸的异构混合物与光学纯的1,1'-BI-2-萘酚之间的三元共晶形成
公开(公告)号：WO2012007814A2
公开(公告)日：2012-01-19
申请号：PCT/IB2011/001605
申请日：2011-07-11
申请人： LUPIN LIMITED , ROY, Bhairab, Nath , SINGH, Girij, Pal , LATHI, Piyush, Suresh , MITRA, Rangan
发明人： ROY, Bhairab, Nath , SINGH, Girij, Pal , LATHI, Piyush, Suresh , MITRA, Rangan
IPC分类号： C07C37/84
CPC分类号： C07C229/14 , C07B2200/07 , C07B2200/13 , C07C37/84 , C07C39/14
摘要： A ternary co-crystal consisting of 1 :0.5:0.5 molar proportion of (S)-1,1'-bi-2-naphthol, 3( S )-propyl-4-[( S )1 '-phenyl-ethylamino]-butanoic acid and 3( R )-propyl-4-[( S )1'- phenyl-ethylamino]-butanoic acid having characteristic powder X-ray diffraction pattern with 2Θ values of 8.41, 9.38, 10.32, 12.16, 15.52, 15.51, 17.84, 17.95, 19.16, 20.37, 21.74, 22.55, 24.44, 25.65, 28.40, 29.15, 29.69, 31.31, 33.54, 34.40, 35.43 (±0.2) and having differential scanning calorimetric peak at about 189.23 ° C when analyzed at the rate of heating of 10°C per minute and process for preparing the same. A process for resolution of ( S )-1,1'-bi-2-naphthol from RS -1,1'-bi-2-naphthol.
摘要翻译：由（S）-1,1'-联-2-萘酚，3（S） - 叔丁基二甲基甲硅烷基氧化物和（S）-1,1'-联-2-萘酚组成的三元共晶体，（S）-1'-苯基 - 乙基氨基] - 丁酸和3（R） - 丙基-4 - [（S） - 丙基-4 - [（S））具有2θ值为8.41,9.38,10.32,12.16,15.52,15.51,17.84,17.95,19.16,20.37,21.74,22.55,24.44的特征性粉末X射线衍射图的1'-苯基 - 乙基氨基] - 丁酸，25.65,28.40,29.15,29.69,31.31,33.54,34.40,35.43（±0.2），并且在约189.23℃具有差示扫描量热峰。当以每分钟10℃的加热速率进行分析时，以及其制备方法。从RS-1,1'-二-2-萘酚中拆分（S）-1,1'-联-2-萘酚的方法。 >

6. 发明申请

WO2011141923A3 IMPROVED SYNTHESIS OF OPTICALLY PURE (S) - 3-CYANO-5-METHYL-HEXANOIC ACID ALKYL ESTER, AN INTERMEDIATE OF (S)- PREGABALIN 审中-公开
标题翻译：改进的光学纯（S）-3-氰基-5-甲基 - 十六烷酸酸式酯，中间体（S） - 孕酮
公开(公告)号：WO2011141923A3
公开(公告)日：2012-01-19
申请号：PCT/IN2010000440
申请日：2010-06-28
申请人： LUPIN LTD , ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , AGRAWAL MANOJ KUNJABIHARI , PISE VIJAY SADASHIV
发明人： ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , AGRAWAL MANOJ KUNJABIHARI , PISE VIJAY SADASHIV
IPC分类号： C07C253/30 , C07C51/363 , C07C67/08 , C07C67/343 , C07C231/02 , C07C253/20
CPC分类号： C07C51/363 , C07B2200/07 , C07C67/08 , C07C67/303 , C07C67/343 , C07C253/20 , C07C253/30 , C07C253/34 , C07C255/22 , C07C53/19 , C07C69/40 , C07C69/593 , C07C69/34 , C07C255/19
摘要： The present invention is directed towards synthesis of (S) - 3-cyano-5-methyl-hexanoic acid ethyl ester. A cost effective, eco-friendly process for preparation of enantiomerically pure (S)-3-cyano-5-methyl-hexanoic acid alkyl ester, intermediate of ?-amino acids, particularly (S)-pregabalin.
摘要翻译：本发明涉及（S）-3-氰基-5-甲基 - 己酸乙酯的合成。用于制备对映异构体纯（S）-3-氰基-5-甲基 - 己酸烷基酯的成本有效，环保的方法，α-氨基酸，特别是（S） - 普瑞巴林的中间体。

7. 发明申请

WO2009113081A1 TRIS (HYDROXYMETHYL ) AMINO METHANE SALT OF QUINAPRIL AND RAMIPRIL 审中-公开
标题翻译：奎尼泊尔和RAMIPRIL的TRIS（羟甲基）氨基甲酸盐
公开(公告)号：WO2009113081A1
公开(公告)日：2009-09-17
申请号：PCT/IN2008/000275
申请日：2008-04-28
申请人： LUPIN LIMITED , ROY, Bhairab, Nath , SINGH, Girij, Pal , GODBOLE, Himanshu, Madhav , NEHATE, Sagar, Purushottam , RANANAWARE, Umesh, Babanrao
发明人： ROY, Bhairab, Nath , SINGH, Girij, Pal , GODBOLE, Himanshu, Madhav , NEHATE, Sagar, Purushottam , RANANAWARE, Umesh, Babanrao
IPC分类号： C07D209/52 , C07D217/26
CPC分类号： C07D217/26 , C07D209/52
摘要： The present invention relates to sable tris (hydroxymethyl) amino methane salts of quinapril and ramipril, process for preparation and pharmaceutical formulations thereof.
摘要翻译：本发明涉及喹诺酮和雷米普利的适当的三（羟甲基）氨基甲烷盐，其制备方法和药物制剂。

8. 发明申请

WO2013021290A1 A STEREOSELECTIVE PROCESS FOR PREPARATION OF 1,3-OXATHIOLANE NUCLEOSIDES 审中-公开
标题翻译：用于制备1,3-二氧杂环己烷核苷酸的立体选择性方法
公开(公告)号：WO2013021290A1
公开(公告)日：2013-02-14
申请号：PCT/IB2012/050117
申请日：2012-01-10
申请人： LUPIN LIMITED , ROY, Bhairab, Nath , SINGH, Girij, Pal , SRIVASTAVA, Dhananjai , AHER, Umesh, Parasharam , PATIL, Sudhakar, Uttam
发明人： ROY, Bhairab, Nath , SINGH, Girij, Pal , SRIVASTAVA, Dhananjai , AHER, Umesh, Parasharam , PATIL, Sudhakar, Uttam
IPC分类号： C07D411/04
CPC分类号： C07D411/04
摘要： The present invention relates to a stereoselective glycosylation for the preparation of 1,3-oxathiolane nucleoside in high yield and high optical purity. The invention specifically relates to a process of the preparation of Lamivudine and Emtricitabine using zirconium (IV) chloride (ZrCl 4 ) as a catalyst in glycosylation.
摘要翻译：本发明涉及以高产率和高光学纯度制备1,3-氧硫杂环戊烷核苷的立体选择性糖基化。本发明具体涉及使用氯化锆（IV）（ZrCl 4）作为糖基化催化剂制备拉米夫定和恩曲他滨的方法。

9. 发明申请

WO2012059798A2 NOVEL METHOD FOR RACEMIZATION OF OPTICALLY PURE β-CYANO ESTER TO CORRESPONDING RACEMIC β-CYANO ACID 审中-公开
标题翻译：用于将光学纯β-脯氨酸酯转化成相应的甲磺酸的新方法
公开(公告)号：WO2012059798A2
公开(公告)日：2012-05-10
申请号：PCT/IB2011/000485
申请日：2011-03-07
申请人： LUPIN LIMITED , ROY, Bhairab, Nath , SINGH, Girij, Pal , LATHI, Piyush, Suresh , AGRAWAL, Manoj, Kunjabihari , MITRA, Rangan , RUPNAWAR, Manoj, Dattatraya
发明人： ROY, Bhairab, Nath , SINGH, Girij, Pal , LATHI, Piyush, Suresh , AGRAWAL, Manoj, Kunjabihari , MITRA, Rangan , RUPNAWAR, Manoj, Dattatraya
IPC分类号： C07C253/30
CPC分类号： C07C253/30 , C07C255/19
摘要： A novel process for racemization of (R)-3-cyano-5 -methyl hexanoic acid ethyl ester directly to (RS)-3-cyano-5 -methyl hexanoic acid has been developed through a base catalyzed mechanism in a specific solvent system.
摘要翻译：（R）-3-氰基-5-甲基己酸乙酯直接与（RS）-3-氰基-5-甲基己酸外消旋化的新方法已经通过特定溶剂体系中的碱催化机理开发出来。

10. 发明申请

WO2011141805A2 AN IMPROVED PROCESS FOR THE MANUFACTURE OF LAMIVUDINE 审中-公开
标题翻译：改进的制造方法
公开(公告)号：WO2011141805A2
公开(公告)日：2011-11-17
申请号：PCT/IB2011/001013
申请日：2011-05-12
申请人： LUPIN LIMITED , ROY, Bhairab, Nath , SINGH, Girij, Pal , SHRIVASTAVA, Dhananjai , JADHAV, Harishchandra, Sambhaji , AHER, Umesh, Parashram , DEOKAR, Sharad, Chandrabhan
发明人： ROY, Bhairab, Nath , SINGH, Girij, Pal , SHRIVASTAVA, Dhananjai , JADHAV, Harishchandra, Sambhaji , AHER, Umesh, Parashram , DEOKAR, Sharad, Chandrabhan
IPC分类号： C07D411/04
CPC分类号： C07D411/04
摘要： The present invention relates to an improved process for the Manufacture of Lamivudine. A process for the preparation of essentially enantiomerically pure (-)-[2R, 5S]-4-amino-1-[2- (hydroxymethyl)-1,3-oxathiolan-5-y1]-2(1H)-pyrimidin-2-one of formula (I), from L-menthyl glyoxylate is described. Also provided is a process for preparation of (+)-1- (2R/S-Cis)-4-amino-1-[(2-hydroxymethyl)-1,3-oxathiolan-5-y1]-2(1H)-pyrimidin-2-one of formula (XII), from L-menthyl glyoxylate.
摘要翻译：本发明涉及一种用于制造拉米夫定的改进方法。制备基本上对映体纯的（ - ） - [2R，5S] -4-氨基-1- [2-（羟基甲基）-1,3-氧硫杂环戊烷-5-基] -2（1H） - 嘧啶-2-基描述了式（I）的2-乙酰基-L-薄荷基乙醛酸酯。还提供了制备（+） - 1-（2R / S-顺式）-4-氨基-1 - [（2-羟甲基）-1,3-氧硫杂环戊烷-5-基] -2（1H）（XII）的嘧啶-2-酮，由乙醛酸L-薄荷酯。

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