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Novel strategy for the preparation of 3-perfluoroalkylated-2H-indazole derivatives |
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| Authors: | Hassen Bel Abed Nils Weißing Jens Schoene Jannik Paulus Norbert Sewald Marc Nazaré | |
| Institution: | 1. Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Campus Berlin-Buch, Robert-Roessle-Str. 10, 13125 Berlin, Germany;2. Department of Chemistry, Bielefeld University, P.O. Box 10 01 31, 33501 Bielefeld, Germany;3. Berlin Institute of Health (BIH), Anna-Louisa-Karsch-Str. 2, 10178 Berlin, Germany | |
| Abstract: | A simple and novel methodology for the synthesis of 3-perfluoroalkylated-2H-indazole derivatives has been elaborated. The perfluoroalkylation of readily available 2-nitrobenzaldimines bearing electron donating groups was performed using the Ruppert-Prakash reagent and its analogues to afford α-difluoromethylated, α-trifluoromethylated and α-pentafluoroethylated benzylamines. A final reductive cyclization mediated by SnCl2·2H2O led to 2H-indazoles containing perfluoroalkyl groups via the generation of a new N | |
| Keywords: | Perfluoroalkylation Ruppert-Prakash reagent Reductive cyclization | |
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