Tianjin Key Laboratory for Modern Drug Delivery & High-Efficiency, School of Pharmaceutical Science and Technology , Tianjin University , Tianjin 300072 , China.
Collaborative Innovation Center of Chemical Science and Engineering (Tianjin) , Tianjin 300072 , China.
Org Lett. 2018 Sep 21;20(18):5933-5937. doi: 10.1021/acs.orglett.8b02614. Epub 2018 Sep 13.
A series of biologically relevant compounds of benzothieno[3,2- b]indole derivatives were conveniently synthesized from reactions of N-protected 2-((2-bromophenyl)ethynyl)anilines and potassium ethylxanthate, mediated by cuprous bromide/ tert-butyl hydroperoxide. The method features the construction of the pyrrole and thiophene rings in a cascade sequence with the pyrrole ring being formed prior to the thiophene ring via a possible reactive Cu(III)-pyrrole intermediate.
方便地从 N-保护的 2-((2-溴苯基)乙炔基)苯胺和乙基黄原酸钾的反应中,通过溴化亚铜/叔丁基过氧化物的介导,合成了一系列具有生物相关性的苯并噻吩[3,2-b]吲哚衍生物。该方法的特点是通过可能的反应性 Cu(III)-吡咯中间体,以级联序列构建吡咯环和噻吩环,首先形成吡咯环,然后再形成噻吩环。