专利号:US-5126456-A 优先权日:1991-10-17 标题:7-chloroquinaldine synthesis 发明人:SONG ZHIGUO; HUGHES DAVID L 权利人:MERCK & CO INC 摘要:An improved process is described which utilizes tetrachloro-1,4(or 1,2)-quinone as an oxidant in the Doebner-Miller synthesis of 7-chloroquinaldine, a starting material in the preparation of leukotriene antagonists. The process improves yield and eliminates the need of forming a ZnCl 2 complex to isolate the end product.
专利号:WO-2011121091-A1 优先权日:2010-03-31 标题:Efficient synthesis for the preparation of montelukast and novel crystalline form of intermediates therein 发明人:KIDEMET DAVOR; BOGDAN STEFANE; KLJAJIC ALEN; BENKIC PRIMOZ; STROPNIK TADEJ; PLAPER IGOR 权利人:KRKA D D NOVO MESTO; KIDEMET DAVOR; BOGDAN STEFANE; KLJAJIC ALEN; BENKIC PRIMOZ; STROPNIK TADEJ; PLAPER IGOR 摘要:The present invention describes the improved process for the preparation of montelukast acid (VII) and its pharmaceutically acceptable salts and esters using a novel synthesis step. The process is cost effective, environment friendly, and easily scale up to commercial level and leads to products having high chemical and optical purity. Moreover, the present invention provides a novel crystalline intermediate (IV) that is useful in this process and a method for its production. In a further aspect, the process of the present invention includes a step of removing ketone by-products be derivatization.
专利号:US-2009099367-A1 优先权日:2006-03-06 标题 :Process for preparing a leukotriene antagonist 发明人:BESSA BELLMUNT JORDI; RAFECAS JANE LLORENC; PASTO AGUILA MIREIA; VERDAGUER ESPAULELLA XAVIER; GORDO CAMPON ESTHER 权利人:FARMAPROJECTS S A 摘要:Process for preparing montelukast or a pharmaceutically acceptable salt thereof, especially its sodium salt, that comprises the condensation of an aldehyde and 7-chloro-2-methylquinoline. Moreover, novel intermediates useful for the synthesis of montelukast are described as well as their preparation.
专利号:HU-P0401607-A2 优先权日:2004-08-10 标题 :Synthesis of aminoquinoline derivatives and of their starting materials
专利号:CN-116514711-A 优先权日:2023-04-28 标题:A new process for the synthesis of key intermediates of montelukast sodium