Green Synthetic Approaches for Biologically Relevant Heterocycles

Volume 1: Advanced Synthetic Techniques

2nd Edition - February 26, 2021
Imprint: Elsevier
Editor: Goutam Brahmachari
Language: English
Paperback ISBN:
9 7 8 - 0 - 1 2 - 8 2 0 5 8 6 - 0
eBook ISBN:
9 7 8 - 0 - 3 2 3 - 8 5 1 3 0 - 5

Green Synthetic Approaches for Biologically Relevant Heterocycles, Second Edition, Volume One: Advanced Synthetic Techniques reviews this significant group of organic compounds… Read more

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Green Synthetic Approaches for Biologically Relevant Heterocycles, Second Edition, Volume One: Advanced Synthetic Techniques reviews this significant group of organic compounds within the context of sustainable methods and processes, expanding on the first edition with fully updated coverage and a whole range of new chapters. Volume One explores advanced synthetic techniques, with each chapter presenting in-depth coverage of various green protocols for the synthesis of a wide variety of bioactive heterocycles that are classified on the basis of ring-size and/or the presence of heteroatoms. Techniques covered range from high pressure cycloaddition reactions and microwave irradiation to sustainable one-pot domino reactions.

This updated edition is an essential resource on sustainable approaches for academic researchers, R&D professionals, and students working across medicinal, organic, natural product and green chemistry.

Cover image
Title page
Table of Contents
Copyright
Dedication
List of contributors
Editor
Foreword
Preface
Chapter 1. Green synthetic approaches for biologically relevant heterocycles: advanced synthetic techniques—an overview
Abstract
1.1 Introduction
1.2 An overview of the book
1.3 Concluding remarks
Chapter 2. High-pressure cycloaddition reactions in the synthesis of biologically relevant heterocycles
Abstract
2.1 Introduction
2.2 Diels-Alder cycloadditions
2.3 Dipolar cycloadditions
2.4 [2+2]-Cycloadditions
2.5 Concluding Remarks
Abbreviations
References
Chapter 3. Microwave-assisted synthesis of medicinally privileged heterocycles
Abstract
3.1 Introduction
3.2 Microwave irradiation: mechanism
3.3 Microwave-induced synthesis of heterocycles of medicinal interests
3.4 Concluding remarks
Acknowledgments
Abbreviations
References
Chapter 4. Application of microwave irradiation in the synthesis of P-heterocycles
Abstract
4.1 Introduction
4.2 Functionalization of cyclic phosphinic acids
4.3 Diels–Alder cycloadditions, fragmentation-related phosphorylations, and inverse Wittig-type reactions
4.4 Phospha-Michael reactions
4.5 Kabachnik–Fields reactions
4.6 The deoxygenation of 2,5-dihydro-1H-phosphole 1-oxides
4.7 Synthesis and reactions of new 7-phosphanorbornene derivatives
4.8 Concluding remarks
Acknowledgments
References
Chapter 5. Microwave-assisted multicomponent reactions as a green synthetic approach to heterocycles: special reference to Hantzsch, Biginelli, and Groebke–Blackburn–Bienayme reactions
Abstract
5.1 Introduction
5.2 Hantzsch reaction
5.3 Biginelli reaction
5.4 Groebke–Blackburn–Bienayme reaction
5.5 Concluding remarks
References
Chapter 6. Use of ball milling for the synthesis of biologically active heterocycles
Abstract
6.1 Introduction
6.2 Synthesis of heterocycles
6.3 General green aspects of mechanochemical reaction
6.4 Concluding remarks
Acknowledgments
References
Chapter 7. Recent advances in photocatalytic Minisci reaction: an eco-friendly functionalization of biologically relevant heteroarenes
Abstract
7.1 Introduction
7.2 Minisci reaction: a synthetic tool for bioactive molecules
7.3 Minisci reaction: the TiO2-mediated photocatalytic approach
7.4 Minisci reaction: recent advances in the photocatalytic approach
7.5 Concluding remarks
References
Chapter 8. Recent advances for construction and late-stage diversification of indole core via C–H bond activation/functionalization
Abstract
8.1 Introduction
8.2 Methods for the synthesis of indoles
8.3 C–H bond activation
8.4 C–H bond activation approaches for synthesis of functionalized indole framework
8.5 Late-stage diversification of indole system (C–H activation of preformed indole framework)
8.6 C–H bond functionalization of indole at C6 position
8.7 Concluding remarks
References
Chapter 9. Cycloaddition reactions in ionic liquids for the synthesis of biologically relevant heterocycles
Abstract
9.1 Introduction
9.2 The hetero-cycloaddition reactions in ionic liquids
9.3 Concluding remarks
Acknowledgments
References
Chapter 10. Advances in greener processes for triazole synthesis via azide-alkyne cycloaddition reactions
Abstract
10.1 Introduction
10.2 Methods of synthesis of triazoles using greener processes
10.3 Concluding remarks
References
Chapter 11. Employing arynes in transition-metal-free synthesis of benzo-fused five and six-membered heterocycles: an update
Abstract
11.1 Introduction
11.2 Synthesis of five-membered heterocycles
11.3 Synthesis of six-membered heterocycles
11.4 Selected examples for the synthesis of medium-sized heterocycles
11.5 Concluding remarks
References
Chapter 12. Multicomponent approach for the sustainable synthesis of lawsone-based heterocycles
Abstract
12.1 Introduction
12.2 Synthesis of lawsone-based heterocycles via multicomponent approach
12.3 Concluding remarks
References
Chapter 13. Synthesis of biologically relevant heterocyclic skeletons under solvent-free condition
Abstract
13.1 Introduction
13.2 Synthesis of nitrogen-containing heterocycles
13.3 Synthesis of biologically relevant oxygen heterocycles
13.4 Syntheses of heterocycles with two different heteroatoms
13.5 Synthesis of larger ring size heterocycles
13.6 Concluding remarks
Acknowledgment
References
Chapter 14. Ultrasound-promoted metal-catalyzed synthesis of heterocyclic compounds of medicinal interest
Abstract
14.1 Introduction
14.2 Ultrasound-promoted metal-catalyzed synthesis of heterocycles of medicinal interest
14.3 Concluding remarks
References
Chapter 15. Ultrasonication under catalyst-free condition: an advanced synthetic technique toward the green synthesis of bioactive heterocycles
Abstract
15.1 Introduction
15.2 Ultrasound wave-assisted catalyst-free multicomponent synthesis of N-/O-heterocycles
15.3 Concluding remarks
References
Chapter 16. Self-catalytic techniques for the synthesis of biologically relevant heterocyclic scaffolds at room temperature: a recent update
Abstract
16.1 Introduction
16.2 Self-catalytic synthetic endeavors for biologically relevant heterocyclic scaffolds without the aid of any catalysts
16.3 Concluding remarks
Acknowledgment
References
Index

Goutam Brahmachari

Born on April 14, 1969 in Barala, a village in the district of Murshidabad (West Bengal, India), Goutam Brahmachari had his early education in his native place. He received his high school degree in scientific studies in 1986 at Barala R. D. Sen High School under the West Bengal Council of Higher Secondary Education (WBCHSE). Then, he moved to Visva-Bharati (a Central University founded by Rabindranath Tagore at Santiniketan, West Bengal, India) to study chemistry at the undergraduate level. After graduating from this university in 1990, he completed his master’s in 1992, specializing in organic chemistry. After receiving his Ph.D. 1997 in chemistry from the same university, he joined his alma mater the next year and has been a full professor of chemistry since 2011. The research interests of Prof. Brahmachari’s group include synthetic organic chemistry, green chemistry, natural products chemistry, and the medicinal chemistry of natural and natural product-inspired synthetic molecules. With more than 25 years of experience in teaching and research, he has produced over 260 scientific publications, including original research papers, review articles, books, and invited book chapters in the field of natural products and green chemistry. He has already authored/edited 27 books published by internationally reputed major publishing houses, namely, Elsevier Science (The Netherlands), Academic Press (Oxford), Wiley-VCH (Germany), Alpha Science International (Oxford), De Gruyter (Germany), World Scientific (Singapore), CRC Press (Taylor & Francis Group, USA), Royal Society of Chemistry (Cambridge), etc. Prof. Brahmachari serves several scientific bodies in India and abroad, and also many international journals as an editorial member. He has also been serving as co-editor-in-chief for Current Green Chemistry. Prof. Brahmachari is the founder series editor of the Elsevier Book Series ‘Natural Product Drug Discovery’. Prof. Brahmachari is an elected fellow of the Royal Society of Chemistry and a recipient of the CRSI (Chemical Research Society of India) Bronze Medal-2021 (for his contribution to research in chemistry), Dr Basudev Banerjee Memorial Award-2021 (for his contribution to the field of chemical sciences) from the Indian Chemical Society, INSA (Indian National Science Academy) Teachers Award-2019, Dr Kalam Best Teaching Faculty Award-2017, and Academic Brilliance Award, 2015 (Excellence in Research). Prof. Brahmachari was featured in the World Ranking of the Top 2% Scientists (Organic Chemistry Category) in 2020-23, the AD Scientific World Ranking of Scientists in 2022-2024, and as the Scholar GPS Highly Ranked Scholar-2024 (Lifetime, securing a position in the top 0.05% of all scholars worldwide).

Affiliations and expertise

Goutam Brahmachari, PhDFull Professor, Organic Chemistry, Department of Chemistry, Visva-Bharati (a Central University), Santiniketan, West Bengal, India

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