The Organic Chemistry of Drug Synthesis / Edition 1

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Overview

The seventh volume in The definitive series that provides a quick yet thorough overview of the synthetic routes used to access specific classes of therapeutic agents, this volume covers approximately 220 new non-proprietary drug entities introduced since the publication of Volumes 6. Many of these compounds represent novel structural types first identified by sophisticated new cell-based assays. Specifically, a significant number of new antineoplastic and antiviral agents are covered.

As in the previous volumes, materials are organized by chemical class and syntheses originate with available starting materials. Organized to make the information accessible, this resource covers disease state, rationale for method of drug therapy, and the biological activities of each compound and preparation. The Organic Chemistry of Drug Synthesis, Volume 7 is a hands-on reference for medicinal and organic chemists, and a great resource for graduate and advanced undergraduate students in organic and medicinal chemistry.

About the Author:
Daniel Lednicer, PhD, was a project officer at the National Cancer Institute

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Editorial Reviews

Booknews
The series meets the needs of practitioners in the field who seek a quick overview of the synthetic routes that have been used to access specific classes of therapeutic agents. Volume 5 covers the literature on the synthesis of medicinal agents from 1988 to 1993. The materials are arranged and discussed in terms of chemical structure; thus, the preparation and detailed organic chemistry of the classes are presented in a unified way. Only drugs which have been granted a US Adopted Name are included. For synthetic organic, pharmaceutical, medicinal, and heterocyclic chemists. Annotation c. Book News, Inc., Portland, OR (booknews.com)
From the Publisher
"The book is up-to-date with regard to the drugs presented and has the potential to be a good resources for experienced researchers in drug design…" (Journal of the American Chemical Society, March 12, 2008)
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Product Details

Meet the Author

Daniel Lednicer, PhD, is the author of several books on drug synthesis and discovery. His career in both the private and public sectors has been devoted to the search for new therapeutic agents. Dr. Lednicer spent two decades at the bench as a chemist at the Upjohn Company. Following that, he served as director of chemical research at Mead Johnson, director of pharmaceutical sciences at Adria Laboratories, and pharmaceutical manager at Analytical Biochemistry Laboratories. Most recently, he was a project officer at the National Cancer Institute.

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Table of Contents


Preface     xi
Open-Chain Compounds     1
Peptidomimetic Compounds     2
Antiviral Protease Inhibitors     2
Human Immunodeficiency Virus     2
Human Rhinovirus j     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
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