Catalytic Asymmetric Friedel–Crafts/Protonation of Nitroalkenes and <i>N</i>-Heteroaromatics

The catalytic asymmetric Friedel–Crafts/protonation of indoles and pyrroles with α-substituted nitroalkenes to give the corresponding adducts in a highly anti-selective manner was achieved by an imidazoline–aminophenol (L2)–Cu complex. The anti-adducts could be successfully transformed to biochemically important α-substituted β-heteroarylalkylamines.采用咪唑啉-氨基酚（imidazoline–aminophenol，L2）-铜配合物作为催化剂，实现了吲哚类与吡咯类化合物和α-取代硝基烯烃之间的不对称傅-克（Friedel–Crafts）/质子化反应，以高反式选择性得到相应加合物。所得反式加合物可进一步转化为具有重要生化价值的α-取代β-杂芳基烷基胺。