2-氨基吡啶,丙烯酸乙酯置于咪唑盐酸盐体系中,用 Neat (No Solvent) 用作溶剂,化学反应 5.0H,以33%的收率获得3-(吡啶-2-基氨基)丙酸乙酯 参考文献:氯化咪唑鎓催化迈克尔加成反应保护氨基并构建中环杂环 标题:氯化咪唑鎓催化迈克尔加成反应保护氨基并构建中环杂环 摘要:已经开发出一种有效的氨基保护和七元环构建方法.该方法采用氯化咪唑在低温下进行迈克尔加成反应,在高温下进行氨基脱保护或构建七元环. Doi:10.3390/molecules24234224
专利信息
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:CN-117756712-A 优先权日:2023-12-13 标 题:Synthesis of dabigatran etexilate intermediate and preparation method of impurities
专利号:US-2015246900-A1 优先权日:2012-10-29 标题 :Process for the Synthesis of Dabigatran and Its Intermediates