异脲盐法合成胍及其N-取代嘧啶胺衍生物的研究

Synthesis of Guanidines and N-Substituted-4-( 3-pyridinyl)-2-pyrimidinamines by O-Methylisourea Sulfate

采用异脲盐法合成一系列N-取代胍和N-取代-4-(3-吡啶基)嘧啶-2-胺类化合物。以O-甲基异脲硫酸盐为起始原料,与脂肪胺类或芳香胺类化合物反应合成脂肪胍或芳香胍类化合物(1),再以3-乙酰吡啶和N,N-二甲基甲酰胺二甲基缩醛(DMF-DMA)为原料反应合成3-(二甲基氨基)-1-(3-吡啶基)-2-丙烯-1-酮(2),将化合物(1)和(2)在碱性条件下反应,最终得到目标产物N-取代-4-(3-吡啶基)嘧啶-2-胺(3)。合成出了6个N-取代胍及其相应的衍生物N-取代-4-(3-吡啶基)嘧啶-2-胺类化合物,并用1H NMR,IR和元素分析表征了目标产物的结构。该方法路线简捷环保、原料廉价易得、反应条件较温和。

To synthesize several N-Substituted guanidines and N-Substituted-d-（ 3-pyridinyl ）-2-pyrimidi- namines by O-Methylisourea Sulfate. O-methylisourea sulfate reacted with aliphatic amine or aromatic amine to give aliphatic guanidine sulfate or aromatic guanidine sulfate （1）. 3-（dimethylamino）-1-（3-pyridinyl）-2-pro- pen-l-one （2） was synthesized by 3-acetylpyridine with DMF-DMA. Compound （1） reacted with compound （2） under the alkaline condition to get N-Substituted-4- （3-pyridinyl） -2-pyrimidinamines （ 3 ）. Six N-Substi- tuted guanidines and their derivatives N-Substituted-4-（3-pyridinyl）-2-pyrimidinamines were synthesized, and the structure of the compounds was characterized by 1H NMR, IR and elementary analysis. The route of this method is simple with milder reaction conditions, raw materials of the reaction are easily got and inexpensive.