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Palladium-Catalyzed Monofluoroalkylation of Aryl Iodides and Aryl Bromides with Nucleophilic Ethyl 2-Fluoro-2-(trimethylsilyl)acetate

Zheng, Kaiting; Liu, Yaomei; Zheng, Chenggong; Yan, Fangpei; Xiao, Hua; Feng, Yi-Si*; Fan, Shilu*
Science Citation Index Expanded
中国科学院

摘要

A palladium-catalyzed monofluoroalkylation of aryl iodides and aryl bromides was developed using nucleophilic ethyl 2-fluoro-2-(trimethylsilyl)acetate as a monofluoroalkyl source. The transformation proceeded with excellent substrate scope to afford a range of monofluoroalkylated products in good yields under mild conditions, and it proved feasible in a gram-scale reaction. This protocol was successfully used in late-stage modification of an estrone derivative, providing a facile route for research on the discovery of biologically active compounds and high-performance materials.

关键词

palladium-catalyzed monofluoroalkylation nucleophilic reagents C-C bonds formation