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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
引用本文: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,2012,31(8):1543-1546.
作者姓名:刘明明  钟东威  周家毅  周璐  叶德泳
作者单位:复旦大学药学院药物化学教研室 上海201203
摘    要: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.

关 键 词:5-芳香二酮-1H-四氮唑  1-甲基-1-甲氧基乙基  四氮唑保护  一锅合成

One-Pot Synthesis of 5-Aryl Diketo-1H-tetrazol Using 1-Methyl-1-methoxyethyl as Protective Group
Liu Mingming , Zhong Dongwei , Zhou Jiayi , Zhou Lu , Ye Deyong.One-Pot Synthesis of 5-Aryl Diketo-1H-tetrazol Using 1-Methyl-1-methoxyethyl as Protective Group[J].Chinese Journal of Organic Chemistry,2012,31(8):1543-1546.
Authors:Liu Mingming  Zhong Dongwei  Zhou Jiayi  Zhou Lu  Ye Deyong
Institution:Liu,Mingming Zhong,Dongwei Zhou,Jiayi Zhou,Lu Ye,Deyong(Department of Medicinal Chemistry,School of Pharmacy,Fudan University,Shanghai 201203)
Abstract: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.
Keywords:5-aryl diketo-1H-tetrazol  1-methyl-1-methoxyethyl(MME)  tetrazole protection  one-pot synthesis
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