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A series of sulfonyl dihydrofuropyrazole derivatives was prepared from one pot multi component condensation of sulfonated β-keto ester, aromatic aldehyde, hydrazine, pyridinium ylide in presence of piperidine catalyst under ethanol solvent conditions and subsequent oxidation of SPh group with MCPBA. All the synthesized compounds were characterized by analytical and spectral techniques and screened in vitro for antimicrobial activity. The activity data revealed that most of the compounds exhibited good to significant activities. Compounds 6b, 6i, 6j, 6k, 6m, 6n exhibited good and broad spectrum activity towards all the tested bacterial strains.

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Aim and Objective: In the work, we have successfully presented a synthetic route for the synthesis of novel 2',4'-dihydrospiro[chroman-2,3'-pyrazol]-4-one derivatives via one pot multicomponent approach. Materials and Method: Substituted 2',4'-dihydrospiro[chroman-2,3'-pyrazol]-4-one were prepared through cascade three-component condensation of ortho-hydroxyacetophenone, β-ketoester, hydrazine in the presence of pyrrolidine as a catalyst under ethanol reflux conditions. Results: A series of novel 2',4'-dihydrospiro[chroman-2,3'-pyrazol]-4-one have been synthesized through a facile strategy. These structures of newly synthesized derivatives were determined by 1H, 13C NMR, HRMS and CHNS analysis. Conclusion: We have achieved the one-pot, three-component synthesis of highly substituted pyrazole spirochromanones in presence of pyrrolidine as a catalyst under ethanol reflux conditions. Using different types of aliphatic and aromatic β-ketoesters, o-hydroxyacetophenone derivatives and different kinds of hydrazine derivatives as building blocks, we could construct novel libraries of substituted pyrazole spirochromanones that make this method suitable for combinatorial and parallel synthesis in drug discovery.

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