Geminal C-4 diarylation of substituted pyrazol-5(4)-ones with generated arynes as the aryl source has been achieved in a one-flask operation. All the newly accessed C4--diarylated pyrazolone entities were found to be non-cytotoxic with varying AChE enzyme inhibitory activities and BBB permeability attributes that augur well for further advancement towards CNS therapeutics for untreatable disorders.
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| http://dx.doi.org/10.1039/d3ob01932b | DOI Listing |
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