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2-二乙胺基甲基咪唑盐酸盐的合成 被引量:1

Synthesis of 2-(Diethylaminomethyl) Imidazole Hydrochloride
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摘要 以咪唑为原料,经过苯甲酰化、选择性脱酰基、加氢还原、酸水解、还原胺化和成盐等六步化学反应得到2-二乙胺基甲基咪唑盐酸盐,总收率为45%.所得中间体及产物均经核磁共振氢谱和核磁共振碳谱进行结构确证. The paper describes the new method for synthesis of the compound starting from commercially available imidazole, which contains six steps including benzoylation, selective debenzoylation, hydrogenation, acidic hydrolysis, reductive amination and salification. The total yield based on imidazole is over 45 %. The structures of all intermediates and product were confirmed by ^1H and ^13C NMR spectral analysis.
出处 《河南科学》 2011年第10期1172-1174,共3页 Henan Science
基金 国家自然科学基金(81072539)
关键词 2-二乙胺基甲基咪唑盐酸盐 尼唑苯酮 中间体 2-甲酰基咪唑 2-(Diethylaminomethyl)imidazole hydrochloride: nizofenone intermediate: 2-formyl imidazole
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参考文献5

  • 1Michio N,Tetsuo Y,Tomio A,et al. 1-F(2-Chlorobenzoyl)-4-nitrophenyl]-2-(diethylamino- methyl)-imidazole:US, 3915981 [P]. 1975-10-28.
  • 2郑正春,童志杰.尼唑苯酮的合成[J].精细化工中间体,2008,38(1):27-28. 被引量:2
  • 3王钝,全哲明,王硕冰,于飞.2-二乙胺基甲基咪唑的合成[J].中国医药工业杂志,2008,39(10):734-735. 被引量:2
  • 4Bastiaansen L A M, Van Lier P M, Godefroi E F. Imidazole-2-carboxaldehyde[J]. Organic Syntheses, 1981,60: 72-74.
  • 5Martinez J M L, Romasanta P N, Chattah A K, et al. NMR characterization of hydrate and aldehyde forms of imidazole-2-carbo- xaldehyde and eerivatives[J]. Organic Chemistry, 2010, 75: 3208-3213.

二级参考文献7

  • 1Nakanishi, Yokobe M, Arai T, et al. 1-[2-(2-Chlorobenzoyl) -4-nitrophenyl ]-2- (diethylaminomethyl)-imidazole [P]. US : 3 915 981, 1975-10-28.
  • 2Yasuda H. Antianoxic effect in animal models [J ]. Pharmacodyn, 1978, 233: 136.
  • 3Saito I. Multicenter clinical studies[J]. Neurol.res., 1983, 5: 29.
  • 4Ohta T.Multicenterclinicalstudies[J].Neurosurg, 1986, 64: 420.
  • 5Horizoe H. Toxicity studies[J]. Oyo Yakuri, 1985, 30: 627.
  • 6Michio N, Tetsuo Y. 1-[2-(2-Chlorobenzoyl)-4- nitrophenyl] -2- (diethylaminomethyl) imidazole: US, 3915981 [P]. 1975-10-28.
  • 7Bastiaansen LAM,Van Lier PM, Godefroi EF. Imidazole-2- carboxaldehyde [J]. Org Synth, 1981, 60: 72-74.

共引文献1

同被引文献9

  • 1Ochiai C, Asano T, Takakura K, et al. Mechanisms of cerebral protection by pentobarbital and nizofenone correlated with the course of local cerebral bloodflow changes[J]. Strokel, 1982,3:788 -796.
  • 2Yasuda H. Antianoxic effect in animalmodels [J]. Phamacodyn, 1978, 233 : 136.
  • 3Saito I. Multieenterclinical studies[ J]. Neurolres, 1983,5:29.
  • 4OhtaT. Multicenterclinical studies[ J]. Neurolres, 1986,64:430.
  • 5Hoizone H. Toxicity studies [ J ]. Oyo Yakuri, 1985,30:627.
  • 6MichioN,TetsuoY. 1 - [ 2 - ( 2 - chlorbenzoyl ) - 4 - nitrophenyl ] - 2 - (diethylaminomethyl) - imidazole: US, 3915981 [ P]. 1975 - 10 - 28.
  • 7Martinez J M L,Romasanta P N,Chattah A K, et al. NMR characteriza- tion of hydrate and aldehyde forms of imidazole - 2 - carboxaldehyde and eerivative [ J ]. Organic Chemistry, 2010,75 : 3208 - 3213.
  • 8郑正春,童志杰.尼唑苯酮的合成[J].精细化工中间体,2008,38(1):27-28. 被引量:2
  • 9王钝,全哲明,王硕冰,于飞.2-二乙胺基甲基咪唑的合成[J].中国医药工业杂志,2008,39(10):734-735. 被引量:2

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