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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Solid-phase synthesis of 5-substituted amino pyrazoles.

An efficient method for the solid-supported synthesis of 5-N-alkylamino and 5-N-arylamino pyrazoles is described. This method is general and mild and utilizes readily accessible resin-immobilized beta-ketoamides 2 as starting materials for the preparation of 1. Resin-immobilized beta-ketoamide, aryl-, or alkylhydazine and Lawesson's reagent are suspended in a mixture of THF/Py and heated at 50-55 degrees C to give a resin-bound 5-aminopyrazole, that is liberated from the solid support by treatment with TFA.[1]

References

  1. Solid-phase synthesis of 5-substituted amino pyrazoles. Dodd, D.S., Martinez, R.L., Kamau, M., Ruan, Z., Van Kirk, K., Cooper, C.B., Hermsmeier, M.A., Traeger, S.C., Poss, M.A. Journal of combinatorial chemistry. (2005) [Pubmed]
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