Convergent synthesis of 2,3-bisarylpyrazolones through cyclization of bisacylated pyrazolidines and hydrazines |
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| Authors: | Todd A Brugel Tomas Hudlicky Michael P Clark Mark Sabat Vu Bui Matthew J Laufersweiler Roger G Bookland |
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| Institution: | a Procter and Gamble Pharmaceuticals, Health Care Research Center, 8700 Mason-Montgomery Road, Mason, OH 45040-8006, USA
b Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, USA |
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| Abstract: | Cyclization of various bisacylated hydrazines and pyrazolidines using DBU or sodium hydride leads to the formation of various mono-, bi- and tricyclic pyrazolone scaffolds in 41-98% yield. The convergent nature by which the precyclization intermediates are constructed allows for rapid derivatization about the pyrazolone core. |
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