专利号:WO-2010146391-A1 优先权日:2009-06-15 标题:Regioselective synthesis of letrozole 发明人:GORE VINAYAK GOVIND; SHUKLA VINAY KUMAR; BHANDARI SHERYAS; HASBE SURESH; MEKDE SANDEEP 权利人:GENERICS UK LTD; MYLAN INDIA PRIVATE LTD; GORE VINAYAK GOVIND; SHUKLA VINAY KUMAR; BHANDARI SHERYAS; HASBE SURESH; MEKDE SANDEEP 摘要:The present invention relates to an improved process for the preparation of letrozole (I) and its pharmaceutically acceptable salts, to compositions comprising letrozole or a pharmaceutically acceptable salt thereof, and to uses of such compositions. In particular it relates to a process and to novel intermediates for preparing letrozole and its salts substantially free from regioisomeric impurities.
专利号:US-7705159-B2 优先权日:2005-07-06 标题:Process for the preparation of letrozole 发明人:MACDONALD PETER LINDSAY; BIGATTI ETTORE; ROSSETTO PIERLUIGI; HAREL ZVI 权利人:SICOR INC 摘要:The invention provides a high-yield process for the preparation of letrozole having a high purity, without the need for removal of the 4-[1-(1,3,4-triazolyl)methyl]benzonitrile impurity at the intermediate stage. The invention also provides a process for the synthesis of letrozole in which formation of the impurity 4-[1-(1,3,4-triazolyl)methyl]benzonitrile during the first stage is minimized. In the process, a 4-(halomethyl)benzonitrile is reacted with a salt of 1H-1,2,4-triazole, reducing the formation of the impurity. Preferably, the preparation is conducted as a one-pot process.
专利号:US-8003804-B2 优先权日:2006-03-17 标题:Synthesis of 4-[1-(4-cyano phenyl)-(1,2,4-triazol-1-yl)methyl] benzonitrile and 4-[1-(1H-1,2,4-triazol-1-yl)methylene benzonitrile intermediate 发明人:PATHI SRINIVAS LAXMINARAYAN; KANKAN RAJENDRA NARAYANRAO; RAO DHARMARAJ RAMACHANDRA; VASANT CHIKHALIKAR SANDIP 权利人:CIPLA LTD 摘要:The present invention relates to a process for the preparation of 4-[1-(4-cyano phenyl)-1-(1,2,4-triazol-1-yl)methyl]benzonitrile (letrozole), substantially free from its isomeric impurity. The preparation involves reaction of 4-[1-(1H-1,2,4-triazol-1-yl)methylene benzonitrile with 4-fluorobenzonitrile in the presence of an organic solvent and a silicon amine. The present invention also relates to a process for the preparation of 4-[1-(1H-1,2,4-triazol-1-yl)methylene benzonitrile which involves: (a) the reaction of a 4-halomethyl benzonitrile with 1,2,4-triazole in the presence of cesium carbonate and an organic solvent to obtain a reaction mass comprising 4-[1-(1,2,4-triazole-1-yl)methyl]benzonitrile of formula II; and (b) precipitation of 4-[1-(1,2,4-triazole-1-yl)methyl]benzonitrile (II) from the reaction mass using a suitable organic solvent.
专利号:WO-2007107733-A1 优先权日:2006-03-17 标 题 :Synthesis of 4-[1-(4-cyano phenyl)-(1,2,4-tr1azol-1-yl)methyl] benzonitrile and 4-[1-(1h-1,2,4-triazol-1-yl)methylene benzonitrile intermediate
专利号:US-2009270633-A1 优先权日:2006-03-17 标题 :Synthesis of 4-[1-(4-cyano phenyl)-(1,2,4-triazol-1-yl)methyl] benzonitrile and 4-[1-(1H-1,2,4-triazol-1-yl)methylene benzonitrile intermediate
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