Copper-Catalyzed Monofluoroalkylation of Allyl Phosphates with Nucleophilic Ethyl 2-Fluoro-2-(trimethylsilyl)acetate

J Org Chem. 2023 Jun 2;88(11):7469-7476. doi: 10.1021/acs.joc.3c00064. Epub 2023 May 11.

Abstract

An efficient method for C(sp3)-CHF bond formation was successfully developed by copper-catalyzed cross-coupling of allyl phosphate with 2-fluoro-2-(trimethylsilyl)acetate. Under moderate circumstances, the conversion was carried out in a good strategic range to provide a series of monofluoroalkylation products in high yields, which also demonstrates the practicality of gram-scale reactions.