Double Synthon Alkyne Trifunctionalization

One-step β-diketone synthesis

Leveraging bimolecular reduction of CO2 to supply both carbonyl and methyl synthons, this method enables the first trifunctionalization of alkynes to efficiently construct β-diketone-containing bioactive heterocycles.

Xiong, Wenfang · Tan, Xiaobin · Liu, Hongjian · Zhu, Baiyao · Zhao, Jinwu · Li, Jianxiao · Qi, Chaorong · Jiang, Huanfeng

Science China Chemistry 2023

Advantages

First Pd-catalyzed trifunctionalization of alkynes with aryl iodides

One-step construction of β-diketone-containing pyrimidines, oxazoles, pyrazoles with important biological activity