Recent Advances in the Multicomponent Reactions of Indoles

Abstract Indoles, which are distinguished by their nitrogen‐containing heterocyclic structure, play a pivotal role in organic chemistry due to their diverse biological profiles and unique chemical reactivity. In particular, poly‐substituted indoles are extensively found in a wide range of natural products, pharmaceuticals, materials, and bioactive compounds. The integration of indoles into multicomponent reactions (MCRs) has emerged as a powerful synthetic strategy, facilitating the construction of these complex poly‐substituted indole frameworks from simple precursors. This review highlights the latest advancements in MCRs involving indoles, focusing on innovative methodologies for site‐selective synthesis of indole derivatives, catalytic systems, mechanistic insights, and their applications. The review encompasses significant developments from 2014 to 2024 and covers a variety of indole MCRs, including those targeting the C3 position, dual‐site reactions at the C2 and C3 positions, and reactions involving the pyrrole and benzene rings of the indole scaffold.