公开(公告)号：EP1907391A1

公开(公告)日：2008-04-09

申请号：EP05779794.6

申请日：2005-07-26

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, bandi ,  RATHNAKAR REDDY, kura, Hetero Drugs Limited (R&D) ,  RAJI REDDY, rapolu, Hetero Drugs Limited (R&D) ,  MURALIDHARA REDDY, d., Hetero Drugs Limited (R&D)

IPC分类号： C07D473/34

CPC分类号： C07D473/34

摘要： The present invention provides a novel process for the preparation of acyclic phosphonate nucleotide analogs using novel intermediates. Thus, for example, (R)-9-(2-phosphonomethoxypropyl)adenine is reacted with dimethylformamide dimethylacetal to give N4-dimethylaminomethyledino-9-(2-phosphonomethoxy ethyl) adenine, which is then reacted with chloromethyl-2-propyl carbonate in presence of triethylamine to give (R)-N4-Dimethylaminomethyledino-9-(2-phosphono methoxypropyl) adenine disoproxil, followed by deprotection with acetic acid to get tenofovir disoproxil. Tenofovir disoproxil is then treated with fumaric acid to give tenofovir disoproxil fumarate.

摘要翻译： 本发明提供了一种使用新型中间体制备无环膦酸酯核苷酸类似物的新方法。 因此，例如，（R）-9-（2-膦酰基甲氧基丙基）腺嘌呤与二甲基甲酰胺二甲基乙缩醛反应，得到N4-二甲基氨基甲基氨基-9-（2-膦酰基甲氧基乙基）腺嘌呤，然后与氯甲基-2-丙基碳酸酯 得到（R）-N4-二甲基氨基甲基亚氨基-9-（2-膦酰基甲氧基丙基）腺嘌呤二吡咯，然后用乙酸脱保护得到替诺福韦二吡呋酯。 随后用富马酸处理替诺福韦二吡呋酯以产生替诺福韦二异丙酯富马酸盐。

公开(公告)号：EP1899356A1

公开(公告)日：2008-03-19

申请号：EP05760572.7

申请日：2005-06-15

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura, Hetero Drugs Limited (R&D) ,  RAJI REDDY, Rapolu, Hetero Drugs Limited (R&D) ,  MURALIDHARA REDDY, Dasari, Hetero Drugs Ltd. R&D ,  MURALI, Nagabelli, HETERO DRUGS LIMITED

IPC分类号： C07D501/22

CPC分类号： C07D501/00

摘要： The present invention provides an improved process for the preparation of high assayed cefdinir. Thus, crude cefdinir is added to water at 25 - 30°C and then 18% hydrochloric acid is slowly added to form a clear solution. The solution is cooled to -5°C and stirred for 5 minutes at -5°C to +5°C. Then temperature of the mass is raised to 35 - 38°C, stirred for 15 minutes at the same temperature. To the reaction mass eno carbon is added at 35 - 38°C and stirred for 30 minutes at 35 - 38°C. Then the contents are filtered on hiflo bed and washed with water. The filtrate is then cooled to 25°C, the pH is slowly adjusted to 2.6 with saturated sodium bicarbonate solution and stirred for 60 minutes at 25 - 30°C. Filtered the solid, washed with water and dried at 40°C under vacuum to give high assayed cefdinir.

公开(公告)号：EP1891037A1

公开(公告)日：2008-02-27

申请号：EP05761003.2

申请日：2005-06-15

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI, Reddy Bandi ,  RATHNAKAR, Reddy Kura, Hetero Drugs Limited (R&D) ,  RAJI, Reddy Rapolu, Hetero Drugs Limited (R&D) ,  MURALIDHARA, Reddy Dasari, Hetero Drugs Ltd (R&D)

IPC分类号： C07D401/04

CPC分类号： C07D471/04

摘要： The present invention provides a novel process for the preparation of gemifloxacin and its pharmaceutically acceptable acid addition salts in high yield. The present invention also relates to novel polymorphs of gemifloxacin free base and its hydrates to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention also relates to infusion solutions of gemifloxacin and to processes for their preparation. Thus, 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphth- yridine-3-carboxylic acid is reacted with a mixture of acetic anhydride, acetic acid and boric acid to give borane compound, which is then treated with 4-Aminomethyl-3-methoxyimino-pyrrolidinium dimethanesulfonate in presence of triethylamine, followed by treatment with 3.5% sodium hydroxide solution to give gemifloxacin free base.

公开(公告)号：EP1885683A2

公开(公告)日：2008-02-13

申请号：EP05760585.9

申请日：2005-06-03

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, Bandi Hetero House ,  RATHNAKAR REDDY, Kura Hetero Drugs Limited (R & D) ,  RAJI REDDY, Rapolu, Hetero Drugs Limited (R & D) ,  MURALIDHARA REDDY, Dasari Hetero Drugs Ltd (R & D) ,  SAMBI REDDY, Jonnala, Hetero Drugs Limited

IPC分类号： C07C209/52

CPC分类号： C07C209/52 ,  C07C2602/10 ,  C07C211/42

摘要： The present invention relates to a process for highly stereoselective synthesis of sertraline and sertraline intermediate. Thus, the mixture of 4-(3,4-Dichlorophenyl)-3,4-dihydro-N-methyl-1(2H)-naphthalenimine, 5 % Pd/CaCO3, water and methanol is taken in a hydrogenation flask and then subjected to hydrogenation under a hydrogen pressure of 0.5 Kg at 20 - 35°C for 3 hours 30 minutes. The catalyst is removed by filtration and the solvent is evaporated completely under vacuum to obtain cis-(±)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-naphthalen amine. (trans-(±): 0.2).

摘要翻译： 本发明涉及一种高立体选择性合成舍曲林和舍曲林中间体的方法。 因此，4-（3,4-二氯苯基）-3,4-二氢-N-甲基-1（2H） - 萘亚胺，5％Pd / CaCO 3 3，水和甲醇的混合物为 置于氢化烧瓶中，然后在氢气压力为0.5Kg，20-35℃下氢化3小时30分钟。 通过过滤除去催化剂，真空蒸发溶剂，得到顺式 - （±）-4-（3,4-二氯苯基）-1,2,3,4-四氢-N-甲基 - 萘胺。 （反 - （±）：0.2）。

公开(公告)号：EP1863822A1

公开(公告)日：2007-12-12

申请号：EP05732994.8

申请日：2005-03-29

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, Bandi ,  RAJI, Reddy, Rapolu, Hetero Drugs Ltd. (R & D) ,  RATHNAKAR, Reddy Kura, Hetero Drugs Ltd. (R & D) ,  MURALI, Nagabelli, Hetero Drugs Ltd. (R & D) ,  MURALIDHARA, Reddy, Dasari

IPC分类号： C07D501/06

CPC分类号： C07D501/00

摘要： There is provided an improved process for preparing cefixime. Thus, for example, 7-amino-3-vinyl-3-cephem-4-carboxylic acid is reacted with 2-mercapto-1,3-benzothiazolyl-(Z)-2-(2-aminothiazol-4-yl)-2-(methoxycarbonyl)-methoxyimino acetate in tetrahydrofuran and water at 4°C in the presence of triethylamine. The reaction mass is extracted with ethyl acetate. 7-[2-(2-Amino-4-thiazolyl)-2-(methoxycarbonylmethoxyimino)acetamido]-3-vinyl-3-cephem-4-carboxylic acid triethylamine salt present in the aqueous layer is hydrolyzed with sodium hydroxide in less than 30 minutes and aqueous hydrochloric acid is added immediately to adjust the pH to 4.8 to 5.2. Then, aqueous hydrochloric acid is added at 35°C to adjust the pH 2.5 and cooled to crystallize cefixime trihydrate in high purity.

公开(公告)号：EP1863788A1

公开(公告)日：2007-12-12

申请号：EP05742906.0

申请日：2005-04-01

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura, ,  RAJI REDDY, Rapolu, ,  MURALIDHARA REDDY, D., ,  SUBASH CHANDER REDDY, K.,

IPC分类号： C07D401/00 ,  A61K31/445

CPC分类号： C07D401/14

摘要： The present invention relates to a novel crystalline form of rupatadine free base, process for its preparation and to a pharmaceutical composition containing it. In accordance with the present invention rupatadine is suspended in n-hexane, n-heptane, cyclohexane, diethyl ether or diisopropyl ether, stirred for at least 1 hour, filtered the solid and dried to give crystalline rupatadine form-B. The isolation of novel rupatadine free base as crystalline form-B may be useful as a purification of rupatadine or a salt thereof.

公开(公告)号：EP1809638A1

公开(公告)日：2007-07-25

申请号：EP04806740.9

申请日：2004-11-01

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, K., Hetero Drugs Limited (R & D) ,  RAJI REDDY, R., Hetero Drugs Limited (R & D) ,  MURALIDHARA REDDY, D., Hetero Drugs Limited R & D ,  MURALI, Nagabelli, Hetero Drugs Limited

IPC分类号： C07D501/04 ,  C07D501/22

CPC分类号： C07D501/22 ,  C07F7/188

摘要： The present invention relates to a process for preparing a key intermediate of cefprozil and use of this intermediate in the preparation of cefprozil thereby avoiding impurity-causing self-acylation. [R-(Z)]-[4-hydroxy-α-[(3-methoxy-l-methyl-3-oxo-1-propenyl)amino]] benzeneacetic acid, mono potassium salt is reacted with ethyl chloroformate to obtain mixed anhydride which is then silylated with N,O-bis(trimethylsilyl)acetamide. The silylated compound obtained is reacted with [7-trimethylsilylamino-3-(Z/E-propen-1-yl)-3-cephem-4-carboxylic acid]trimethylsilyl ester and deprotected with aqueous hydrochloric acid to give cefprozil.

公开(公告)号：EP1776354A1

公开(公告)日：2007-04-25

申请号：EP04770686.6

申请日：2004-08-11

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, bandi Hetero House ,  RATHNAKAR REDDY, kura Hetero Drugs Limited (R & D) ,  RAJI REDDY, rapolu Hetero Drugs Limited (R & D) ,  MURALIDHARA REDDY, dasari Hetero Drugs Limited ,  SRINIVAS REDDY, itiyala Hetero House

IPC分类号： C07D311/58

CPC分类号： C07D311/58

摘要： The present invention relates to a process for separation of desired diastereomeric pair from a mixture of diastereomeric pairs thereby obtaining nebivolol intermediates. Thus, the mixture of (+)-[1S*(R*)]-6-fluoro-3,4-dihydro-α-[[(phenylmethyl)amino]methyl]-2H-1-benzopyran-2-methanol, (+)-[1S*(S*)]-6-fluoro-3,4-dihydro-2-oxiranyl-2H-1-benzopyran and ethanol is heated to reflux temperature and stirred for 8 hours at the same temperature to obtain (+)-[2R*[1S*,5S*(S*)]]+[2R*[1S*,5R*(R*)]]-α,α'-[phenylmethyliminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol]. Then the reaction mass is cooled to 10ºC, the pH is adjusted to 2 with HCl gas and stirred for 45 minutes at 25ºC to 30ºC. Then the separated solid is filtered and dried to give (+)-[2R*[1S*,5S*(S*)]]-α,α'-[phenylmethyliminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2- methanol] hydrochloride salt, which can be converted into nebivolol.

公开(公告)号：EP1687287A1

公开(公告)日：2006-08-09

申请号：EP03773997.6

申请日：2003-11-24

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, B., Hetero House ,  RATHNAKAR REDDY, K., Hetero Drugs Limited (R & D) ,  RAJI REDDY, R., Hetero Drugs Limited (R & D) ,  MURALIDHARA REDDY, D., Hetero Drugs Limited (R&D) ,  SUBASH CHANDER REDDY, K., Hetero Drugs Ltd. (R&D)

IPC分类号： C07D291/04

CPC分类号： C07D205/08 ,  C07D263/22 ,  C07D263/26 ,  C07D277/34 ,  C07D277/36

摘要： The invention provides a process for preparing intermediate of ezetimibe, which shows hypocholesterolemic activity. Thus 3-[5-(4-fluorophenyl)-1,5-dioxopentyl]-4-phenyl-2-oxazolidinone is reduced with (-)-DIP chloride to obtain 3-[(5S)-5-(4-fluorophenyl)-5-hydroxy-1-oxopentyl]-4-phenyl-2-oxazolidinone.

公开(公告)号：EP2162444B1

公开(公告)日：2014-06-04

申请号：EP07827518.7

申请日：2007-07-11

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura ,  RAJI REDDY, Rapolu ,  MURALIDHARA REDDY, Dasari ,  SRINIVASA RAO, Thungathurthy

IPC分类号： C07D239/94

CPC分类号： C07D239/94