“Overview of Synthetic Approaches to Commercially Successful Drugs with Small-Ring Heterocyclicâ€

Mahesh Parit, Sanjeev Mali, Aravind Pawar and Nayana D
Additional contact information
Mahesh Parit: Pharmaceutical Chemistry, Shri Sharanabasaveshwar College of Pharmacy, Vijayapur,India
Sanjeev Mali: Pharmaceutical Chemistry, Shri Sharanabasaveshwar College of Pharmacy, Vijayapur,India
Aravind Pawar: Pharmaceutical Chemistry, Shri Sharanabasaveshwar College of Pharmacy, Vijayapur,India
Nayana D: Pharmaceutical Chemistry, Shri Sharanabasaveshwar College of Pharmacy, Vijayapur,India

International Journal of Research and Innovation in Applied Science, 2025, vol. 10, issue 4, 1000-1013

Abstract: Small-ring heterocycles are essential building blocks in pharmaceutical chemistry, widely found in approved drugs due to their unique reactivity and biological activity. This review summarizes recent synthetic strategies for constructing three- and four-membered rings such as aziridines, β-lactams, and azetidines. These rings exhibit high ring strain, enabling versatile transformations like cycloaddition and nucleophilic substitution. Chalcones are helpful building blocks for making various nitrogen-containing compounds, like pyrroles and triazoles, and eco-friendly methods like microwave and ultrasound treatment often improve this process. Oxygen-containing rings such as tetrahydropyrans and isoxazolines are synthesized via organocatalytic oxa-Michael reactions. Additionally, ring-closing metathesis and copper-catalyzed 1,3-dipolar cycloaddition offer efficient access to five- and six-membered heterocycles under mild, eco-friendly conditions. Thiosemicarbazides are known for synthesizing N-, O-, and S-containing heterocycles but remain underutilized in small-ring construction and biological evaluation. Ternary condensation strategies also yield bioactive fused heterocycles. Future efforts should focus on expanding structural diversity and understanding structure–activity relationships.

Date: 2025
References: Add references at CitEc
Citations:

Downloads: (external link)
https://www.rsisinternational.org/journals/ijrias/ ... ssue-4/1000-1013.pdf (application/pdf)
https://rsisinternational.org/journals/ijrias/arti ... l-ring-heterocyclic/ (text/html)

Related works:
This item may be available elsewhere in EconPapers: Search for items with the same title.

Export reference: BibTeX RIS (EndNote, ProCite, RefMan) HTML/Text

Persistent link: https://EconPapers.repec.org/RePEc:bjf:journl:v:10:y:2025:i:4:p:1000-1013

Access Statistics for this article

International Journal of Research and Innovation in Applied Science is currently edited by Dr. Renu Malsaria

More articles in International Journal of Research and Innovation in Applied Science from International Journal of Research and Innovation in Applied Science (IJRIAS)
Bibliographic data for series maintained by Dr. Renu Malsaria ().