Trifluoromethylations of Alkenes Using PhICF3Cl as Bifunctional Reagent
Cong Xu1, Wanqiao Huang2, Ruzhong Zhang2
1National Engineering Laboratory for Druggable Gene and Protein Screening, School of Life Sciences , Northeast Normal University , Changchun 130117 , China.
Abstract:
We described a trifluoromethylation of alkenes using PhICF3Cl as bifunctional reagent. Chlorotrifluoromethylated products were obtained when nonconjugated alkenes were treated with PhICF3Cl in 1,4-dioxane at 60 °C, while vinyl C-H trifluoromethylated products were obtained by further elimination of hydrochloride in the case of those conjugated alkene substrates in DMF. Broad substrate scope, especially including complex alkenes bearing biological active motifs, suggests that this mild reaction is feasible for late-stage modification in drug discovery.
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