期刊文献+

4-(4-氨基苯基)-3-吗啉酮的合成

Synthesis of 4-(4-Aminophenyl)-3-Morpholinone
原文传递
导出
摘要 4-(4-氨基苯基)-3-吗啉酮是合成利伐沙班的一个重要中间体,以吗啉酮为原料,利用Buchwald-Hartwig偶联反应制得4-苯基-3-吗啉酮,再经硝化,还原三步反应制备4-(4-氨基苯基)-3-吗啉酮。 4-(4-amino-phenyl)-3-morpholinone as the key mtermecllate in the Syntnesls rivaroxaban, 4-phenyl-3-morpholinone was prepared by. the raw material morpholinone using the Buchwald-Hartwig coupling reaction, and then via nitration,reduction three-step reaction was obtained 4- (4-amino-phenyl) - 3-morpholinone.
出处 《光谱实验室》 CAS 2013年第3期1075-1077,共3页 Chinese Journal of Spectroscopy Laboratory
关键词 4-(4-氨基苯基)-3-吗啉酮 利伐沙班中间体 偶联反应 合成 4-( 4-Amino-Phenyl )-3-Morpholinone Rivaroxaban Intermediates CoupledSynthesis Coupling Reaction Synthesis
  • 相关文献

参考文献10

  • 1Gulseth M, Michaud J, Nutescu EA. Rivaroxaban : an Oral Direct Inhibitor of Factor Xa[J]. Am J Health Pharm. , 2008,45 (16) : 1520-1529. 被引量:1
  • 2刘薇,董金华.利伐沙班[J]. Chiese Journal of Medicinal Chemh'try, 2011,21 ( 6): 508-510. 被引量:1
  • 3Susanne Roehrig, Alexander Straub, Jens Pohlmann. Discovery of the Novel Antithrombotic Agent 5-Chloro-N-( { (5S)-2-oxo-3-[4- (3-oxomorpholin-4-yl) phenyl]-l, 3-oxazolidin-5-yl} thiophene-2-carboxamlde (BAY 59-7939): An Oral, Direct FACTOR Xa Inhibitor[J]. J. Med. Chem, 2005,48(19) : 5900-5908. 被引量:1
  • 4高扬,梁斌,倪国伟,王环,张福利.利伐沙班合成路线图解[J].中国新药杂志,2012,21(4):371-374. 被引量:8
  • 5Rami A,Meha,Akul Y,Desai, Umesh R. Potent Direct Inhibitors of Factor Xa Based on the Tetrahydroisoquinoline Scaffold [J] European ,Journal of Medicblal Chemistry,2012,54(1) :771-783. 被引量:1
  • 6Song Y H, Zhu B Y, Wang S M et al. Beta-aminoacid-derivatives as Factor Xa Inhibitors[P]. WO 2006063113A2,2006-06-15. 被引量:1
  • 7Straub A, Lampe T, Pohlmann J. Substitutes Oxazolidino-nes and Their use in the Field of Blood Coagulation [P]. US 20030153610A1,2003-08-14. 被引量:1
  • 8Sanjay Trehan, Mallesham B, Rajesh B M. Highly Effcient CuI-Catalyzed Coupling of Aryl Bromides with Oxazolidinones Using Buehwalds Protoeol:A Short Route to Linezolid and Toloxatone[J]. Organic Letters, 2003 ,$(7) :963-965. 被引量:1
  • 9Werner W, Peter Ludwig Wendel, Markus Woissyk. Practical and Efficient Processes for the Preparation of 4-(4-aminophenyl) Morpholin-3-ones on a Large.r Scale : Precursor of Factor Xa Inhibitors[J]. Heteroe'ycles, 2007,74 (1) : 437-445. 被引量:1
  • 10Werner W K R. Mederski, Bertram C. Amsterdam C V, Buhring K U, Dorsch D, Gleitz J, Marz J, Tsaklakidis C. Chlorothiophenecarboxamides as P1 surrogates of inhibitors of Blood Coagulation Factor Xa[J]. Bioorganic-Medicinal Chemistry Letters. , 2004,14(23) : 5817-5822. 被引量:1

二级参考文献21

  • 1GULSETH MP, MICHAUD J, NUTESCU EA. Rivaroxaban: an oral direct inhibitor of factor Xa[J]. Am J Health Pharm, 2008, 65(16) : 1520 -1529. 被引量:1
  • 2PERZBORN E, STRASSBURGER J, WILMEN A, et al. In vitro and in vivo studies of the novel antithrombotic agent BAY 59- 7939-an oral, direct factor Xa inhibitor[J]. J Thromb Haemost, 2005, 3(3): 514-521. 被引量:1
  • 3MUECK W, BECKA M, KUBITZA D, et al. Population model of the pharmacokinetics and pharmacodynamics of rivaroxaban-an oral, direct factor Xa inhibitor-in healthy subjects[J]. Int J Clin Pharmacol Ther, 2007, 45 (6) : 335 -344. 被引量:1
  • 4KUBITZA D, BECKA M, WENSING G, et al. Safety, pharmacodynamics, and pharmacokinetics of BAY 59-7939-an oral, direct factor Xa inhibitor-after multiple dosing in healthy male subjects[J]. Eur J Clin Pharmaeol, 2005, 61(12) : 873 -880. 被引量:1
  • 5C 托马斯,M 贝尔韦,A 施特劳布.制备4-(4-氨基苯基)-3-吗啉酮的方法:中国,200480026537.X[P].2006-10-25. 被引量:1
  • 6GLICKMAN SA, EASTON, SCHULTZ HS, et al. Preparation of N-substituted-3-morpholones: US, 3092630[P]. 1963-06-04. 被引量:1
  • 7STRAUB A, LAMPE T, POHLMANN J, et al. Substituted oxazolidinones and their use in the field of blood coagulation : WO, 0147919[P]. 2001 -07 -05. 被引量:1
  • 8DIETER D, WERNER M, CHRISTOST, et al. Phenyl derivatives: WO, 2002057236[P]. 2002-07-25. 被引量:1
  • 9MASSE CE. Substituted oxazolidione derivatives: WO, 2009023233 [P]. 2009 -02 - 19. 被引量:1
  • 10THOMAS C, BERWE M, STRAUB A. Method for the production of 4-(4-amlnophenyl)-3-morpholinone: WO, 2005026135 [P]. 2005-03-24. 被引量:1

共引文献7

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部