期刊文献+

盐酸多奈哌齐的合成研究 被引量:4

Study on synthesis of donepezil hydrochloride
在线阅读 下载PDF
导出
摘要 以5,6-二甲氧基-1-茚酮为原料,经缩合、催化氢化、N-苄基化、成盐反应得到目标化合物,总收率达到75.9%,产品结构经IR、1HNMR、MS确证。该路线原料价廉易得、反应条件温和、危险性小、收率较高,适合于工业化生产。 Donepezil hydrochloride was synthesized from 5,6-dimethoxy-1-indanone via condensation,catalytic hydrogenation,N-benzylation and salification,with the overall product yield reaching 75.9%.The structure of the compound was identified by IR,1HNMR and MS spectroscopy.This synthetic route featuring lower production cost,less hazard,mild reaction conditions and high yield is worthy of a commercial scale manufacture.
出处 《化学试剂》 CAS CSCD 北大核心 2011年第2期175-176,共2页 Chemical Reagents
关键词 盐酸多奈哌齐的合成研究 donepezil 5,6-dimethoxy-1-indanone synthesis
  • 相关文献

参考文献7

  • 1程勇,宋友华,傅得兴.新一代治疗阿尔茨海默病的胆碱酯酶抑制剂多奈哌齐[J].中国新药杂志,2000,9(5):300-303. 被引量:17
  • 2邹士宗.阿尔茨海默病的药物治疗[J].中国煤炭工业医学杂志,2007,10(5):497-499. 被引量:3
  • 3LENSKY S. Process for the preparation of benzyl-piperidylmethyl-indanones : US ,5 606 064 [ P]. 1997-02-25.
  • 4IIMURA Y. Process for production of donepezil derivative : US ,6 252 081 [ P ]. 2001-06-26.
  • 5GUTMAN A L, SHKOLNIK E, TISHIN B, et al. Process and intermediates for production of donepezil and related compounds : US, 6 492 522 [ P ]. 2002-12-10.
  • 6LERMAN O, KASPI J, ARAD O, et al. Proeess for the preparation of donepezil : US,6 844 440 [ P 1. 2005-01-18.
  • 7REDDY M S,ESWARAIAH S,THIPPANNACHAR M V, et al. Process for preparation of donepezil:US,7 148 354 [ P]. 2006-12-12.

二级参考文献37

共引文献18

同被引文献21

  • 1何兵明,邱友春,陈捷,张福利.盐酸多奈哌齐的合成[J].中国医药工业杂志,2005,36(11):657-659. 被引量:8
  • 2SUGIMOTO H, TSUCHIYA Y, HIGURASHI K, et al. Cyclic amine compounds with activity against ace- tylcholinesterase :US ,4895841 [ P ]. 1990 - 01 - 23.
  • 3ILMURA Y. Process for production of donepezil de- rivative: US,6252081 [ P ]. 2001 - 06 - 26.
  • 4LENSKY S. Process for the preparation of benzyl-pi- peridylmethyl-indanones: US, 5606064 [ P ]. 1997 - 02 - 25.
  • 5RAO R, RAO A, MURTHY Y. Efficient and indus- trially viable synthesis of donepezil[ J]. Synth Com- mun,2007,37 ( 17 ) :2847 - 2853.
  • 6梁国辉,贺清凯.多奈哌齐合成新工艺:中国,1733728[P].2006-02-15.
  • 7DEVRIES K. Processes and intermediates for prepar- ing 1-benzyl-4 [ ( 5, 6-dimethoxy-1-indonon ) -2-yl ] methylpiperidine: WO,97/22584 [ P ]. 1997 - 06 - 26.
  • 8GUTMAN A, SHKOLNIK E, TISHIN B, et al. Novel process and intermediates for production of donepezil and related compounds : WO, 00/09483 [ P ]. 2000 - 02 - 24.
  • 9GUTMAN A,SHKOLNIK E,TISHIN B,et al. Process and intermediates for production of donepezil and re- lated compounds: US,6492522[ P ]. 2002 - 12 - 10.
  • 10Ramon C. Donepezil in Alzheimer' s disease: from conventional trials to phamacogenetics[J]. Neuropsychiatr Disease and Treat- ment,2007,3(3) :303-333.

引证文献4

二级引证文献3

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