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。

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。