A Comprehensive Review on Traditional and Modern Synthetic Approaches to Pyrazole and Its Analogs

ABSTRACT Pyrazoles constitute a pivotal heterocyclic scaffold found in anti‐inflammatory, anticancer, anticonvulsant, antidepressant, and anti‐infective agents, highlighting their significance in pharmaceutical development. This review critically examines two principal synthetic methodologies: (i) the condensation of 1,3‐dicarbonyl compounds and conjugated π‐systems with hydrazine derivatives, focusing on substrate scope, regioselectivity challenges, and mechanistic underpinnings, and (ii) [3 + 2] cycloaddition strategies involving alkynes or activated olefins with 1,3‐dipoles, emphasizing catalyst systems and functional group tolerance. Recent innovations, including solvent‐free microwave‐assisted synthesis, visible‐light photocatalysis, and flow chemistry, are highlighted for their roles in improving atom economy and scalability of pyrazole frameworks. By comparing classical methods with emerging green and continuous synthesis techniques, this review provides practical insights to facilitate the design of efficient and sustainable pyrazole syntheses tailored for pharmaceutical and materials applications.

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Publication Details

Journal
Journal of Heterocyclic Chemistry
Published
2025-08-31
DOI
https://doi.org/10.1002/jhet.70065
Citations
2
Primary Topic
Synthesis and biological activity
Type
article
Field-Weighted Citation Impact
1.87
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article

A Comprehensive Review on Traditional and Modern Synthetic Approaches to Pyrazole and Its Analogs

R. Ramajayam
2 citations
Journal of Heterocyclic Chemistry
Synthesis and biological activity
1.87
article

A Comprehensive Review on Traditional and Modern Synthetic Approaches to Pyrazole and Its Analogs

R. Ramajayam
article en
2 citations

Abstract

ABSTRACT Pyrazoles constitute a pivotal heterocyclic scaffold found in anti‐inflammatory, anticancer, anticonvulsant, antidepressant, and anti‐infective agents, highlighting their significance in pharmaceutical development. This review critically examines two principal synthetic methodologies: (i) the condensation of 1,3‐dicarbonyl compounds and conjugated π‐systems with hydrazine derivatives, focusing on substrate scope, regioselectivity challenges, and mechanistic underpinnings, and (ii) [3 + 2] cycloaddition strategies involving alkynes or activated olefins with 1,3‐dipoles, emphasizing catalyst systems and functional group tolerance. Recent innovations, including solvent‐free microwave‐assisted synthesis, visible‐light photocatalysis, and flow chemistry, are highlighted for their roles in improving atom economy and scalability of pyrazole frameworks. By comparing classical methods with emerging green and continuous synthesis techniques, this review provides practical insights to facilitate the design of efficient and sustainable pyrazole syntheses tailored for pharmaceutical and materials applications.

Journal of Heterocyclic ChemistryVol. 62(11)
Bethlem Royal Hospital (GB)
Openalex Percentile: Top 14%
Synthesis and biological activity
1.87
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A Comprehensive Review on Traditional and Modern Synthetic Approaches to Pyrazole and Its Analogs — R. Ramajayam · Journal of Heterocyclic Chemistry (2025) | TGRS Research Map | TGRS