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The Organic Chemistry of Drug Synthesis, 4 Volume Set




The Organic Chemistry of Drug Synthesis, 4 Volume Set

Daniel Lednicer (Editor), Lester A. Mitscher (Editor)

ISBN: 978-0-471-53176-0 April 1991 1616 Pages


Updated every five years, the series represents the optimal compromise between currency and a sufficient body of material for cohesive and comprehensive treatment in a monograph. Provides a quick yet thorough overview of the synthetic routines that have been used to access specific classes of therapeutic agents. Materials are organized by chemical class, and syntheses are taken back to available starting materials. Discusses disease state, rational for method of drug therapy, biological activities of each compound and preparation. Coverage also includes those generic pharmaceutical compounds not accorded clinical status. A glossary defines biological terms.
Preface xi

Open-Chain Compounds 1

Peptidomimetic Compounds 2

Antiviral Protease Inhibitors 2

Human Immunodeficiency Virus 2

Human Rhinovirus 9

Miscellaneous Peptidomimetic Compounds 11

References 19

Alicyclic Compounds 21

Monocyclic Compounds 21

Prostaglandins 21

Antiviral Agents 25

Miscellaneous Monocyclic Compounds 29

Polycyclic Compounds: Steroids 31

19-Nor Steroids 31

Corticosteroid Related Compounds 34

Polycyclic Compounds / 38

References 40

Monocyclic Aromatic Compounds 43

Arylcarbonyl Derivatives 43

Biphenyls 47

Compounds Related to Aniline 50

Compounds Related to Arylsulfonic Acids 53

Diarylmethanes 58

Miscellaneous Monocyclic Aromatic Compounds 60

References 67

Carbocyclic Compounds Fused to a Benzene Ring 69

Indenes 69

Naphthalenes 73

Tetrahydronaphthalenes 74

Other benzofused carbocyclic compounds 79

References 81

Five-Membered Heterocycles 83

Compounds with One Heteroatom 83

Compounds with Two Heteroatoms 91

Oxazole and Isoxazoles 91

Imidazoles and a Pyrrazole 94

Thiazoles 99

Triazoles 103

Tetrazoles 109

References 112

Six-Membered Heterocycles 115

Compounds with One Heteroatom 115

Pyridines 115

Reduced Pyridines 117

Miscellaneous 119

Compounds with Two Heteroatoms 121

Pyrimidines 121

Miscellaneous Six-Membered Heterocycles 133

References 136

Five-Membered Heterocycles Fused to One Benzene Ring 139

Compounds with One Heteroatom 139

Benzofurans 139

Indoles 141

Indolones 148

Miscellaneous Compounds with One Heteroatom 153

Five-Membered Rings with Two Heterocyclic Atoms 156

Benzimidazoles 156

Miscellaneous Compounds  158

References 160

Six-Membered Heterocycles Fused to One Benzene Ring 163

Compounds with One Heteroatom 163

Benzopyrans 163

Quinolines and Their Derivatives 167

Quinolone Antibacterial Agents 172

Compounds with Two Heteroatoms 176

Benzoxazines 176

Quinazolines 178

Miscellaneous Benzo-Fused Heterocycles 184

References 186

Bicyclic Fused Heterocycles 189

Compounds with Five-Membered Rings Fused to Six-Membered Rings 189

Compounds with Two Heteroatoms 189

Compounds with Three Heteroatoms 191

Compounds with Four Heteroatoms 195

Compounds with Two Fused Six-Membered Rings 208

Miscellaneous Compounds with Two Fused Heterocyclic Rings: Beta Lactams 213

References 215

Polycyclic Fused Heterocycles 217

Compounds with Three Fused Rings 217

Compounds with Four Fused Rings 228

Compounds with Five or More Fused Rings: Camptothecins 230

References 232

Subject Index 233

Cross Index of Biological Activity  241

Cumulative Index 245