Microwave-assisted synthesis of 1-aryl-1H-indazoles via one-pot two-step Cu-catalyzed intramolecular N-arylation of arylhydrazones |
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Authors: | Chittari Pabba Hong-Jun Wang Susan R Mulligan Zhen-Jia Chen Todd M Stark Brian T Gregg |
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Institution: | Department of Medicinal Chemistry, Albany Molecular Research, Inc., PO Box 15098, 21 Corporate Circle, Albany, NY 12212-5098, USA |
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Abstract: | A highly efficient one-pot two-step microwave procedure was developed for the synthesis of 1-aryl-1H-indazoles. Microwave heating of 2-halobenzaldehydes or 2-haloacetophenones with phenylhydrazines at 160 °C for 10 min quantitatively yielded the arylhydrazones, which were further cyclized to give 1-aryl-1H-indazoles via CuI/diamine-catalyzed N-arylation under microwave heating (160 °C, 10 min). Good to excellent yields were observed for 2-iodo, 2-bromo, and 2-chloro benzaldehydes or acetophenones. |
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Keywords: | 1H-Indazole Hydrazone Copper Cyclization Arylation Microwave irradiation |
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