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CC BY-ND-NC 4.0 · SynOpen 2017; 01(01): 0084-0090
DOI: 10.1055/s-0036-1588544
DOI: 10.1055/s-0036-1588544
paper
An Approach to 1,1-Disubstituted Pyrazolylcyclopropane Building Blocks
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)
![](https://www.thieme-connect.de/media/10.1055-s-00032269/201701/lookinside/thumbnails/so-2017-d0029-op_10-1055_s-0036-1588544-1.jpg)
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 synthesisSupporting Information
- Supporting information for this article is available online at https://doi.org/10.1055/s-0036-1588544.
- Supporting Information
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