CC BY ND NC 4.0 · SynOpen 2017; 01(01): 0084-0090
DOI: 10.1055/s-0036-1588544
paper
Copyright with the author

An Approach to 1,1-Disubstituted Pyrazolylcyclopropane Building Blocks

Pavel S. Nosika, b, Oleksiy S. Artamonova, Sergey V. Ryabukhin*b, Oleksandr O. Grygorenkob
  • aInstitute of Organic Chemistry, National Academy of Sciences of Ukraine, Murmanska Street 5, Kyiv 02660, Ukraine   Email: s.v.ryabukhin@gmail.com
  • bTaras Shevchenko National University of Kyiv, Volodymyrska Street 64, Kyiv 01601, Ukraine
The work was supported by Ukrainian Government Funding (state registry No. 0114U003956) and Life Chemicals Group.
Further Information

Publication History

Received: 03 July 2017

Accepted after revision: 31 July 2017

Publication Date:
14 August 2017 (online)

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.

Supporting Information