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.
刘明明
,
钟东威
,
周家毅
,
周璐
,
叶德泳
. 以1-甲基-1-甲氧基乙基为保护基的一锅法合成5-芳香二酮-1H-四氮唑[J]. 有机化学, 2012
, 32(08)
: 1543
-1546
.
DOI: 10.6023/cjoc1112111
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.
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