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 quantita- tively,and then followed by the reaction with bromoacetonitrile catalyzed by KI in one-pot furnishing the target compounds under the effect of NaHCO3. The structure were confirmed by IR, ^1HNMR,and MS techniques and elemental analysis.
出处
《化学试剂》
CAS
北大核心
2016年第9期914-916,共3页
Chemical Reagents