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

K. A. Sudarshana; Manas Jyoti Sarma; Mydhili Radhakrishnan; Sumana Chakravarty; Pabbaraja Srihari; Goverdhan Mehta

doi:10.1039/D3OB01932B

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

K. A. Sudarshana,‡^ab Manas Jyoti Sarma,

‡^ac Mydhili Radhakrishnan,^bd Sumana Chakravarty,

^bd Pabbaraja Srihari

*^ab and Goverdhan Mehta

*^c

Author affiliations

* Corresponding authors

^a Department of Organic Synthesis and Process Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad-500007, India
E-mail: srihari@iict.res.in

^b Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India

^c School of Chemistry, University of Hyderabad, Hyderabad-500046, India
E-mail: gmehta43@gmail.com

^d Applied Biology, CSIR-Indian Institute of Chemical Technology, Hyderabad-500007, India

Abstract

Geminal C-4 diarylation of substituted pyrazol-5(4H)-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.

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DOI: https://doi.org/10.1039/D3OB01932B
Article type: Communication
Submitted: 28 Nov 2023
Accepted: 19 Dec 2023
First published: 19 Dec 2023

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Org. Biomol. Chem., 2024,22, 714-719

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

K. A. Sudarshana, M. J. Sarma, M. Radhakrishnan, S. Chakravarty, P. Srihari and G. Mehta, Org. Biomol. Chem., 2024, 22, 714 DOI: 10.1039/D3OB01932B

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Organic & Biomolecular Chemistry

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

Abstract

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

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