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Novel and efficient synthesis of triazolobenzodiazepine analogues through the sequential Ugi 4CR-click-N-arylation reactions
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2019-01-07 , DOI: 10.1016/j.tetlet.2019.01.009
Mohammad Sadegh Asgari , Mehdi Soheilizad , Parviz Rashidi Ranjbar , Bagher Larijani , Rahmatollah Rahimi , Mohammad Mahdavi

An efficient approach for the synthesis of N-alkyl-2-aryl-2-(6-oxo-4H-benzo[f][1,2,3]triazolo[1,5-a][1,4]diazepin-5(6H)-yl)acetamides is described. The protocol involves Ugi four-component reaction of 2-bromobenzoic acid, propargylamine, aldehydes and isocyanides followed by in situ sequential click reaction of azide ion with triple bond and N-arylation reaction to afford desired products in good to excellent yields.



中文翻译:

通过连续的Ugi 4CR- click - N-芳基化反应,新颖高效地合成三唑并二氮杂卓类似物

一种合成N-烷基-2-芳基-2-(6-oxo-4 H-苯并[ f ] [1,2,3]三唑[1,5- a ] [1,4]二氮杂pin的有效方法描述了-5(6 H)-基)乙酰胺。该方案涉及2-溴苯甲酸,炔丙基胺,醛和异氰酸酯的Ugi四组分反应,然后进行叠氮化物离子与三键的原位连续点击反应和N-芳基化反应,从而以良好或优异的收率提供所需的产物。

更新日期:2019-01-07
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