An Approach to 1,1-Disubstituted Pyrazolylcyclopropane Building Blocks

Abstract

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.

Keywords

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