Heterocyclic Chemistry in Drug Discovery

Detalles Bibliográficos
Autor principal: Li, Jie Jack
Formato: Electrónico eBook
Idioma:Inglés
Publicado: Newark : John Wiley & Sons, Incorporated, 2013.
Colección:New York Academy of Sciences Ser.
Temas:
Electronic books.
Acceso en línea:Texto completo
Tabla de Contenidos:
  • Cover
  • Title Page
  • Copyright Page
  • Contents
  • Preface
  • Contributing Authors
  • Chapter 1 Introduction
  • 1.1 Nomenclature of Heterocycles
  • 1.2 Aromaticity of Heterocycles
  • 1.3 Importance of Heterocycles in Life
  • 1.4 Importance of Heterocycles in Drug Discovery
  • 1.4.1 Five-Membered Heterocycles with One Heteroatom
  • 1.4.2 Five-Membered Heterocycles with Two Heteroatoms
  • 1.4.3 Six-Membered Heterocycles with One Heteroatom
  • 1.4.4 Six-Membered Heterocycles with Two Heteroatoms
  • PART I FIVE-MEMBERED HETEROCYCLES WITH ONE HETEROATOM
  • Chapter 2 Pyrroles
  • 2.1 Introduction
  • 2.2 Reactivity of the Pyrrole Ring
  • 2.2.1 Protonation
  • 2.2.2 C2 Electrophilic Substitution
  • 2.2.3 C3 Electrophilic Substitution
  • 2.2.4 Metalation
  • 2.3 Construction of the Pyrrole Rings
  • 2.3.1 Knorr Pyrrole Synthesis
  • 2.3.2 Paal-Knorr Pyrrole Synthesis
  • 2.3.3 Hantsch Pyrrole Synthesis
  • 2.3.4 Barton-Zard Reaction
  • 2.4 Palladium Chemistry of Pyrroles
  • 2.5 Possible Liabilities of Pyrrole-Containing Drugs
  • 2.6 Problems
  • 2.7 References
  • Chapter 3 Indoles
  • 3.1 Introduction
  • 3.2 Reactivity of the Indole Ring
  • 3.2.1 Protonation
  • 3.2.2 C3 Electrophilic Substitution
  • 3.2.3 C2 Electrophilic Substitution
  • 3.2.4 Metallation
  • 3.3 Construction of the Indole Rings
  • 3.3.1 Fischer Indole Synthesis
  • 3.3.2 Mori-Ban Indole Synthesis
  • 3.3.3 Larock Indole Synthesis
  • 3.3.4 Bischler-Möhlau Indole Synthesis
  • 3.3.5 Nenitzescu Indole Synthesis
  • 3.3.6 Bartoli Indole Synthesis
  • 3.3.7 Batcho-Leimgruber Indole Synthesis
  • 3.3.8 Gassman Indole Synthesis
  • 3.3.9 Cadogan-Sundberg Indole Synthesis
  • 3.4 Oxindole-containing Drug Synthesis
  • 3.5 Cross-coupling Reactions for Indoles
  • 3.5.1 Palladium-Catalyzed Oxidative Coupling
  • 3.5.2 Negishi Coupling
  • 3.5.3 Suzuki Coupling
  • 3.5.4 Sonogashira Coupling
  • 3.5.5 Heck Reaction
  • 3.6 Azaindoles
  • 3.6.1 Larock Reaction
  • 3.6.2 Bartoli Reaction
  • 3.6.3 Batcho-Leimgruber Reaction
  • 3.6.4 Cadogan-Sundberg Indole Synthesis
  • 3.7 Possible Liabilities of Drugs Containing 3-Methylindole
  • 3.8 Problems
  • 3.9 References
  • Chapter 4 Furans, Benzofurans, Thiophenes, and Benzothiophenes
  • 4.1 Introduction
  • 4.2 Furans and Benzofurans
  • 4.2.1 Reactions of Furans and Benzofurans
  • 4.2.2 Furan and Benzofuran Synthesis
  • 4.2.3 Synthesis of Furan- and Benzofuran-Containing Drugs
  • 4.3 Thiophenes and Benzothiophenes
  • 4.3.1 Reactions of Thiophene and Benzothiophene
  • 4.3.2 Synthesis of Thiophene and Benzothiophene
  • 4.3.3 Synthesis of Thiophene- and Benzothiophene-Containing Drugs
  • 4.4 Possible Liabilities of Furan- and Thiophene-Containing Drugs
  • 4.5 Problems
  • 4.6 References
  • PART II FIVE-MEMBERED HETEROCYCLES WITH TWO OR MORE HETEROATOMS
  • Chapter 5 Pyrazoles, Pyrazolones, and Indazoles
  • 5.1 Introduction
  • 5.1.1 Basicity and Acidity
  • 5.1.2 Tautomerization
  • 5.2 Reactivities of the Pyrazole Ring
  • 5.2.1 Alkylation of the Pyrazole Ring

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