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Published on: November 30, 2022
Enantioselective Copper-Catalyzed Synthesis of Trifluoromethyl-Cyclopropylboronates
Julia Altarejos1,2,3, David Sucunza1,2,3, Juan J Vaquero1,2,3
1Universidad de Alcalá, Departamento de Química Orgánica y Química Inorgánica,, Alcalá de Henares 28805, Spain.
Abstract:
A copper-catalyzed enantioselective cyclopropanation involving trifluorodiazoethane in the presence of alkenyl boronates has been developed. This transformation enables the preparation of 2-substituted-3-(trifluoromethyl)cyclopropylboronates with high levels of stereocontrol. The products are valuable synthetic intermediates by transformation of the boronate group. This methodology can be applied to the synthesis of novel trifluoromethylated analogues of trans-2-arylcyclopropylamines, which are prevalent motifs in biologically active compounds.
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