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1. 发明申请

US20130303780A1 PROCESS FOR THE PREPARATION OF 2-ARYLTHIAZOLE DERIVATIVES 审中-公开
标题翻译：制备2-芳基噻唑衍生物的方法
公开(公告)号：US20130303780A1
公开(公告)日：2013-11-14
申请号：US13883843
申请日：2011-11-03
申请人： Siva Rama Prasad Vellanki , Arabinda Sahu , Satyanarayana Raavi , Ravi Nuchu , Ramesh Dandala
发明人： Siva Rama Prasad Vellanki , Arabinda Sahu , Satyanarayana Raavi , Ravi Nuchu , Ramesh Dandala
IPC分类号： C07D277/56
CPC分类号： C07D277/56
摘要： The present invention relates an improved process for the preparation of 2-arylthiazole derivatives which are intermediates of Febuxostat and further conversion to Febuxostat or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及一种制备2-芳基噻唑衍生物的改进方法，它是非焦ost素的中间体，并进一步转化成非索非泮或其药学上可接受的盐。

2. 发明授权

US08703980B2 Process for the preparation of darunavir 有权
标题翻译：制备地瑞那韦的方法
公开(公告)号：US08703980B2
公开(公告)日：2014-04-22
申请号：US13496642
申请日：2010-09-16
申请人： Siva Rama Prasad Vellanki , Arabinda Sahu , Aravind Kumar Katukuri , Vikram Vanama , Satishbabu Kothari , Venkata Suryanarayana Ponnekanti , Debashish Datta
发明人： Siva Rama Prasad Vellanki , Arabinda Sahu , Aravind Kumar Katukuri , Vikram Vanama , Satishbabu Kothari , Venkata Suryanarayana Ponnekanti , Debashish Datta
IPC分类号： C07D493/04 , A61P31/12 , A61P31/18
CPC分类号： C07D493/04
摘要： A process for the preparation of Darunavir comprises the reacting of 4-amino-N-(2R, 3S) (3-amino-2-hydroxy-4-phenylbutyl)-N-isobutyl-benzenesulfonamide with (3R, 3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol derivative in N-methyl-2-pyrrolidinone and isolating the resulting Darunavir. The process yields Darunavir with a very low level of the difuranyl impurity.
摘要翻译：制备达鲁那韦的方法包括4-氨基-N-（2R，3S）（3-氨基-2-羟基-4-苯基丁基）-N-异丁基 - 苯磺酰胺与（3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-醇衍生物在N-甲基-2-吡咯烷酮中分离并分离得到的达鲁那韦。该方法产生具有非常低水平的二氟烷基杂质的达鲁那韦。

3. 发明申请

US20130005969A1 PROCESS FOR THE PREPARATION OF TENOFOVIR DISOPROXIL FUMARATE 有权
标题翻译：制备天竺葵异黄酮的方法
公开(公告)号：US20130005969A1
公开(公告)日：2013-01-03
申请号：US13583951
申请日：2011-03-11
申请人： Debashish Datta , Siva Rama Prasad Vellanki , Arabinda Sahu , Raja Babu Balusu , Mastan Rao Ravi , Hari Babu Nandipati , Shankar Rama , Lakshmana Rao Vadali , Srikanth Sarat Chandra Gorantla , Srinivasa Rao Dasari , Nagaraju Mittapelly
发明人： Debashish Datta , Siva Rama Prasad Vellanki , Arabinda Sahu , Raja Babu Balusu , Mastan Rao Ravi , Hari Babu Nandipati , Shankar Rama , Lakshmana Rao Vadali , Srikanth Sarat Chandra Gorantla , Srinivasa Rao Dasari , Nagaraju Mittapelly
IPC分类号： C07F9/6561
CPC分类号： C07F9/65616
摘要： The present invention relates to an improved process for the preparation of Tenofovir Disoproxil and its pharmaceutically acceptable salts comprising the steps of: a) esterifying Tenofovir with chloromethyl isopropyl carbonate in presence of a base, phase transfer catalyst and optionally dehydrating agent, in a suitable solvent; b) optionally purifying Tenofovir Disoproxil; and c) converting of Tenofovir Disoproxil into its pharmaceutically acceptable salts. The present invention further relates to a process for the preparation of Tenofovir by reacting 1-(6-amino-purin-9-yl)-propan-2-ol with toluene-4-sulfonic acid diethoxy phosphoryl methyl ester in presence of a base in a non-polar solvent medium followed by hydrolysis.
摘要翻译：本发明涉及一种用于制备替诺福韦替泊芬及其药学上可接受的盐的改进方法，其包括以下步骤：a）在碱，相转移催化剂和任选的脱水剂存在下，在合适的溶剂中酯化替诺福韦与氯甲基异丙基碳酸酯 ; b）任选地净化替诺福韦酯; 和c）将替诺福韦酯替代物转化为其药学上可接受的盐。本发明还涉及通过使1-（6-氨基 - 嘌呤-9-基） - 丙-2-醇与甲苯-4-磺酸二乙氧基磷酰基甲基酯在碱的存在下反应制备替诺福韦的方法在非极性溶剂介质中进行水解。

4. 发明申请

US20120251826A1 PROCESS FOR THE PREPARATION OF DARUNAVIR 有权
标题翻译：制备DARUNAVIR的方法
公开(公告)号：US20120251826A1
公开(公告)日：2012-10-04
申请号：US13496642
申请日：2010-09-16
申请人： Siva Rama Prasad Vellanki , Arabinda Sahu , Aravind Kumar Katukuri , Vikram Vanama , Satishbabu Kothari , Venkata Suryanarayana Ponnekanti , Debashish Datta
发明人： Siva Rama Prasad Vellanki , Arabinda Sahu , Aravind Kumar Katukuri , Vikram Vanama , Satishbabu Kothari , Venkata Suryanarayana Ponnekanti , Debashish Datta
IPC分类号： C07D493/04
CPC分类号： C07D493/04
摘要： A process for the preparation of Darunavir comprises the reacting of 4-amino-N-(2R,3S) (3-amino-2-hydroxy-4-phenylbutyl)-N-isobutyl-benzenesulfonamide with (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol derivative in N-methyl-2-pyrrolidinone and isolating the resulting Darunavir. The process yields Darunavir with a very low level of the difuranyl impurity.
摘要翻译：制备达鲁那韦的方法包括4-氨基-N-（2R，3S）（3-氨基-2-羟基-4-苯基丁基）-N-异丁基 - 苯磺酰胺与（3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-醇衍生物在N-甲基-2-吡咯烷酮中分离并分离得到的达鲁那韦。该方法产生具有非常低水平的二氟烷基杂质的达鲁那韦。

5. 发明授权

US08759515B2 Process for the preparation of tenofovir disoproxil fumarate 有权
标题翻译：制备替诺福韦地索他米尔富马酸盐的方法
公开(公告)号：US08759515B2
公开(公告)日：2014-06-24
申请号：US13583951
申请日：2011-03-11
申请人： Debashish Datta , Siva Rama Prasad Vellanki , Arabinda Sahu , Raja Babu Balusu , Mastan Rao Ravi , Hari Babu Nandipati , Shankar Rama , Lakshmana Rao Vadali , Srikanth Sarat Chandra Gorantla , Srinivasa Rao Dasari , Nagaraju Mittapelly
发明人： Debashish Datta , Siva Rama Prasad Vellanki , Arabinda Sahu , Raja Babu Balusu , Mastan Rao Ravi , Hari Babu Nandipati , Shankar Rama , Lakshmana Rao Vadali , Srikanth Sarat Chandra Gorantla , Srinivasa Rao Dasari , Nagaraju Mittapelly
IPC分类号： C07F9/40 , C07D473/34
CPC分类号： C07F9/65616
摘要： The present invention relates to an improved process for the preparation of Tenofovir Disoproxil and its pharmaceutically acceptable salts comprising the steps of: a) esterifying Tenofovir with chloromethyl isopropyl carbonate in presence of a base, phase transfer catalyst and optionally dehydrating agent, in a suitable solvent; b) optionally purifying Tenofovir Disoproxil; and c) converting of Tenofovir Disoproxil into its pharmaceutically acceptable salts. The present invention further relates to a process for the preparation of Tenofovir by reacting 1-(6-amino-purin-9-yl)-propan-2-ol with toluene-4-sulfonic acid diethoxy phosphoryl methyl ester in presence of a base in a non-polar solvent medium followed by hydrolysis.
摘要翻译：本发明涉及一种用于制备替诺福韦替泊芬及其药学上可接受的盐的改进方法，其包括以下步骤：a）在碱，相转移催化剂和任选的脱水剂存在下，在合适的溶剂中酯化替诺福韦与氯甲基异丙基碳酸酯 ; b）任选地净化替诺福韦酯; 和c）将替诺福韦酯替代物转化为其药学上可接受的盐。本发明还涉及通过使1-（6-氨基 - 嘌呤-9-基） - 丙-2-醇与甲苯-4-磺酸二乙氧基磷酰基甲基酯在碱的存在下反应制备替诺福韦的方法在非极性溶剂介质中进行水解。

6. 发明申请

US20130244297A1 PROCESS FOR THE PREPARATION OF (3R, 3AS, 6AR)-HEXAHYDROFURO [2, 3- B] FURAN-3-OL 有权
标题翻译：（3R，3AS，6AR） - 六氢呋喃[2,3-b]呋喃-3-醇的制备方法
公开(公告)号：US20130244297A1
公开(公告)日：2013-09-19
申请号：US13989166
申请日：2011-07-14
申请人： Siva Rama Prasad Vellenki , Arabinda Sahu , Nitin Ashok Shimpi , Anil Ponnuru , Satish Babu Kothari
发明人： Siva Rama Prasad Vellenki , Arabinda Sahu , Nitin Ashok Shimpi , Anil Ponnuru , Satish Babu Kothari
IPC分类号： C07D493/04 , C07D307/20
CPC分类号： C07D493/04 , C07D307/20
摘要： The present invention relates to a novel process for the preparation of (3R, 3aS, 6aR)-hexahydrofuro[2, 3-b]furan-3-ol of formula I by reacting a compound of formula VII with the compound of formula R2-OH in the presence of haloginating agent to obtain a compound of formula VI and treating a compound of formula VI with dehaloginating agent to obtain a compound of formula V by reducing a compound of formula V, followed by cylization to obtain compound of formula IV and separating the enantiomer and diastereomers from compound of formula IV to yield a compound of formula I. Compound of formula I is useful as an intermediate in the preparation of protease inhibitors, in particular broad spectrum HIV protease inhibitors, the present invention also relates to process for the preparation of Darunavir from (3R, 3aS, 6aR)-hexahydrofuro[2, 3-b]furan-3-ol.
摘要翻译：本发明涉及通过使式Ⅶ化合物与式R 2 -R 3化合物反应制备式（ⅩⅢa，6aR） - 六氢呋喃并[2,3-b]呋喃-3-醇的新方法， OH，得到式Ⅵ化合物，并用脱卤剂处理式Ⅵ化合物，通过还原式Ⅴ化合物，得到式Ⅴ化合物，然后进行环化，得到式Ⅳ化合物和分离来自式IV化合物的对映异构体和非对映异构体，得到式I化合物。式I化合物可用作制备蛋白酶抑制剂，特别是广谱HIV蛋白酶抑制剂的中间体，本发明还涉及（3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-醇制备达鲁那韦。

7. 发明授权

US08350030B2 Process for producing 5-fluoro-1-(2R, 5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine 有权
标题翻译： 5-氟-1-（2R，5S） - [2-（羟甲基）-1,3-氧硫杂环戊烷-5-基]胞嘧啶的制备方法
公开(公告)号：US08350030B2
公开(公告)日：2013-01-08
申请号：US12746739
申请日：2008-12-05
申请人： Om Dutt Tyagi , Umamaheswar Vasireddy Rao , Vellanki Sivarama Prasad , Arabinda Sahu
发明人： Om Dutt Tyagi , Umamaheswar Vasireddy Rao , Vellanki Sivarama Prasad , Arabinda Sahu
IPC分类号： C07D411/04
CPC分类号： C07D411/04
摘要： Disclosed herein an improved process for producing 5-Fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine and its pharmaceutical acceptable salts.
摘要翻译：本文公开了5-氟-1-（2R，5S） - [2-（羟甲基）-1,3-氧硫杂环戊烷-5-基]胞嘧啶及其药学上可接受的盐的改进方法。

8. 发明授权

US08841467B2 Process for the preparation of (3R, 3aS, 6aR)-hexahydrofuro [2, 3-b] furan-3-ol 有权
标题翻译：制备（3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-醇的方法
公开(公告)号：US08841467B2
公开(公告)日：2014-09-23
申请号：US13989166
申请日：2011-07-14
申请人： Siva Rama Prasad Vellenki , Arabinda Sahu , Nitin Ashok Shimpi , Anil Ponnuru , Satish Babu Kothari
发明人： Siva Rama Prasad Vellenki , Arabinda Sahu , Nitin Ashok Shimpi , Anil Ponnuru , Satish Babu Kothari
IPC分类号： C07D493/04 , C07D307/20
CPC分类号： C07D493/04 , C07D307/20
摘要： The present invention relates to a novel process for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol of formula I by reacting a compound of formula VII with the compound of formula R2-OH in the presence of haloginating agent to obtain a compound of formula VI and treating a compound of formula VI with dehaloginating agent to obtain a compound of formula V by reducing a compound of formula V, followed by cylization to obtain compound of formula IV and separating the enantiomer and diastereomers from compound of formula IV to yield a compound of formula I. Compound of formula I is useful as an intermediate in the preparation of protease inhibitors, in particular broad spectrum HIV protease inhibitors, the present invention also relates to process for the preparation of Darunavir from (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol.
摘要翻译：本发明涉及通过使式Ⅶ化合物与式R 2的化合物反应来制备式（Ⅸ）的（3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-醇的新方法， OH，得到式Ⅵ化合物，并用脱卤剂处理式Ⅵ化合物，通过还原式Ⅴ化合物，得到式Ⅴ化合物，然后进行环化，得到式Ⅳ化合物和分离来自式IV化合物的对映异构体和非对映异构体，得到式I化合物。式I化合物可用作制备蛋白酶抑制剂，特别是广谱HIV蛋白酶抑制剂的中间体，本发明还涉及（3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-醇制备达鲁那韦。

9. 发明申请

US20100256372A1 PROCESS FOR PRODUCING 5-FLUORO-1-(2R, 5S)-[2-(HYDROXYMETHYL)-1,3-OXATHIOLAN-5-YL]CYTOSINE 有权
标题翻译：生产5-氟-1-（2R，5S） - [2-（羟甲基）-1,3-氧硫杂环戊烷-5-基]胞嘧啶的方法
公开(公告)号：US20100256372A1
公开(公告)日：2010-10-07
申请号：US12746739
申请日：2008-12-05
申请人： Om Dutt Tyagi , Umamaheswar Vasireddy Rao , Vellanki Sivarama Prasad , Arabinda Sahu
发明人： Om Dutt Tyagi , Umamaheswar Vasireddy Rao , Vellanki Sivarama Prasad , Arabinda Sahu
IPC分类号： C07D411/04
CPC分类号： C07D411/04
摘要： Disclosed herein an improved process for producing 5-Fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine and its pharmaceutical acceptable salts.
摘要翻译：本文公开了5-氟-1-（2R，5S） - [2-（羟甲基）-1,3-氧硫杂环戊烷-5-基]胞嘧啶及其药学上可接受的盐的改进方法。

10. 发明申请

US20070244318A1 Process for the Preparation of Levofloxacin Hemihydrate 审中-公开
标题翻译：左氧氟沙星半水合物的制备方法
公开(公告)号：US20070244318A1
公开(公告)日：2007-10-18
申请号：US10578078
申请日：2004-08-11
申请人： Davuluri Rao , Shiprakash Dwivedi , Pamujula Sreenivasulu , Arabinda Sahu , Ganala Trinadhachari , Surapaneni Sasi Kiran
发明人： Davuluri Rao , Shiprakash Dwivedi , Pamujula Sreenivasulu , Arabinda Sahu , Ganala Trinadhachari , Surapaneni Sasi Kiran
IPC分类号： C07D491/14
CPC分类号： C07D498/06
摘要： The present invention relates to an improved process for preparation of Levofloxacin hemihydrate having single individual impurity not more than 0.1% and free from particulate matter & from the other enantiomer (R-form) which comprises dissolving levofloxacin technical grade in aqueous alkaline solution, treating the resulting solution with activated carbon at room temperature, removing the undissolved particulate matter filtration, bringing the pH of the aqueous alkaline levofloxacin solution to neutral using dilute mineral acid, removing the precipitated particulate matter by filtration, acidifying the resulting solution, treating the acidified solution with activated carbon at room temperature, filtering the undissolved particulate matter by filtration, neutralizing the acidic solution, filtering again to remove any particulate matter present and, extracting the resulting product with chlorinated solvent and concentrating under vacuum using aqueous tetrahydrofuran or in admixture with other organic solvents to get highly pure levofloxacin hemihydrate having single individual impurity is less than 0.1% and free from particulate matter & from the other enantiomer (R-form).
摘要翻译：本发明涉及一种制备具有不大于0.1％单个杂质且不含颗粒物质的另一种对映异构体（R-型）的左氧氟沙星半水合物的改进方法，其包括将左氧氟沙星工业级溶解在碱性水溶液中，在室温下生成活性炭溶液，除去未溶解的颗粒物过滤，使用稀无机酸使碱性左氧氟沙星水溶液的pH变为中性，通过过滤除去沉淀的颗粒物质，酸化所得溶液，用酸活性炭，通过过滤过滤未溶解的颗粒物质，中和酸性溶液，再次过滤除去存在的任何颗粒物质，并用氯化溶剂萃取所得产物，并在真空下浓缩，使用四氢呋喃水溶液或混合物其他有机溶剂得到具有单一杂质的高纯度左氧氟沙星半水合物小于0.1％，不含颗粒物质和另一种对映异构体（R-型）。

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