报道了5-芳香二酮-1H-四氮唑(2)的一锅合成法,并且首次报道了1-甲基-1-甲氧基乙基作为四氮唑氮原子的保护基团,保护与脱保护反应条件温和,操作简便,收率高,为该类化合物的合成提供了一条捷径.采用该方法共合成6个未见文献报道的5-芳香二酮-1H-四氮唑类新化合物,以用于药理活性筛选.
One-pot reaction was reported for the synthesis of 5-aryl diketo-1H-tetrazols(2).Meanwhile,1-methyl-1-methoxyethyl(MME) as protective group of tetrazole was firstly reported.The protective and deprotective reactions were performed in moderate conditions and the new method leads to simplified process and increased productivity.Six novel 5-aryl diketo-1H-tetrazol compounds were synthesized by using this method for further biological screening.