Synthesis of tetra-substituted pyrazoles |
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| Authors: | Anne J. Rüger Martin Nieger Stefan Bräse |
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| Affiliation: | 1. Karlsruhe Institute of Technology (KIT), Institute for Organic Chemistry, Fritz-Haber-Weg 6, 76131 Karlsruhe, Germany;2. Department of Chemistry, Laboratory of Inorganic Chemistry, P.O. Box 55, FIN-00014 University of Helsinki, Finland |
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| Abstract: | A set of highly substituted pyrazoles bearing different functional groups on the pyrazole core was developed. Employing a suitable protecting group strategy we could regioselectively introduce various substituents in position 1, 3 and 4 of the pyrazole. This enabled the synthesis of various derivatives of a pyrazole–biscarboxamide with insecticidal activity. During the optimization process we focused on the precise exchange of carboxamide as well as other functional groups based on the concept of bioisosterism. |
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