期刊文献+

盐酸氟西汀的合成 被引量:6

Synthesis of Fluoxetine Hydrochloride
下载PDF
导出
摘要 苯乙酮与甲胺盐酸盐、多聚甲醛进行M ann ich反应生成3-甲胺基-1-苯基丙酮盐酸盐(1);1在甲醇中用硼氢化钾还原制备3-甲胺基-1-苯基丙醇(2);2经醚化、成盐合成了抗抑郁药———盐酸氟西汀(4),总收率41%。4的结构经1H NMR和MS表征。 Fluoxetine hydrochloride(4) in overall yield of 41.0% was synthesized by a four-step reaction in which acetophenone reacted with methylamine hydrochloride and paraformaldehyde to obtain 3-methylaminopropiophenone hydrochloride (1); then 1 was reduced by potassium borohydride i,n methanol to prepare 3-methylamino-1-phenylpropanol(2) ; finally, 2 reacted with 4-chlorobenzo-trif- luoride and formed salt. The structrue of 4 was characterized by ^1H NMR and MS.
出处 《合成化学》 CAS CSCD 2008年第3期354-355,361,共3页 Chinese Journal of Synthetic Chemistry
基金 国家自然科学基金资助项目(20576094)
关键词 MANNICH反应 氟西汀 抗抑郁药 药物合成 Mannich reaction Fluoxetine antidepressant synthesis
  • 相关文献

参考文献13

  • 1Wirth D D, Miller M S, Boini S K, et al. Identification and comparison of impurities in fluoxetine hydrochloride synthesized by seven different routes [ J ]. Org Process Res Dev,2000,4(6) :513 -519.
  • 2Kumar N, Vijayaraghavan B, Ramana K V, et al. Process for the preparation of fluoxetine hydrochloride[P]. US 6 77 485,2004.
  • 3Eva A C, Ference D R, Zsuzsanna A T, et al. Preparation of N-methyl-3-phenyl-3-[ 4-( trifluoromethyl ) phenoxy] propylamine and acid addition salts thereof [P]. WO 9 400 416,1994.
  • 4Takeshi Ohkuma, Dai Ishii, Hiroshi Takeno, et al. Asymmetric hydrogenation of amino ketones using chiral RuCl2(diphophine) ( 1,2-diamine ) Complexes [J]. J Am Chem Soc,2000,122:6510 -6511.
  • 5Alexander Zelenin, San Antonio. Synthesis of 3-aminomethyl-l-propanol, a fluoxetine precursor [ P ]. US 6 846 957 B2,2005.
  • 6Sanyo Chemical Industries, Ltd. Preparation of betaaketo acid[ P]. JP 55 151 532,1980.
  • 7Sorger Klas, Petersen Hermann, Stohrer Jurgen. Enantioseleetive reformatsky process for preparing optically active alcohols, amines and derivatives thereof[ P]. US 6 924 386,2005.
  • 8Koenig T M, Mitchell D. A convenient method for preparing enanfiomerically pure norlluoxetine, fluoxetine and tomoxetine [ J ]. Tetrahedron Letters, 1994,35 (9) : 1339 - 1342.
  • 9Thefiot K J. Preparation and use of 2-methyl-5-phenylisoxazolidine[ P]. US 5 760 243,1998.
  • 10李于善.β-甲胺基苯丙醇的合成研究[J].湖北化工,2000,17(6):14-15. 被引量:8

二级参考文献1

共引文献7

同被引文献35

引证文献6

二级引证文献17

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