一种3,4-二氢嘧啶-2(1H)-酮衍生物四唑的合成

Synthesis of Tetrazole-Complex Based on Biginelli 3,4-Dihydropyrimidin-2(1H)-one Derivatives

意大利化学家Biginelli首次利用芳香醛、乙酰乙酸乙酯和尿素三组分通过“一锅煮法”合成得到3,4-二氢嘧啶-2(1H)-酮,此类化合物具有良好的药物活性。四唑结构在药物化学中可代替羧酸基团在代谢中起稳定作用。作者以对氰基苯甲醛作为原料,将氰基基团引入Biginelli衍生物中,在水中合成该衍生物的四唑化合物,并通过红外、质谱、核磁、X射线单晶衍射加以表征。

Biginelli developed the one-pot synthesis loith aromatic aldehyde,urea and ethyl acetoacetate to obtain 3,4-dihydropyimidin-2(1H)-ones which have good drug activity.The tetrazoles can replace the carboxylic acid group in pharmaceutical chemistry to play a stabilizing rold in the metabolic process.The Biginelli derivative with cyanogroup was obtained from p-cyanobenzaldehyde as raw materials,and the tetrazole compound from it was synthetized in water.Then the tetrazole compounds was characterized by IR,MS,NMR and X-ray diffraction.