Efficient green catalyst for one-pot synthesis of benzimidazole
Journal name: World Journal of Pharmaceutical Research
Original article title: New and efficient green catalyst one-pot synthesis of benzimidazole and derivatives
The WJPR includes peer-reviewed publications such as scientific research papers, reports, review articles, company news, thesis reports and case studies in areas of Biology, Pharmaceutical industries and Chemical technology while incorporating ancient fields of knowledge such combining Ayurveda with scientific data.
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Gurumeet C. Wadhawa, Vitthal S. Shivankar, Yashwant A. Gaikwad, Nilam S. Dhumale, Charansingh H. Gill and Laxman V. Gavali
World Journal of Pharmaceutical Research:
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Full text available for: New and efficient green catalyst one-pot synthesis of benzimidazole and derivatives
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr20187-11579
Copyright (license): WJPR: All rights reserved
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Summary of article contents:
Introduction
Benzimidazole and its derivatives are crucial components in numerous biologically active compounds, including pharmaceuticals. Their synthesis has gained significant attention due to their diverse applications in medicine, agrochemicals, and other fields. Traditional methods for preparing benzimidazoles often suffer from inefficiencies such as low yields and lengthy reaction times. In this context, the research conducted by Gurumeet C. Wadhawa et al. presents a novel and efficient approach for the one-pot synthesis of benzimidazole and its derivatives using ferrous sulphate as a catalyst, aiming to improve yield and streamline the synthesis process.
Green Catalysis in Synthesis
One of the pivotal concepts highlighted in this research is the use of ferrous sulphate as a green catalyst in the synthesis of benzimidazole derivatives. The method entails a one-pot reaction involving o-phenylenediamine and various aromatic aldehydes. By employing ferrous sulphate, the reaction not only achieves high yields with excellent chemo selectivity but also emphasizes an eco-friendly approach, avoiding toxic solvents and minimizing harmful by-products. This incorporation of a mild and readily available oxidizing agent paves the way for more sustainable chemical processes in benzimidazole synthesis.
Methodology and Experimental Conditions
The experimental framework relies on two distinct solvent systems, namely ethanol and water, to facilitate the reaction at room temperature under sonication and grinding. This dual-approach allows for the exploration and comparison of solvent effects on reaction performance. Throughout the study, the progress of reactions was monitored using thin-layer chromatography (TLC), and a simple work-up procedure was employed post-reaction. The study's results indicated that ethanol provided superior yields compared to water, demonstrating the importance of solvent choice in optimizing reaction outcomes.
Reaction Performance and Observations
The research presents comprehensive observations regarding the efficiency of various aromatic aldehydes in the proposed synthesis. Entries in multiple tables detail the reaction times and yields corresponding to different aldehydes, noting how electron-withdrawing groups tend to accelerate the reaction rate, while electron-donating groups decrease it. Additionally, the effect of substitution at the ortho position of the aldehyde on reaction times is discussed, highlighting how these structural factors influence the overall synthesis duration. Overall, the study successfully illustrates that a diverse range of aldehydes can be employed to synthesize benzimidazole derivatives with varying efficiencies.
Conclusion
In conclusion, the research underscores the efficacy and sustainability of using ferrous sulphate for the one-pot synthesis of benzimidazole derivatives. The method not only provides excellent yields under mild conditions but also adheres to environmentally friendly practices by minimizing the use of toxic solvents and reducing the generation of hazardous waste. This innovative approach not only advances the field of heterocyclic chemistry but also contributes to the pursuit of greener chemistry, making it a valuable addition to synthetic methodologies for benzimidazole compounds.
FAQ section (important questions/answers):
What are benzimidazoles and their significance in pharmaceuticals?
Benzimidazoles are heteroaromatic compounds important in many biologically active drugs, playing crucial roles in the metabolism of living cells, including essential amino acids and nucleic acids.
What is the method used for synthesizing benzimidazoles in this study?
The study employs a one-pot reaction of o-phenylenediamine with aromatic aldehydes using ferrous sulphate as a catalyst, conducted under sonication or grinding in ethanol or water.
Why is ferrous sulphate used as a catalyst in this research?
Ferrous sulphate is a cheap, accessible oxidizing agent that enhances the efficiency of synthesizing 2-arylbenzimidazoles and allows for quick reaction times and easy work-up procedures.
What are the solvents used in the synthesis of benzimidazoles?
Ethanol and water are used as solvents in the synthesis process, and the results indicated that ethanol provides better yields and faster reaction times.
What are the advantages of the proposed benzimidazole synthesis method?
The method offers advantages like short reaction times, easy purification, excellent chemo-selectivity, and minimizes the use of toxic solvents, contributing to an eco-friendly synthesis.
What factors influence the reaction rates in benzimidazole synthesis?
Electron-withdrawing groups on benzaldehyde accelerate reaction rates, while electron-donating groups might slow them. Additionally, substitutions at the ortho position can extend reaction times significantly.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Efficient green catalyst for one-pot synthesis of benzimidazole”. This list explains important keywords that occur in this article and links it to the glossary for a better understanding of that concept in the context of Ayurveda and other topics.
1) Water:
Water serves as a solvent in chemical reactions, including the synthesis of benzimidazoles in this study. It is utilized due to its eco-friendly properties, making reactions more sustainable by avoiding toxic solvents. Additionally, water helps in the reaction's clean-up process, enabling a more straightforward work-up and enhancing the overall reaction efficiency.
2) Table:
The term 'Table' refers to organized data presentation summarizing experimental results, such as yields and melting points of synthesized compounds. In scientific literature, tables offer clear insights into findings, allowing readers to assess the effectiveness of various conditions or reagents used in experiments, facilitating reproducibility and comparative analysis.
3) Purification:
Purification is a crucial step in chemistry that involves isolating a desired product from its raw reaction mixture. In this study, recrystallization from ethanol is suggested to enhance the purity of synthesized benzimidazole compounds. High purity is essential in pharmaceutical applications to ensure efficacy and safety of the final product.
4) Maharashtra (Maharastra, Maha-rashtra):
Maharashtra is a state in India, home to various educational and research institutions, including Karmaveer Bhaurao Patil College, where this research was conducted. The geographical context is relevant as it provides insight into the regional academic landscape and promotes local sciences, contributing to the development of drug discovery and other fields.
5) Observation:
In scientific research, observation entails gathering data and noting phenomena during experiments. Regular monitoring of reaction progress, commonly through techniques like TLC, ensures that researchers can optimize reaction conditions effectively. This systematic observations are essential for achieving reproducible results and valid conclusions in the context of chemical syntheses.
6) India:
India, as the country where this research took place, has a rapidly growing pharmaceutical sector known for its contributions to drug development and production. The country's biodiversity and rich traditional medicinal knowledge complement modern research, enabling innovative approaches to synthesize compounds like benzimidazoles that can have significant pharmacological benefits.
7) Patil:
Patil refers to Karmaveer Bhaurao Patil College, an educational institution where the research was conducted. The involvement of academic institutions indicates the collaborative nature of scientific research, providing a platform for students and professionals to explore advancements in chemistry and contribute to the pharmaceutical industry's growth.
8) Vasi (Vasin, Vashin, Vashi):
Vashi is a locality in Navi Mumbai, Maharashtra, where Karmaveer Bhaurao Patil College is situated. The local environment, including academic resources and collaboration opportunities, directly affects research outputs. Its significance lies in fostering innovation, education, and scientific exploration within its community, particularly in chemistry and drug synthesis.
9) Study (Studying):
The study represents systematic research aimed at exploring new methods for synthesizing benzimidazole and its derivatives. It showcases the progression of chemical methodologies, emphasizing the need for greener techniques. Such studies contribute to the broader scientific understanding, advancing both academic knowledge and practical applications within the medicinal chemistry domain.
10) Post:
The term 'Post' in this context refers to the Post Graduate Department of Chemistry where researchers investigate new chemical synthesis methods. The postgraduate education framework is vital for cultivating advanced knowledge and skills in the area of pharmaceuticals, allowing students to contribute meaningfully to scientific literature and practical applications.
11) Drug:
Drugs represent compounds utilized for medical treatment, and the synthesis of new drugs or drug derivatives is vital for developing therapies for various diseases. The study contributes to this effort by presenting efficient methods for synthesizing benzimidazole derivatives, which can expand clinical treatment options and improve patient care.
12) Pharmacological:
Pharmacological pertains to the study of drugs and their effects on biological systems. The relevance of pharmacology in this research underlines the importance of investigating compounds like benzimidazole derivatives for their potential medical applications. Understanding their interactions and activities is essential for developing effective therapeutic agents.
13) Similarity:
The term 'similarity' highlights the comparative aspect of chemical structures in pharmaceutical compounds. Biological active compounds often share structural similarities with heteroaromatic rings in benzimidazole derivatives, which can lead to significant biological interactions in the body. This relationship is fundamental in drug design and discovery, ensuring efficacy in treatment.
14) Pesticide:
Pesticides are chemicals used for controlling pests and are derived from various compounds, including heterocyclic ones. The relevance here is the broader application of synthetic methods developed in this study that could extend beyond pharmaceuticals, addressing agricultural needs and the synthesis of agrochemicals that ensure crop protection and productivity.
15) Medicine:
Medicine refers to the field concerned with the diagnosis, treatment, and prevention of illness. The synthesis of benzimidazole derivatives is significant in this context because these compounds often have therapeutic properties, making this research crucial for advancing medical treatments and improving health outcomes in various diseases.
16) Activity:
Activity in this scientific context refers to the biological activity of synthesized compounds. The research highlights how the synthesized benzimidazole derivatives demonstrate different levels of pharmacological activity, which is critical for evaluating their effectiveness and potential applications in medical settings, guiding further drug development efforts.
17) Vitthal:
Vitthal refers to one of the authors of the study, indicating the collaborative effort behind the research. The involvement of multiple researchers denotes the importance of teamwork in scientific endeavors, as diverse perspectives and expertise contribute to more comprehensive and innovative outcomes in the field of chemistry.
18) Nature:
Nature encompasses the physical world, including organic and inorganic compounds. The relevance of nature in this study underscores the significance of utilizing environmentally benign methods like green chemistry, which aligns with sustainability principles by minimizing harmful by-products and opting for safer methodologies in chemical synthesis.
19) Animal:
Animal references the biological aspect related to the effects of the synthesized benzimidazole derivatives, as many pharmaceutical compounds act by interacting with animal physiology. Understanding how these compounds behave in biological systems can guide further research and development, ultimately benefiting therapeutic practices in both human and veterinary medicine.
20) Field:
Field denotes the area of study, in this case, the field of chemistry and pharmaceutical research. This designation underscores the specific focus of the work in developing methodologies for synthesizing important biologically active compounds like benzimidazoles, facilitating advancements in drug discovery and related sectors.
21) Nilam:
Nilam refers to one of the authors involved in the research. The individual contribution emphasizes the collaborative nature of scientific investigation, showcasing how different expertise fosters innovation and comprehensive studies, ultimately leading to advancements in the understanding and synthesis of medicinal compounds like benzimidazole.
22) Hand:
Hand signifies the practical aspect of conducting experiments, underlying the importance of hands-on experience in scientific research. In the synthesis of compounds, the direct involvement of researchers in the experimental process is crucial for achieving results, validating methods, and gaining insights that contribute to the field of medicinal chemistry.
23) Life:
Life pertains to the biological context in which pharmacologically active compounds operate. Understanding the interaction of synthesized drugs with biological systems is essential for developing effective treatments. This research contributes to enhancing therapeutic options, ultimately aiming to improve health and well-being in living organisms.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Efficient green catalyst for one-pot synthesis of benzimidazole’. Further sources in the context of Science might help you critically compare this page with similair documents:
Aromatic aldehyde, One pot reaction, Pharmaceutical product, Electron withdrawing group, Electron donating group, Ferrous sulfate, Short reaction time.