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Heterocycles feature widely in natural products, agrochemicals, pharmaceuticals and dyes, and their synthesis is of great interest to synthetic chemists in both academia and industry. The contributions of recent applications of new methodologies in C–H activation, photoredox chemistry, cross-coupling strategies, borrowing hydrogen catalysis, multicomponent and solvent-free reactions, regio- and stereoselective syntheses, as well as other new, attractive approaches for the construction of heterocyclic scaffolds are of great interest. This Special Issue is dedicated to featuring the latest research that is ongoing in the field of heterocyclic synthesis. It is expected that most submissions will focus on five- and six-membered oxygen and nitrogen-containing heterocycles, but structures incorporating other rings/heteroatoms will also be considered. Original research (communications, full papers and reviews) that discusses innovative methodologies for assembling heterocycles with potential application in materials, catalysis and medicine are therefore welcome.
Enables researchers to fully realize the potential to discover new pharmaceuticals among heterocyclic compounds Integrating heterocyclic chemistry and drug discovery, this innovative text enables readers to understand how and why these two fields go hand in hand in the effective practice of medicinal chemistry. Contributions from international leaders in the field review more than 100 years of findings, explaining their relevance to contemporary drug discovery practice. Moreover, these authors have provided plenty of practical guidance and tips based on their own academic and industrial laboratory experience, helping readers avoid common pitfalls. Heterocyclic Chemistry in Drug Discovery is ideal for readers who want to fully realize the almost limitless potential to discover new and effective pharmaceuticals among heterocyclic compounds, the largest and most varied family of organic compounds. The book features: Several case studies illustrating the role and application of 3, 4, 5, and 6+ heterocyclic ring systems in drug discovery Step-by-step descriptions of synthetic methods and practical techniques Examination of the physical properties for each heterocycle, including NMR data and quantum calculations Detailed explanations of the complexity and intricacies of reactivity and stability for each class of heterocycles Heterocyclic Chemistry in Drug Discovery is recommended as a textbook for organic and medicinal chemistry courses, particularly those emphasizing heterocyclic chemistry. The text also serves as a guide for medicinal and process chemists in the pharmaceutical industry, offering them new insights and new paths to explore for effective drug discovery.
This book focuses on direct nitrogenation strategies to incorporate one or more N-atoms into simple substrates especially hydrocarbons via C–H and/or C–C bond cleavage, which is a green and sustainable way to synthesize nitrogen-containing compounds. The book consists of seven chapters demonstrating interesting advances in the preparation of amines, amides, nitriles, carbamides, azides, and N-heterocyclic compounds and illustrating the mechanisms of these novel transformations. It offers an accessible introduction to nitrogenation reactions for chemists involved in N-compound synthesis and those interested in discovering new reagents and reactions. Ning Jiao is a Professor of Chemistry at Peking University, China.
Established in 1960, Advances in Heterocyclic Chemistry is the definitive serial in the area—one of great importance to organic chemists, polymer chemists, and many biological scientists. Written by established authorities in the field, the comprehensive reviews combine descriptive chemistry and mechanistic insight and yield an understanding of how the chemistry drives the properties. - Provides up-to-date material on a fast-growing and highly topical subject area - Contains the latest research covering a wide variety of heterocyclic topics - Written by leading authorities and designed as a handbook for students and industry and academic researchers
A comprehensive overview of synthetic strategies for nonaromatic nitrogen heterocycles Nitrogen heterocycles are extremely widely distributed in nature, as well as in synthetic substances found in pharmaceuticals, agrochemicals, and materials chemistry. With new structures and medicines that include these structures emerging yearly, and a vast new journal literature to describe them, anyone who wants to be effective in R&D needs to easily access a synthesis of the latest research. This state-of-the-art survey explores recent developments in the most widely used reactions, as well as completely new ones. Highlights the major modern synthetic methods known to obtain nonaromatic nitrogen heterocycles, and their practical applications Topics include enantioselective synthesis and catalysis, photocatalysis, biocatalysis, microwave-assisted synthesis, reactions of oximes and nitrones, and ionic liquids Discusses how to synthesize rings of specific sizes Covers sustainable synthetic approaches for obtaining salts Whether you are using nonaromatic nitrogen compounds as an academic researcher, a synthetic chemist in industry, or an advanced student, this book is an essential, up-to-date resource to support your work.
A comprehensive overview of synthetic strategies for nonaromatic nitrogen heterocycles Nitrogen heterocycles are extremely widely distributed in nature, as well as in synthetic substances found in pharmaceuticals, agrochemicals, and materials chemistry. With new structures and medicines that include these structures emerging yearly, and a vast new journal literature to describe them, anyone who wants to be effective in R&D needs to easily access a synthesis of the latest research. This state-of-the-art survey explores recent developments in the most widely used reactions, as well as completely new ones. Highlights the major modern synthetic methods known to obtain nonaromatic nitrogen heterocycles, and their practical applications Topics include enantioselective synthesis and catalysis, photocatalysis, biocatalysis, microwave-assisted synthesis, reactions of oximes and nitrones, and ionic liquids Discusses how to synthesize rings of specific sizes Covers sustainable synthetic approaches for obtaining salts Whether you are using nonaromatic nitrogen compounds as an academic researcher, a synthetic chemist in industry, or an advanced student, this book is an essential, up-to-date resource to support your work.
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. Provides fully updated coverage of the field of greener heterocycle synthesis Includes new chapters on varied multicomponent reactions, alongside both traditional and novel approaches Presents information in an accessible style with an emphasis on sustainability
Advances in Heterocyclic Chemistry, Volume 142, the latest release in this definitive series, combines descriptive synthetic chemistry and mechanistic insight to yield an understanding of how chemistry drives the preparation and useful properties of heterocyclic compounds. Chapters in this new release include Recent advances in the Synthesis of Benzo[b]furans, Recent Advances in the Synthesis of 6-Membered Heterocycles via Domino and Multicomponent Reactions (from 2017-2022), Multi-component synthesis of isatin based bioactive heterocycles, Recent advances in the chemistry of pyrazolo[1,5-a]pyrimidines, The Literature of Heterocyclic Chemistry, Part XXI, 2021, and much more.Additional sections present the latest Advances in applications of dihydropyridines in organic chemistry and Strategies for the annulation of five-membered sulfur-nitrogen rings to benzene and heterocycles. - Considered the definitive serial in the field of heterocyclic chemistry - Serves as the go-to reference for organic chemists, polymer chemists, and many biological scientists - Provides the latest comprehensive reviews written by established authorities in the field - Combines descriptive synthetic chemistry and mechanistic insights to enhance understanding on how chemistry drives the preparation and useful properties of heterocyclic compounds
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Sulfonyl ynamides are highly versatile and synthetically useful reagents. This thesis details the modular synthesis and use of sulfonyl ynamides in order to access N-heterocyclic scaffolds, such as quinolines and pyrazoles. The synthesis of a wide array of sulfonyl ynamides can be realized via copper-catalyzed amidative cross-couplings or by elimination of dichloroenamide precursors. Additionally the use of Sonogashira chemistry to further diversify terminal ynamides and the synthesis of solid-supported ynamides was investigated. Electrophilically-activated amides can be reacted with sulfonyl ynamides in order to access highly functionalized 4-aminoquinolines. The straightforward amide activation procedure with triflic anhydride and 2-chloropyridine was found to tolerate a wide range of substrates, which allowed for the development of a library of 4-aminoquinolines with ease. Moreover, 4-aminopyrazoles can be prepared by reacting terminal sulfonyl ynamides with sydnones under copper catalysis. However, as the copper catalysts were also found to promote the degradation of the ynamides, a copper-free strain-promoted alternative was developed. An in situ prepared 3-azacyclohexyne was found to tolerate a wide array of C-4 substituted sydnones, producing a mixture of both the 3,4- and 4,3-fused pyrazoles in good yields. Additional investigations into heterocyclic methodology led to the development of highly sophisticated, non-symmetrical and axially-chiral dibenzo-1,3-diazepines, -oxazepines and -thiazepines from simple, commercially available anilines. The anilines were coupled to their corresponding reaction partners via a chloromethyl intermediate and the 7-membered ring was subsequently formed using direct arylation.