Copper-Catalyzed Trifunctionalization of Alkynes: One-Pot Assembly of Antifungal
Zhi-Jie Kang1, Ben-Jun Han1, Yuan-Qi Li1
1School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China.
Abstract:
A copper-catalyzed, three-component tandem reaction for the synthesis of benzofuro[3,2-d]pyrimidine-containing fused heterocycles has been developed. This one-pot protocol efficiently couples terminal alkynes, salicylaldehydes, and α-aminoazoles through a sequential process involving A3 coupling and an intermolecular oxidative 1,2-difunctionalization of the alkyne. This strategy represents a rare example of alkyne trifunctionalization for the construction of polycyclic aromatic heterocycles. Notably, several synthesized derivatives exhibit promising antifungal activity against plant pathogenic fungi.
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