Huisgen [3+2]环加成/N-芳基化串联反应合成三氮唑苯二氮卓化合物

Synthesis of Triazolobenzodiazepine Analogs via Sequential Huisgen[3+2]Cycloaddition/N-Arylation Reactions

研究了四氢吡咯并[3,4-c]吡咯-1,3-二酮经N-炔丙基化反应,铜催化的Huisgen[3+2]环加成和N-芳基化串联反应一步法合成三氮唑苯二氮卓化合物的新方法。产物经熔点仪、质谱、1 H NMR和13 C NMR进行了表征。该方法原料易得、操作简单、反应条件温和、产物收率高。

A novel and efficient approach is studied for the synthesis of triazolobenzodiazepine analogs by employing tetrahydropyrrolo[3,4-c]pyrrole-1,3-dione as the substrates,via sequential N-propargylation,Cu-catalyzed Huisgen[3+2]cycloadditon and N-arylation reactions.The desired products have been characterized by melting point,mass spectra,1 H NMR and 13 C NMR.This procedure is conducted under mild reaction condition with simple substrates and easy operation to give corresponding products in high yield.