4-氯-3-硝基苯甲酸置于甲胺体系中,用 水 作为反应溶剂,以86%的收率获得产物4-甲氨基-3-硝基苯甲酸 参考文献:Novel Compounds And Compositions For Treating Diseases Asociated With Protease Activity 标题:Novel Compounds And Compositions For Treating Diseases Asociated With Protease Activity 摘要:描述了用于预防和治疗由肥大细胞介导的炎症性疾病的新化合物,组合物和方法.这些化合物,组合物和方法对预防和治疗与呼吸道相关的炎症性疾病(如哮喘和过敏性鼻炎)以及其他类型的免疫介导性炎症性疾病(如类风湿关节炎,结膜炎和炎症性肠病,各种皮肤病症以及某些病毒性疾病)有效.这些化合物包括对肥大细胞蛋白酶组胺酶的有效和选择性抑制剂.用于治疗这些疾病的组合物包括口服,吸入,局部和静脉制剂,以及包含这些制剂的装置.
专利号:US-9533971-B2 优先权日:2012-10-29 标 题 :Process for the synthesis of dabigatran and its intermediates 发明人:PULLAGURLA MANIK REDDY; RANGISETTY JAGADEESH BABU; NANDAKUMAR MECHERIL VALSAN 权利人:BIOPHORE INDIA PHARMACEUTICALS PVT LTD; BIOPHORE INDIA PHARMACEUTICALS PVT LTD 摘要:The present invention describes an improved process for the preparation of Dabigatran Etexilate (Formula-VII) or it's pharmaceutically acceptable salt for the treatment of thrombosis, cardiovascular diseases etc. and intermediates involved in the synthesis.
专利号:US-10077251-B2 优先权日:2012-10-29 标题:Process for the synthesis of Dabigatran Etexilate and its intermediates 发明人:PULLAGURLA MANIK REDDY; RANGISETTY JAGADEESH BABU; NANDAKUMAR MECHERIL VALSAN 权利人:BIOPHORE INDIA PHARMACEUTICALS PVT LTD 摘要:The present invention describes an improved process for the preparation of Dabigatran Etexilate (Formula-VII) or it's pharmaceutically acceptable salt for the treatment of thrombosis, cardiovascular diseases etc. and intermediates involved in the synthesis.
专利号:US-9273030-B2 优先权日:2012-04-02 标题 :Process for the preparation of benzimidazole derivatives and salts thereof 发明人:THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; RAGHURAM SURAPARAJU 权利人:MSN LAB PRIVATE LTD 摘要:Provided are novel salts of benzimidazole derivatives, preferably salts of benzimidazole derivatives which are useful intermediates in the synthesis of pure 1-methyl-2-[N-[4-(N-n-hexyloxycarbonylamidino)phenyl]aminomethyl]benzimidazol-5-yl-carboxylicacid-N-(2-pyridyl)-N-(2-ethoxycarbonylethyl)amide and its salts.
专利号:US-9688657-B2 优先权日:2013-03-25 标题:Synthesis of dabigatran 发明人:PATKAR LAXMIKANT NARHARI; MONDKAR HARISH KASHINATH; AROTE NITIN DNYANESHWAR; PATIL SACHIN SHIVAJI; JADHAV TANAJI SHAMRAO; HAGAVANE NITIN NIVRUTTI; BHOPALKAR RAJESH GANPAT 权利人:USV PRIVATE LTD 摘要:The present invention relates to a process for preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof. The present invention relates to novel compounds, in particular Ethyl-3-{[(2-formyl-1-methyl-1H-benzimidazole-5-yl)carbonyl]-(2-pyridinyl) amino}propanoate and Ethyl-3-{[(2-dichloromethyl-1-methyl-1H-benzimidazole-5-yl)carbonyl]-(2-pyridinyl)amino}propanoate and process for preparation thereof. The present invention further relates to the use of these novel compounds in the preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof.
专利号:CA-2907839-A1 优先权日:2013-03-25 标题 :Synthesis of dabigatran
专利号:CN-117756712-A 优先权日:2023-12-13 标 题:Synthesis of dabigatran etexilate intermediate and preparation method of impurities