A practical, two-step synthesis of 1-alkyl-4-aminopyrazoles |
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Authors: | Anna A. Zabierek |
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Affiliation: | Department of Drug Design and Optimization, Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA |
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Abstract: | A novel synthesis of N1 alkyl-substituted pyrazoles with a free amino group at the C4 position is described. Commercially available 4-nitropyrazole was found to readily undergo Mitsunobu reactions with primary and secondary alcohols. Subsequent reduction of the nitro group via hydrogenation affords 1-alkyl-4-aminopyrazoles, which are valuable intermediates in the synthesis of pharmaceutically active compounds. |
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Keywords: | 1-Alkyl-4-aminopyrazoles Mitsunobu reaction |
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