氮杂环并二氢嘧啶及嘧啶衍生物的合成及生物活性评价

Synthesis and Biological Activity of Azaclozodihypyrimidine and Pyrimidine Derivatives

利用微波促进,以芳香醛、乙酰乙酸乙酯、2-氨基咪唑或3-氨基-1,2,4-三唑为原料,通过Knoevenagel缩合反应和Atwal改进的Biginelli反应串联,简便、高效地合成了系列新型芳基取代咪唑(三唑)并二氢嘧啶衍生物.对所合成化合物进一步芳构化,得到系列氮杂环并嘧啶类化合物,为此类嘧啶化合物的合成提供一条简便的途径.对所合成的部分化合物进行了体外肿瘤细胞(Hela和A549)的细胞毒性及苹果树腐烂病菌的抑制活性测试.

A series of novel aryl-substituted imidazo[1,2-a]pyrimidine and triazolo[1,5-a] pyrimidine were synthesized by the tandem reaction of Knoevenagel and Atwal modified Biginelli, following by aromatization. Some of their cytotoxic activities against Hela and A549 cells and inhibition for apple tree canker were preliminarily evaluated.