作者:Chuangchuang Xu、Wenlai Xie、Jiaxi Xu
DOI:10.1039/d0ob00317d
日期:——
arylhydrazine hydrochlorides and Fischer indolization. The organic base triethylamine plays a crucial role in the final elimination step in the Fischer indole synthesis, affording 3-arylindoles regiospecifically. The reaction features advantages of microwave acceleration, non-metal participation, short reaction time, organic acid-base co-catalysis, and broad substrate scope.
已经开发了一种方便的,无金属的,有机酸碱促进的合成方法,该方法可从3-芳基环氧乙烷-2-甲腈和芳基肼盐酸盐制备3-芳基吲哚。在反应中,有机酸催化芳基环氧乙烷甲腈和芳基肼盐酸盐的串联亲核开环反应和费歇尔吲哚化反应。有机碱三乙胺在Fischer吲哚合成的最后消除步骤中起着至关重要的作用,可以区域特异性地提供3-芳基吲哚。该反应具有微波加速,无金属参与,反应时间短,有机酸碱共催化,底物范围宽等优点。