Heterocyclic Chemistry in Drug Discovery

Jie Jack Li 지음

Wiley 2013년 04월 26일 출간

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Enables researchers to fully realize the potential to discover new pharmaceuticals among heterocyclic compoundsIntegrating 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 heterocyclesHeterocyclic 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.

목차

Chapter 1 Introduction 11.1 Nomenclature of Heterocycles 11.2 Aromatic Heterocycles 41.3 Importance of Heterocycles in Life 51.4 Importance of Heterocycles in Drug Discovery 8PART I FIVE-MEMBERED HETEROCYCLES WITH ONE HETEROATOM 17Chapter 2 Pyrroles 182.1 Introduction 182.2 Reactivity 222.3 Construction of the Pyrrole Rings 342.4 Palladium Chemistry of Pyrroles 442.5 Possible Liabilities of Pyrrole-Containing Drugs 462.6 Problems 492.7 References 51Chapter 3 Indoles 543.1 Introduction 543.2 Reactivity of the Indole Ring 583.3 Construction of the Indole Rings 643.4 Oxindole-Containing Drug Synthesis 883.5 Cross-coupling Reactions for Indoles 913.6 Azaindole 1043.7 Possible Liabilities of Drugs Containing 3-Methylindole 1093.8 Problems 1113.9 References 113Chapter 4 Furans, Benzofurans, Thiophenes, and Benzothiophenes 1194.1 Introduction 1194.2 Furans and Benzofuran 1264.3 Thiophenes and Benzothiophenes 1584.4 Possible Liabilities of Furan and Thiophene-Containing Drugs 1854.5 Problems 1874.6 References 191PART II FIVE-MEMBERED HETEROCYCLES WITH TWO OR MORE HETEROATOMS 197Chapter 5 Pyrazoles, Pyrazolones, and Indazoles 1985.1 Introduction 198 viii5.2 Reactivity of the Pyrazoles and Indazoles 2025.3 Construction of the Pyrazole and Indazole Rings 2065.4 Pyrazolone-containing Drugs 2175.5 Indazole-containing Drugs 2205.6 Problems 2235.7 References 226Chapter 6 Oxazoles, Benzoxazoles, and Isoxazoles 2316.1 Introduction 2316.2 Construction of the Heterocyclic Ring 2356.3 Reactivity 2446.4 Cross-Coupling Reactions 2506.5 Selected Reactions of Isoxazoles 2696.6 Possible Liabilities of Oxazole-Contain

출판사 서평

“In summary, both students and experts in the field would find useful information in this book.”& (ChemMedChem, 1 January 2014)“[Li] has assembled a team of 20 contributing authors from academia and the industry to write this book, which … comes across as a successful fusion of heterocyclic chemistry and drug discovery, from which intending medicinal chemists will derive much benefit, or as Li puts it, a ‘jump-start&' on the competition!.”& (Chemistry in Australia, 1 July 2013)&

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저자(글) Jie Jack Li

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JIE JACK LI, PhD, is a chemist at Bristol#45;Myers Squibb Company. He has authored or edited several books published by Wiley, including Name Reactions in Heterocyclic Chemistry, Name Reactions for Functional Group Transformations, Name Reactions for Homologations (Part I and Part ll ), Name Reactions for Carbocyclic Ring Formations, Contemporary Drug Synthesis, The Art of Drug Synthesis, and Modern Drug Synthesis.