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

Liu, Yaomei; Chen, Rui; Lu, Lishuai; Yin, Dengyu; Yan, Fangpei; Li, Xiao-Xuan; Xiao, Hua; Fan, Shilu*; Feng, Yi-Si*
Science Citation Index Expanded
中国科学院

摘要

An efficient method for C-(sp ( 3 ))-CHF bond formation was successfully developedby copper-catalyzedcross-coupling of allyl phosphate with 2-fluoro-2-(trimethylsilyl)-acetate.Under moderate circumstances, the conversion was carried out in agood strategic range to provide a series of monofluoro-alkylationproducts in high yields, which also demonstrates the practicalityof gram-scale reactions.

关键词

ENANTIOSELECTIVE SYNTHESIS TRIFLUOROMETHYLATION FLUORINE SUBSTITUTION ALKYLATION PALLADIUM DIASTEREO DIFLUOROMETHYLATION PHARMACEUTICALS ALLYLATIONS