3-Indolyl methanamine derivatives have attracted much attention due to their multiple potent bioactivities. The Friedel-Crafts reaction between indole and N-sulfonylaldimine is a major method for preparation of 3-indolyl methanamine derivatives, however, abundant bisindolyl methane will be formed during the reaction. 3-Indolylmethanamine derivatives were selectively synthesized in 65%~93% yields by the Friedel-Crafts amidoalkylation reaction of indoles and N-sulfonylaldimines utilizing Cu(OTf) 2 and N-sulfinylprolinamide as catalysts. This method exhibited several features such as broad substrate applicability, mild reaction condition and simple operation.
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