De novo Synthesis of Chiral 3,4‐DihydroquinazolinesviaOne‐Pot Enantioselective Ugi‐Azide/Cyclization Sequences†

Abstract

Comprehensive SummaryHerein, we reported a precise de novo synthesis of chiral 3,4‐dihydroquinazoline frameworks via a one‐pot anionic stereogenic‐at‐cobalt(III) complex‐catalyzed enantioselective Ugi‐azide/Pd‐catalyzed cyclization sequence. This powerful protocol involves 5 components and 2 catalytic systems, delivering chiral 3,4‐dihydroquinazolines with excellent enantioselectivities (up to 94% ee). The preliminary antifungal experiments suggest that both Ugi‐adducts and 3,4‐dihydroquinazolines have great potential in inhibiting plant pathogens such as Trichoderma viride and Fusarium graminearum.