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Direct electrophilic N-trifluoromethylation of azoles by a hypervalent iodine reagent |
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| Authors: | Niedermann Katrin Früh Natalja Senn Remo Czarniecki Barbara Verel René Togni Antonio |
| Institution: | Departement Chemie und Angewandte Biowissenschaften, Eidgen?ssische Technische Hochschule (ETH) Zürich, 8093 Zürich (Switzerland) |
| Abstract: | Effective CF(3) transfer: Various electron-rich nitrogen heterocycles (pyrazoles, triazoles, and tetrazoles) can be directly N-trifluoromethylated by a hypervalent iodine reagent in an efficient manner. The optimized procedure, which includes an in situ silylation of the substrate followed by an acid-catalyzed CF(3) transfer, provides ready access to a series of new and previously challenging or inaccessible NCF(3) compounds. |
| Keywords: | electrophilic addition hypervalent compounds nitrogen heterocycles synthetic methods trifluoromethylation |
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