摘要
以2-氨基-5-卤代吡啶为原料,与N,N-二甲基甲酰胺二甲基缩醛(DMF-DMA)在DMF中反应,几乎定量得到(E)-N'-(5-卤代吡啶-2-基)-N,N-二甲基甲脒中间体。然后以KI为催化剂,在Na HCO3作用下,于"一锅中"甲脒中间体和溴乙腈发生反应得到标题化合物,总收率为59.2%~73.6%。产物结构通过IR、1HNMR、元素分析和MS进行了表征。
6-Haloimidazo[1,2-a]pyridines-3-carbonitriles were prepared from 2-amino-5-halopyridine via a two-step one-pot process,with the total yield of 59. 2% ~ 73. 6%. Firstly,2-amino-5-halopyridine reacted with N,N-dimethylformamide dimethyl acetyl( DMF-DMA) in DMF to afford( E)-N'-( 5-halopyridin-2-yl)-N,N-dimethylformamidines as intermediates almost quantitatively,and then followed by the reaction with bromoacetonitrile catalyzed by KI in one-pot furnishing the target compounds under the effect of Na HCO3. The structure were confirmed by IR,1HNMR,and MS techniques and elemental analysis.
引文
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