One‐Pot Multicomponent Synthesis of Indoles from 2‐Iodobenzoic Acid

Abstract

A synergism: The multicomponent assembly of an alkyne, a nucleophile, and a carboxylic acid gave indole derivatives in good yield and high regioselectivity by a one-pot Curtius rearrangement/palladium-catalyzed indolization process (see scheme). A synergistic effect was observed; the by-product of the first reaction served as a reagent for the second step. The first synthesis of indole N-carboxamide derivatives by heteroannulation is also described.