Iridium-Catalyzed Cascade Reaction of Sulfoxonium Ylides with o-Aminoaryl Aldehydes for the Synthesis of 2-Acylindoles

Graphical The synthesis of 2-acylindoles from sulfoxonium ylides with o-aminoaryl aldehydes via iridium-catalyzed N−H insertion and intramolecular condensation has been demonstrated. 2-Acylindoles possess widespread applications in functional chemicals. However, the convenient and selective synthesis of such important substructures has to date remained a challenge. Herein, a method to achieve 2-acylindoles from sulfoxonium ylides with o-aminoaryl aldehydes catalysed by Iridium has been developed with the merits of broad substrate scope, good functional tolerance, high efficiency and operational simplicity, which provides an alternative way to access functionalized indoles.