罗氟司特合成路线图解
摘要
<正>罗氟司特(roflumilast,1)化学名为N-(3,5-二氯吡啶-4-基)-3-环丙甲氧基-4-二氟甲氧基苯甲酰胺,是由德国安达(Altana)公司研发,瑞士奈科明公司(Nycomed Pharma GmbH)完成Ⅲ期临床试验的磷酸二酯酶4(PDE4)抑制剂,于2010年7月在欧洲获得批准,随后在德国、英国和西班牙上市,商品名为Daxas。2011年3月又获得美国FDA批准,在美国上市。该药是十多年来首个
引文
[1]钟永刚,陈国华,李昂,等.罗氟司特的合成[J].中国医药工业杂志,2011,42(12):884-886.
[2]AMARI G,ARMANI E,GHIDINI E.Derivatives of1-phenyl-2-pyridynyl alkylene alcohols as phosphodiesterase inhibitors:WO,2008006509[P].2008-01-17.
[3]LOHRAY B B,LOHRAY V B,DAVE M G.Preparation of roflumilast and its analogs:IN,2004MU00478[P].2007-10-12.
[4]GAVHANE S B,WAKADE S M,KADAM S M.Novel process for the preparation of 3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide:WO,2012147098[P].2012-11-01.
[5]王一茜,戚太林,刘威加.一种罗氟斯特原料及中间体的制备方法:中国,102532011[P].2012-01-05.
[6]WILLIAMS E L,WU T C.Process for production of fluoroalkoxy-substituted benzamides and their intermediates:WO,2004033430[P].2004-04-22.
[7]廖明毅,李瑞,杨少宁,等.3-环丙基甲氧基-4-二氟甲氧基苯甲酸的合成新方法:中国,102093194[P].2011-06-15.
[8]严洁,黄欣.高生物利用度的罗氟司特化合物:中国,102351787[P].2012-02-15.
[9]BOSE P,SACHDEVA Y P,RATHORE R S,et al.Process foe the preparation of roflumilast:WO,2005026095[P].2005-03-24.
[10]丁克,朱克明,肖广常.一种制备罗氟司特的方法:中国,102336704[P].2012-02-01.
[11]AMSCHLER H,RADOLFZELL.Fluoroalkoxy-substituted benzamides and their use as cyclic nucleotide phosphodiesterase inhibitors:US,5712298[P].1998-06-27.
[12]田广辉,王治升,陈基,等.制备罗氟斯特的方法及中间体:中国,102775345[P].2012-11-14.
[13]剧仑,邹江,杨琰,等.一种制备罗氟司特的方法:中国,102336703[P].2012-02-01.
[14]KOHL B,MUELLER B,PALOSCH W.Novel process for the preparation of roflumilast:WO,2004080967[P].2004-09-23.
[15]王颖,闫革新,李泽林.一种制备N-(3,5-二氯吡啶-4-基)-3-环丙基甲氧基-4-二氟甲氧基苯甲酰胺的方法:中国,102336705[P].2012-02-01.
[16]刘立刚,李瑞文,王猛,等.一种制备罗氟斯特的方法及其中间体:中国,102276522[P].2011-12-14.
[2]AMARI G,ARMANI E,GHIDINI E.Derivatives of1-phenyl-2-pyridynyl alkylene alcohols as phosphodiesterase inhibitors:WO,2008006509[P].2008-01-17.
[3]LOHRAY B B,LOHRAY V B,DAVE M G.Preparation of roflumilast and its analogs:IN,2004MU00478[P].2007-10-12.
[4]GAVHANE S B,WAKADE S M,KADAM S M.Novel process for the preparation of 3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide:WO,2012147098[P].2012-11-01.
[5]王一茜,戚太林,刘威加.一种罗氟斯特原料及中间体的制备方法:中国,102532011[P].2012-01-05.
[6]WILLIAMS E L,WU T C.Process for production of fluoroalkoxy-substituted benzamides and their intermediates:WO,2004033430[P].2004-04-22.
[7]廖明毅,李瑞,杨少宁,等.3-环丙基甲氧基-4-二氟甲氧基苯甲酸的合成新方法:中国,102093194[P].2011-06-15.
[8]严洁,黄欣.高生物利用度的罗氟司特化合物:中国,102351787[P].2012-02-15.
[9]BOSE P,SACHDEVA Y P,RATHORE R S,et al.Process foe the preparation of roflumilast:WO,2005026095[P].2005-03-24.
[10]丁克,朱克明,肖广常.一种制备罗氟司特的方法:中国,102336704[P].2012-02-01.
[11]AMSCHLER H,RADOLFZELL.Fluoroalkoxy-substituted benzamides and their use as cyclic nucleotide phosphodiesterase inhibitors:US,5712298[P].1998-06-27.
[12]田广辉,王治升,陈基,等.制备罗氟斯特的方法及中间体:中国,102775345[P].2012-11-14.
[13]剧仑,邹江,杨琰,等.一种制备罗氟司特的方法:中国,102336703[P].2012-02-01.
[14]KOHL B,MUELLER B,PALOSCH W.Novel process for the preparation of roflumilast:WO,2004080967[P].2004-09-23.
[15]王颖,闫革新,李泽林.一种制备N-(3,5-二氯吡啶-4-基)-3-环丙基甲氧基-4-二氟甲氧基苯甲酰胺的方法:中国,102336705[P].2012-02-01.
[16]刘立刚,李瑞文,王猛,等.一种制备罗氟斯特的方法及其中间体:中国,102276522[P].2011-12-14.