Regioselective Halogenation of Arenes and Heterocycles in Hexafluoroisopropanol
Ren-Jin Tang, Thierry Milcent and Benoit Crousse*
*Faculty of Pharmacy, UMR 8076, BioCIS, Univ. Paris-Sud-CNRS, Université Paris-Saclay, 92290 Châtenay-Malabry, France, Email: benoit.crousseu-psud.fr
R.-J. Tang, T. Milcent, B. Crousse, J. Org. Chem., 2018, 83, 930-938.
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The use of a hexafluoroisopropanol as solvent enables a mild and regioselective halogenation of a broad range of arenes and heterocycles with N-halosuccinimides in good yields. In addition, the versatility of the method is demonstrated by the development of one-pot sequential dihalogenation and halogenation-Suzuki cross-coupling reactions.
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Halogenation-Suzuki cross-coupling reactions