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Rapid, microwave accelerated synthesis of [1,2,4]triazolo[3,4-b][1,3,4]oxadiazoles from 4-acylamino-1,2,4-triazoles
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2016-08-17 01:54:18 Stephanie L. Breunig, Margaret E. Olson, Daniel A. Harki
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2016-08-17 01:54:18 Stephanie L. Breunig, Margaret E. Olson, Daniel A. Harki
1,2,4-Triazoles and 1,3,4-oxadiazoles are prevalent moieties in pharmaceutical agents, yet fused [1,2,4]triazolo[3,4-b][1,3,4]oxadiazoles are surprisingly under-represented for both synthesis and biological application. We report a rapid, two-step synthesis of [1,2,4]triazolo[3,4-b][1,3,4]oxadiazoles from commercial 4-amino-1,2,4-triazoles that is highlighted by a microwave accelerated intramolecular cyclization to generate the fused ring system. Our efforts to optimize reaction conditions and elucidate reaction mechanism are also described.
中文翻译:
从4-酰基氨基-1,2,4-三唑快速微波加速合成[1,2,4]三唑[3,4-b] [1,3,4]恶二唑
1,2,4-三唑和1,3,4-恶二唑是药剂中的主要部分,但令人惊讶的是,稠合的[1,2,4]三唑[3,4-b] [1,3,4]恶二唑在-代表用于合成和生物学应用。我们报告了快速,两步合成[1,2,4]三唑[3,4-b] [1,3,4]恶二唑从商业4-氨基-1,2,4-三唑的突出显示微波加速了分子内环化反应以生成稠环系统。还描述了我们优化反应条件和阐明反应机理的努力。
更新日期:2016-08-17
中文翻译:
从4-酰基氨基-1,2,4-三唑快速微波加速合成[1,2,4]三唑[3,4-b] [1,3,4]恶二唑
1,2,4-三唑和1,3,4-恶二唑是药剂中的主要部分,但令人惊讶的是,稠合的[1,2,4]三唑[3,4-b] [1,3,4]恶二唑在-代表用于合成和生物学应用。我们报告了快速,两步合成[1,2,4]三唑[3,4-b] [1,3,4]恶二唑从商业4-氨基-1,2,4-三唑的突出显示微波加速了分子内环化反应以生成稠环系统。还描述了我们优化反应条件和阐明反应机理的努力。