3-取代吲哚甲胺衍生物因其多种生物活性而备受关注.吲哚与N-磺酰醛亚胺的Friedel-Crafts反应是制备3-取代吲哚甲胺衍生物的主要方法,但反应中通常会伴随大量的双吲哚甲烷化合物的生成.应用Cu(OTf)_2和脯氨亚磺酰胺共同催化吲哚与N-磺酰醛亚胺的Friedel-Crafts反应,可以选择性地合成3-取代吲哚甲胺衍生物,产率为65%~93%.该方法具有底物适用性好、反应条件温和、操作简单等优点. The 3-substituted indolylmethylamine derivatives have drawn much attention because of their various biological activities.The Friedel-Crafts reaction of indoles with N-sulfonyl-aldimines is the main method for the preparation of 3-substituted indolylmethylamine derivatives, However, the reaction often accompanied by a large number of bisindole methane compounds.Using Cu (OTf) _2 and prolyl sulfenamide co-catalyzed Friedel-Crafts reaction of indoles and N-sulfonyl aldimines can be selectively Synthesis of 3-substituted indolylmethylamine derivatives, the yield was 65% ~ 93%. This method has the advantages of good substrate, mild reaction conditions, simple operation and so on.