Iodine‐Catalyzed Tandem Cyclization for Efficient Synthesis of Quinazolinones from Indoles and Amines

Abstract In this study, we report an iodine‐catalyzed multicomponent reaction of indoles, glyoxylic acid or DMSO, and aliphatic amines to synthesize quinazolinone derivatives via oxygenation cleavage of the C=C double bonds of indoles. This method features mild conditions, high efficiency, and excellent functional group tolerance. The practicality of this approach is demonstrated through its application in synthesizing rutaecarpine and a scalable protocol for efficient quinazolinone production.