An Approach to 1,1-Disubstituted Pyrazolylcyclopropane Building BlocksThe work was supported by Ukrainian Government Funding (state registry No. 0114U003956) and Life Chemicals Group.
Received: 03 July 2017
Accepted after revision: 31 July 2017
14 August 2017 (online)
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.