Pd-Catalyzed Four-Component Cascade Cyclization of Alkynols, Aryl Iodides, CO, and Amines

Abstract

Controlling selectivity and reaction pathways in multicomponent reactions for the synthesis of complex molecules from readily available starting materials is an attractive yet challenging goal in synthetic organic chemistry. Herein, we disclose a concise Pd-catalyzed four-component cyclization that enables the modular synthesis of dihydrofuran and pyrazoline scaffolds bearing quaternary carbon centers in high yields. The high-yielding nature, broad substrate scope, and successful late-stage modification of biologically relevant molecules collectively demonstrate the practicality of this method.