Abstract

Abstract We developed a novel method for synthesizing fused-tricyclic indole derivatives with a 3-aminomethyl indole motif through a reaction cascade involving ipso -Friedel–Crafts alkylation of phenols, rearomatization of the spirocyclohexadienone unit, and iso -Pictet–Spengler reaction. Using TFA as an acid promoter, six-, seven-, and eight-membered ring-fused indoles were obtained in 31–99% yield.

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