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 discoveryStep-by-step descriptions of synthetic methods and practical techniquesExamination of the physical properties for each heterocycle, including NMR data and quantum calculationsDetailed 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.
Summarizes for each drug: respective disease area, important properties and SAR (structure-activity relationship), and chemical synthesis routes / optionsIncludes case studies in each chapterIllustrates how chemistry, biology, pharmacokinetics, and a host of disciplines come together to produce successful medicinesExplains the advantages of process synthesis versus the synthetic route for drug discovery
Edited by Jie Jack Li and Nobel laureate E. J. Corey, two leading pioneers in drug discovery and medicinal chemistry, this book synthesizes great moments in history, the current state of the science, and future directions of drug discovery into one expertly written and organized work. Exploring all major therapeutic areas, the book introduces readers to all facets and phases of drug discovery, including target selection, biological testing, drug metabolism, and computer-assisted drug design.
Drug Discovery features chapters written by an international team of pharmaceutical and medicinal chemists. Contributions are based on a thorough review of the current literature as well as the authors' firsthand laboratory experience in drug discovery. The book begins with the history of drug discovery, describing groundbreaking moments in the field. Next, it covers such topics as:Target identification and validationDrug metabolism and pharmacokineticsCentral nervous system drugsIn vitro and in vivo assaysCardiovascular drugsCancer drugs
Each chapter features a case study, helping readers understand how science is put into practice throughout all phases of drug discovery. References at the end of each chapter serve as a gateway to groundbreaking original research studies and reviews in the field.
Drug Discovery is ideal for newcomers to medicinal chemistry and drug discovery, providing a comprehensive overview of the field. Veterans in the field will also benefit from the perspectives of leading international experts in all aspects of drug discovery.
These developments highlight the need for a monograph dedicated solely to the palladium chemistry in heterocycles and this book provides a comprehensive explanation of the subject. The principal aim of the book is to highlight important palladium-mediated reactions of heterocycles with emphasis on the unique characteristics of individual heterocycles.
1. Palladium chemistry of heterocycles has its “idiosyncrasies stemming from their different structural properties from the corresponding carbocyclic aryl compounds. Even activated chloroheterocycles are sufficiently reactive to undergo Pd-catalyzed reactions. As a consequence of &agr and &bgr activation of heteroaryl halides, Pd-catalyzed chemistry may take place regioselectively at the activated positions, a phenomenon rarely seen in carbocyclic aryl halides. In addition, another salient peculiarity in palladium chemistry of heterocycles is the so-called "heteroaryl Heck reaction". For instance, while intermolecular palladium-catalyzed arylations of carbocyclic arenes are rare, palladium-catalyzed arylations of azoles and many other heterocycles readily take place. Therefore, the principal aim of this book is to highlight important palladium-mediated reactions of heterocycles with emphasis on the unique characteristics of individual heterocycles. 2. A myriad of heterocycles are biologically active and therefore of paramount importance to medicinal and agricultural chemists. Many heterocycle-containing natural products (they are highlighted in boxes throughout the text) have elicited great interest from both academic and industrial research groups. Recognizing the similarities between the palladium chemistry of arenes and heteroarenes, a critical survey of the accomplishments in heterocyclic chemistry will keep readers abreast of such a fast-growing field. We also hope this book will spur more interest and inspire ideas in such an extremely useful area. This book comprises a compilation of important preparations of heteroaryl halides, boranes and stannanes for each heterocycle. The large body of data regarding palladium-mediated polymerization of heterocycles in material chemistry is not focused here; neither is coordination chemistry involving palladium and heterocycles. Many heterocycle-containing natural products (highlighted throughout the text) have elicited great interest from both academic and industrial research groups. Recognizing the similarities between the palladium chemistry of arenes and heteroarenes, a critical survey of the accomplishments in heterocyclic chemistry keeps readers abreast of this fast-growing field. It is also hoped that this book will stimulate more interest and inspire new ideas in this exciting area.Contains the most up-to-date developments in this fast-moving fieldIncludes 3 new chaptersIncorporates material from selected well-respected authors on heterocyclic chemistry
Unlike other books on name reactions in organic chemistry, Name Reactions, A Collection of Detailed Reaction Mechanisms and Synthetic Applications focuses on the reaction mechanisms. It covers over 320 classical as well as contemporary name reactions.
The field of heterocyclic chemistry has long presented a specialchallenge for chemists. Because of the enormous amount and varietyof information, it is often a difficult topic to cover forundergraduate and graduate chemistry students, even in simplifiedform. Yet the chemistry of heterocyclic compounds and methods fortheir synthesis form the bedrock of modern medicinal chemical andpharmaceutical research. Thus there is a great need for highquality, up-to-date, and authoritative books on heterocyclicsynthesis helpful to both the professional research chemist as wellas the advanced student.
Name Reactions in Heterocyclic Chemistry provides aone-stop repository for this important field of organic chemistry.The primary topics include three- and four-membered heterocycles,five-membered heterocycles including indoles, furans, thiophenes,and oxazoles, six-membered heterocycles including quinolines,isoquinolines, and pyrimidines, and other heterocycles.
Each name reaction is summarized in seven sections:DescriptionHistorical perspectiveMechanismVariations and improvementsSynthetic utilityExperimentalReferencesAuthored by a team of world-renowned contributors - some of whomhave discovered the very reactions they describe - NameReactions in Heterocyclic Chemistry represents astate-of-the-art resource for students and researchers alike.