A protocol for directly accessing geminal C-4 diarylated pyrazol-5(4 H )-ones via tandem C-H aryne insertion and their inceptive neurobiological evaluation.

Geminal C-4 diarylation of substituted pyrazol-5(4 H )-ones with in situ generated arynes as the aryl source has been achieved in a one-flask operation. All the newly accessed C4- gem -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.