Construction of pyrrole- and indole-fused CF3-piperazine derivatives

Article abstract of DOI:10.1016/j.jfluchem.2019.109361

A series of pyrrole- and indole-fused trifluoromethyl-functionalized piperazine derivatives were constructed in moderate to good yields with excellent chemoselectivities via a Pictet-Spengler reaction under mild and operationally simple conditions. The synthetic utility of this protocol was further extended by the facile preparation of indole-fused CF₃-1,4-diazocane and enantioenriched CF₃-piperazines via a vinylogous Pictet-Spengler reaction and an asymmetric Pictet-Spengler reaction, respectively.