Synthetic methods in drug discovery edited by David Blakemore (Pfizer Cambridge UK) ; volume 2 This book highlights key synthetic methodologies that have real impact in drug discovery and facilitate delivery of drug molecules 6.1.1 Overview of Pd catalysed C N Cross coupling6.1.2 Overview of Cu catalysed C N Cross coupling; 6.2 Primary and Secondary Aliphatic Amines; 6.3 Anilines and Amino Heterocycles; 6.4 Amides Sulfonamides and Other Weak N H Nucleophiles; 6.5 Azoles; 6.6 Ammonia Hydrazine and their Surrogates; 6.7 Summary and Outlook; References; Chapter 7 Chan Lam Coupling Reaction: Copper promoted C Element Bond Oxidative Coupling Reaction with Boronic Acids; 7.1 General Introduction; 7.2 C N Oxidative Coupling with Arylboronic Acids; 7.2.1 Recent C N Oxidative Coupling with Arylboronic Acids 7.2.2 Intramolecular C N Oxidative Coupling7.2.3 Recent Pharmaceutical Applications; 7.3 C O Oxidative Coupling with Arylboronic Acids; 7.3.1 Intramolecular C O Oxidative Coupling; 7.3.2 Pharmaceutical Applications; 7.4 C N and C O Oxidative Coupling with Alkenyl Alkyl and Alknylboronic Acids; 7.4.1 Boron Reagents; 7.5 Other C Element Oxidative Coupling (C S C P C F C Cl C Br C I C Se C Te C F C C C H); 7.6 Mechanistic Studies; 7.7 Future and Conclusions; Acknowledgments; References; Chapter 8 C H Activation Approaches to Molecules; 8.1 Introduction; 8.2 C H Arylation Cover; Contents; Preface; Chapter 1 Suzuki Miyaura Coupling; 1.1 Introduction; 1.2 The Catalytic Cycle of the SMC; 1.3 The Impact of the Ligand; 1.4 Electron rich Sterically Hindered Phosphine Ligands; 1.5 N Heterocyclic Carbene Ligands; 1.6 The Boronate Species; 1.7 Base and Solvent; 1.8 Optimal Reaction Conditions; 1.9 Examples of Process scale SMC Reactions; 1.10 Side Reactions in SMC Reactions; 1.10.1 Oxidation and Homo coupling; 1.10.2 Protodeboronation; 1.11 SMC Reactions of Dihalogenated Aromatic Systems; 1.12 SMC Reactions of Aryl Tosylates Mesylates and Diazonium Species Chapter 4 Sonogashira Coupling4.1 Introduction; 4.2 Development of the Sonogashira Reaction; 4.3 Mechanistic Aspects of the Reaction; 4.3.1 Typical Reaction Conditions; 4.4 Utility of the Sonogashira Reaction; 4.5 The Glaser Hay Coupling Reaction; 4.6 The Copper free Sonogashira Coupling Reaction; 4.7 Summary; Acknowledgments; References; Chapter 5 Heck Coupling; 5.1 Introduction; 5.2 Intermolecular Heck Couplings; 5.3 Intramolecular Heck Reactions; 5.4 Conclusion; References; Chapter 6 Palladium and Copper catalysed C N Cross coupling in Drug Discovery; 6.1 Introduction 1.13 Generation of Vinyl Cyclopropyl and Benzyl Derivatives1.14 Conclusion; References; Chapter 2 Negishi Coupling; 2.1 Introduction; 2.2 Mechanism; 2.3 Formation of Organozinc Reagents; 2.4 Applications in Drug Discovery; 2.4.1 sp3 sp3 Carbon Bond Formation; 2.4.2 sp3 sp2 Carbon Bond Formation; 2.4.3 sp2 sp2 Carbon Bond Formation; 2.5 Conclusion; References; Chapter 3 Hiyama Coupling; 3.1 Introduction; 3.2 Development of the Hiyama Coupling Reaction; 3.3 Mechanistic Considerations; 3.4 Fluoride free Hiyama Coupling; 3.5 Hiyama Denmark Coupling; 3.6 Summary; References