An Approach to 1,1-Disubstituted Pyrazolylcyclopropane Building Blocks

Abstract

An approach to isomeric 1,1-disubstituted pyrazolylcyclopropanes that relies on lithium diisopropylamide (LDA) mediated bis-alkylation­ of the corresponding pyrazolylacetonitriles is developed. The building blocks obtained can be considered as lead-like bioisosteres of arylpyrazole and pyrazolecarboxamide moieties and are thus useful for early drug discovery projects.

Key words

cyclopropanes - pyrazoles - hetarylacetonitriles - nucleophilic substitution - lead-oriented synthesis

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