N-氨基酰基甲脒类化合物的合成研究

Synthesis of N-Aminoacyl Formamidines

以N-取代脲和甲酰胺为原料,合成了一系列N-氨基酰基甲脒类化合物,讨论了活化剂、溶剂、反应温度及底物投料比对反应的影响。结果表明,以草酰氯为活化剂、二氯甲烷为溶剂,在n(N-取代脲)∶n(甲酰胺)∶n(草酰氯)为1.0∶1.5∶1.2时,室温反应1~4 h可得到产率高达98%的目标化合物。该方法具有底物范围广、操作简便、反应条件温和、反应时间短、产率高等优点。

Using N-substituted ureas and formamides as raw materials,we synthesized a series of N-aminoacyl formamidines.Moreover,we investigated the effects of activating reagent,solvent,reaction temperature,and reactant molar ratio on the reaction.The results show that the target compound with the yield of 98%is obtained at room temperature for 1~4 h under the optimum conditions as follows:using oxalyl chloride as the activating reagent,and dichloromethane as the solvent,the molar ratio of N-substituted urea,formamide,and oxalyl chloride is 1.0∶1.5∶1.2.This method has the advantages of wide range of substrates,simple operation,mild reaction conditions,short reaction time,and high yield.