Synthesis of Biologically Active 2-Arylbenzoxazoles Using “Green Reagent”


Authors : Dr. Nagesh Sutar

Volume/Issue : Volume 10 - 2025, Issue 8 - August


Google Scholar : https://tinyurl.com/ne4p9sy2

Scribd : https://tinyurl.com/5n8vzs7m

DOI : https://doi.org/10.38124/ijisrt/25aug343

Note : A published paper may take 4-5 working days from the publication date to appear in PlumX Metrics, Semantic Scholar, and ResearchGate.

Note : Google Scholar may take 30 to 40 days to display the article.


Abstract : A chemical reaction has been developed to prepare 2-arylbenzoxazoles which are known for the biological activities. In this protocol, 2-aminophenol was made to react with aromatic aldehydes bearing different substituents, anhydrous bismuth tribromide serving as a catalyst and ethyl alcohol as solvent. The noteworthy attributes of this methodology are the utilization of an eco-friendly catalyst, mild reaction parameters and the achievement of moderate to good yields for the desired products.

Keywords : 2-Arylbenzoxazole, Biological Activities, Anhydrous Bismuth Tribromide, Eco-Friendly Catalyst, Good Yields.

References :

  1. P. Anusha, J. Venkateshwar Rao, ‘‘Synthesis and Biological Evaluation of benzoxazole derivatives as new anti-microbial agents, International Journal of Pharmacy and Biological Sciences,’’ Volume 4, Issue 4, Oct-Dec 2014, 83-89.
  2. L.Turker, E. Sener, I. Yalcin, U. Akbulut, I. Kayalidere, ‘‘QSAR of some antifungal- active benzoxazole using the quantum chemical parameters,’’ Scientia Pharmaceutica, 58, 107 113, (1990)
  3. (i) K.R. Kumar, P.V.V. Satyanarayana, B.S. Reddy, “NaHSO4-SiO2-Promoted Solvent-Free Synthesis of Benzoxazoles, Benzimidazoles, and Benzothiazole Derivatives,’’ Journal of Chemistry, 2013, 2013, 151273. (ii) S. Sato, Kajiura, M. Noguchi, K. Takehana, T. Kobayashi, T.Tsuji, “AJI9561, a new cytotoxic benzoxazole derivative produced by Streptomyces sp.’’ J Antibiot. 2001, 54: 102–104.
  4. S. Rezayati, M. Mehmannavaz, E. Salehi, S. Haghi, R. Hajinasiri, S. Afshari Sharif Abad, “Phospho Sulfonic Acid Catalyzed Synthesis of Benzimidazole, Benzoxazole and Quinoxaline Derivatives under Green Solvent at Ambient Temperature,’’ Journal of Sciences, Islamic Republic of Iran, 2016, 27, 51–63.
  5. S. Wijekoon, C. Gunasekara, L. Palliyaguru, N. Fernando, P. Jayaweera, U. Kumarasinghe, “Solvent-free synthesis and antifungal activity of 3-alkenyl oxindole derivatives” Asian Journal of Green Chemistry, 2022, 6, 297–319.
  6. A. Datta, “Dowex 50W: A Green Mild Reusable Catalyst for the Synthesis of 2-Aryl Benzoxazole Derivatives in Aqueous Medium,’’ Oriental Journal of Chemistry, 2021, 37, 341–347.
  7. Fatemeh Hakimi, Mohammad Taghvaee , Elaham Golrasan, Synthesis of Benzoxazole Derivatives Using Fe3O4@SiO2-SO3H Nanoparticles as a Useful and Reusable Heterogeneous Catalyst Without Using a Solvent, Advanced Journal of Chemistry-Section A, 2023, 6(2), 188-197
  8. Scott W. Krabbe, Ram S. Mohan, Environmentally Friendly Organic Synthesis Using Bismuth (III) Compounds, Top Curr Chem (2012) 311: 45–68.
  9. G. Sabitha, R. S. Babu, E. V. Reddy, J. S. Yadav, “A Novel, Efficient, and Selective Cleavage of Acetals Using Bismuth (III) Chloride,” Chemistry Letters, 2000, 29(9): 1074-1075.
  10. H. Firouzabadi, I. Mohammadpoor-Baltork, S. Kolagar, “A rapid, selective and efficient method for deprotection of silyl ethers catalyzed by bismuth (III) salts’’ Synthetic Communication. 2001, 31, 905.
  11. N. M. Leonard, L. C. Wieland, R. S. Mohan, Tetrahedron 2002, 58, 8373.: N. M. Leonard, L. C. Wieland and R. S. Mohan, “Applications of Bismuth (III) Compounds in Organic Synthesis,” Tetrahedron, Vol. 58, No. 42, 2002, pp. 8373-8397.
  12. Y. Matano and T. Ikegami, in Organobismuth Chemistry, H. Suzuki and Y. Manato, Eds., chapter 2, pp. 21–245, Elsevier, New York, NY, USA, 2001.
  13. R. S. Varma, R. K. Saini and O. Prakash, “Hypervalent Iodine Oxidation of Phenolic Schiff’s Bases: Synthesis of 2-Arylbenzoxazoles,” Tetrahedron Letters, Vol. 38, No. 15, 1997, pp. 2621-2622.
  14. K. Bourgrin, A. Loupy, M. Soufiaoui, “Trois nouvelles voies de synthèse des dérivés 1,3-azoliques sous micro-ondes,’’ Tetrahedron 1998, 54, 8055.
  15. S. Harsha Vardhan, G. Yashwanthi Sai, B. Ishwarya Lxami and N. Krishnarao, One-pot Synthesis of Benzoxazole analogous catalyzed by Zn (OAc)2, World Journal of Pharmaceutical Research, Volume 14, Issue 8, 984-991.
  16. K. Ravi Kumar, P. V. V Satyanarayana, B. Srinivasa Reddy, Direct and practical synthesis of 2-Arylbenzoxazoles promoted by Silica supported sodium hydrogen sulphate, Der Pharma Chemica, 2012, 4 (2):761-766.
  17. Priyanka, Manish Kumar Gautam, Neeraj Kant Sharma, Keshari Kishore Jha, M. Vijayakumar, Design, Synthesis and Pharmacological Screening of 2-(2-(benzo [d] oxazol-2-yl) phenylamino)-n-(substituted phenyl) acetamides as Anti-inflammatory and Analgesic agents, Journal of Advanced Scientific Research, 2014, 5(1): 22-27.
  18. Heraclio López-Ruiz, Horacio Briseño-Ortega, Susana Rojas-Lima, Rosa Santillan, Norberto Farfán, Phenylboronic acid catalyzed-cyanide promoted, one-pot synthesis of 2-(2-hydroxyphenyl) benzoxazole derivatives, / Tetrahedron Letters 52 (2011) 4308–4312.

A chemical reaction has been developed to prepare 2-arylbenzoxazoles which are known for the biological activities. In this protocol, 2-aminophenol was made to react with aromatic aldehydes bearing different substituents, anhydrous bismuth tribromide serving as a catalyst and ethyl alcohol as solvent. The noteworthy attributes of this methodology are the utilization of an eco-friendly catalyst, mild reaction parameters and the achievement of moderate to good yields for the desired products.

Keywords : 2-Arylbenzoxazole, Biological Activities, Anhydrous Bismuth Tribromide, Eco-Friendly Catalyst, Good Yields.

CALL FOR PAPERS


Paper Submission Last Date
30 - November - 2025

Video Explanation for Published paper

Never miss an update from Papermashup

Get notified about the latest tutorials and downloads.

Subscribe by Email

Get alerts directly into your inbox after each post and stay updated.
Subscribe
OR

Subscribe by RSS

Add our RSS to your feedreader to get regular updates from us.
Subscribe