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.