期刊文献+
任意字段
题名或关键词
题名
关键词
文摘
作者
第一作者
机构
刊名
分类号
参考文献
作者简介
基金资助
栏目信息

2-(1-咪唑基)乙胺的合成 被引量：1

Synthesis of 2-(1-Imidazolyl) ethanamine
下载PDF
导出
摘要 2-（1-咪唑基）乙胺（1）是重要的药物中间体,如具有抑制γ-分泌酶作用的N-烷基磺胺类药物、具有多种药学活性的含氮稠杂环类和具有抗疟作用的Famesyl蛋白转移酶抑制剂都含有该结构片段。 2-（1-Imidazolyl）ethanamine was synthesized from ethyl acrylate by Michael addition with imidazole to give ethyl 3-（1-imidazolyl）propionate,which was subjected to hydrazinolysis,followed by the Curtius rearrangement and hydrolysis with an overall yield of about 72%.
作者 江来恩 邓胜松 李婷婷 姚日生
机构地区 合肥工业大学化学工程学院
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2010年第4期253-254,共2页 Chinese Journal of Pharmaceuticals
关键词 咪唑基 乙胺 合成 药物中间体 磺胺类药物 N-烷基 酶抑制剂 酶作用 2-（1-imidazolyl）ethanamine intermediate synthesis
分类号 O626.23 [理学—有机化学]
  • 相关文献

参考文献10

  • 1Bergstrom CP,Sloan CP,Lau WY,et al.Carbamateappended N-alkylsulfonamides as inhibitors of y-secretase[J].Bioorg Med Chem Lett,2008,18 (2):464-468.
  • 2Priepke H,Pfau R,Gerlach K,et al.Substituted nitrogen-containing heterobicycles,the preparation thereof and their use as pharmaceutical compositions:US,7429597[P].2008-09-30.(CA 2004,141:71557).
  • 3Windsor WT,Weber PC,Strickland CO,et al.Treatment of malaria with farnesyl protein transferase inhibitors:US,6645966[P].2003-11-11.(CA2002,137:125178).
  • 4Popkov SV,Skvortsova MN.A new method for the synthesis of n-(2-aminoethyl) azoles by alkylation of azoles with 2-alkyl-4,5-dihydrooxazoles[J].Russ Chem Bull,2006,55(10):1848-1851.
  • 5Cuadro AM,Matia MP,Garcia JL,et al.Syntheis of N-(aminoethyl) azoles under phase transfer catalysis[J].Synth Commun,1991,21 (4):535-544.
  • 6Xu LW,Li L,Xia CG.Transition-metal-based Lewis acid catalysis of aza-type Michael additions of amines to a,p-unsaturated electrophiles in water[J].Helv Chim Acta,2004,87(6):1522-1526.
  • 7Martin-Aranda RM,Ortega-Cantero E,Rojas-Cervantes ML,et al.Sonocatalysis and basic clays.Michael addition between imidazole and ethyl acrylate[J].Catal Lett,2002,84 (3-4):201-204.
  • 8Yang L,Xu LW,Xia CG.Highly efficient KF/Al_2O_3-catalyzed versatile hetero-Michael addition of nitrogen,oxygen,and sulfur nucleophiles to α,β-ethylenic compounds[J].Tetrahedron Lett,2005,46 (19):3279-3282.
  • 9郭柏淑,张锋明,沈菊英,杨玉社.盐酸奈法唑酮的合成[J].中国医药工业杂志,2003,34(6):265-266. 被引量：2
  • 10陶锋,吕春绪.拉夫替丁的合成[J].中国医药工业杂志,2004,35(7):393-395. 被引量：6

二级参考文献11

  • 1[5] 闻韧.药物合成化学[M].北京:化学工业出版社，1988.278-282.
  • 2[1]Fujirebio TS. Lafutidine [J]. Drugs Future, 1999, 24 (9): 1024-1025.
  • 3[2]Hirakawa N, Kashiwaka H, Matsumoto H, et al. Preparation of N- [ (pyridyloxy) butenyl] - (furfurylthio) acetamides and analogs as ulcer inhibitors [P]. EP: 282077, 1988-09-14. (CA 1990, 112: 20902)
  • 4[3]Hirakawa N, Matsumoto H, Hosoda A, et al. A novel histamine 2 (H2) receptor antagonist with gastroprotective activity.Ⅱ .Synthesis and pharmacological evaluation of 2-furfurylthio and 2-furfurylsulfinyl acetamide derivatives with heteroaromatic rings [J]. Chem Pharm Bull, 1998, 46 (4): 616-622.
  • 5[4]Ishii A, Nishimura Y, Kondo H, et al. Preparation of N[(pyridyloxy) alkyl] - or N- [ (pyridyloxy) alkenyl] -2-(furfurylsulfinyl) acetamides as histamine H2 receptor antagonists [P]. JP: 5059045, 1993-03-09. (CA 1993, 119:139114)
  • 6Davis R, Whittington R, Bryson HM. Nefazodone, a review of its pharmacology and clinical efficacy in the management of major depression [J]. Drugs, 1997,53(4) : 608-636.
  • 7Temple DL, Lobeck WG. 1, 2, 4-Triazol-3-one antidepressants[P]. US: 4487773, 1984-12-11. (CA1985,102 : 166780d).
  • 8Temple DL, Lobeck WG. Phenoxyethyl-1,2,4-triazol-3-one antidepressants [P]. US : 4338317,1982-07-06. (CA 1982,97:182432a).
  • 9Madding GD, Smith DW, Sheldon RI, et al. Synthesis and X-Ray crystal structure of a 2,4,5-trisubstituted 1,2,4-triazolin-3-one [J]. J Heterocycl Chem, 1985,22(4):1121-1126.
  • 10Lei B, Tam TF, Karimian K, et al. Methods for the manufacture of nefazodone[P]. US: 5900485,1999-03-04. (CA 1999,130:311820b).

共引文献6

同被引文献5

引证文献1

二级引证文献1

中国医药工业杂志
2010年 第4期

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