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:EP-2287154-A1 优先权日:2009-07-14 标题 :Efficient synthesis for the preparation of montelukast 发明人:KIDEMET DAVOR; BENKIC PRIMOZ; KLJAJIC ALEN; STEFANE BOGDAN 权利人:KRKA D D NOVO MESTO 摘要:The present invention describes the improved process for the preparation of montelukast acid and its pharmaceutically acceptable salts and esters. The process is cost effective, environment friendly, and easily scale up to commercial level.
专利号:WO-2008035086-A2 优先权日:2006-09-22 标题:Synthesis of leukotriene compounds
专利号:CN-102633683-B 优先权日:2012-04-06 标 题:Synthesis method of 1-hydroxymethyl cyclopropylacetonitrile