Strategies for Organic Drug Synthesis and Design

by Daniel Lednicer

Overview

This book examines and evaluates the strategies utilized to design and synthesize pharmaceutically active agents. Significant updates over the last 10 years since the publication of the 1st edition include synthesis of enantiomerically pure isomers, novel chemical methodologies, and new pharmaceutical agents targeted at novel biological endpoints. Written by an experienced successful author, this book meets the needs of a growing community of researchers in pharmaceutical R &D, as well as medical professionals, by providing a useful guide for designing and synthesizing pharmaceutical agents. Additionally, it is a useful text for medicinal chemistry students.

Product Details

ISBN-13:	9780470190395
Publisher:	Wiley
Publication date:	10/27/2008
Edition description:	2nd ed.
Pages:	700
Product dimensions:	6.40(w) x 9.30(h) x 1.50(d)

About the Author

Daniel Lednicer, PhD, is the acclaimed author of several books on drug synthesis and discovery. His career 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. He has also 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

1. PROSTAGLANDINS, PEPTIDOMIMETIC COMPOUNDS, AND RETINOIDS.

1.1 Prostaglandnis.

1.2 Peptidonimetic Compounds.

1.3 Retinoids.

1.4 A Miscellaneous Drug.

References.

2. DRUG BASED ON A SUBSTITUTED BENZENE RING

2.1 Arylethanolamines.

2.2 Aryloxypropanolamines.

2.3 Arylsulfonic Acid Derivatives.

2.4 Arylacetic and Arylpropionic Acids.

3. INDENES, NAPHTHALENES AND OTHER POLYCYCLIC AROMATIC COMPOUNDS

3.1 Indenes.

3.2 Naphthalenes.

3.3 Partly Reduced Naphthalenes.

3.4 Tricyclic Compounds.

References.

4. STEROIDS; PART 1: ESTRANES, GONANES, AND ANDROSTANES

4.1 Introduction.

4.2 Steroid Starting Materials.

4.3 Estranes.

4.4 Gonanes, the 19-nor Steroids.

4.5 Androstanes.

References.

5. STEROIDS; PART 2: COMPOUNDS RELATED TO PROGESTERONE, CORTISONE, AND CHOLESTEROL.

5.1 Introduction.

5.2 Progestins.

5.3 Corticosteroids.

5.4 Compounds Derived from Cholesterol.

References.

6. NONSTEROIDAL SEX HORMONES AND THEIR ANTAGONISTS

6.1 Introduction.

6.2 Estrogens.

References.

7. OPIOID ANAlGESICS

7.1 Introduction

7.2 Drugs Derived from Morphine.

7.3 Compounds Prepared from Thebaine.

7.4 Morphinans.

7.5 Benzomorphans.

7.6 Analgesics Based on Nonfused Piperidines.

References.

8. DRUGS BASED ON FIVE-MEMBERED HETEROCYCLES

8.1 Introduction.

8.2 Rings that Contain One Heteroatom.

8.3 Rings that Contain Two Heteroatoms.

8.4 Rings that Contains Three or More Heteroatoms.

References.

9. DRUGS BASED ON SIX-MEMBERED HETEROCYCLES.

9.1 Rings that Contain One Heteroatom.

9.2 Rings that Contain Two Heteroatoms.

9.3 Rings Containing Three Heteroatoms: The Triazines.

References.

10. FIVE-MEMBERED HETEROCYCLES FUSED TO A BENZENE RING.

10.1 Compounds that Contain One Heteroatom.

10.2 Compounds that Contain Two Heteroatoms.

10.3 Compounds that Contain Three Heteroatoms.

References.

11. SIX-MEMBERED HETEROCYCLES FUSED TO A BENZENE RING

11.1 Compounds that Contain One Heteroatom.

11.2 Compounds that Contain Two Heteroatoms.

11.3 Compounds that Contain Three Heteroatoms.

References.

12. SEVEN-MEMBERED HETEROCYCLIC FUSED TO BENZENE.

12.1 Compounds with a Single Heterocyclic Atom.

12.2 Compounds with Two Heteroatoms.

References.

13. HETEROCYLES FUSED TO TWO AROMATIC RINGS

13.1 Compounds Containing a Single Heteroatom.

13.2 Compounds Containing Two Heteroatoms.

13.3 Pyridine-Based Fused Tricyclic Compounds.

References.

14. BETA LACTAM ANTIBIOTICS

14.1 Penicillins.

14.2 Cephalosporins.

14.3 Monobactams.

References.

15. HETEROCYCLES FUSED TO OTHER HETEROCYCLIC RINGS.

15.1 Two Fused Five-Membered Rings.

15.2 Five-Membered Heterocycles Fused to Six-Membered Rings.

15.3 Two Fused Six-Membered Rings.

15.4 Heterodiazepines.

15.5 Heterocyclic Compounds with Three or More Rings.

References.

Subject Index.

Reaction Index.

Cross Index of Biological Activities.

What People are Saying About This

From the Publisher

'In this book, Lednicer presents a detailed discussion of strategies toward the synthesis of pharmaceutical compounds. . . The strength of the book is the wealth of data collected in one relatively short tone?.

Editorial Reviews

'In this book, Lednicer presents a detailed discussion of strategies toward the synthesis of pharmaceutical compounds. . . The strength of the book is the wealth of data collected in one relatively short tone?.

From the Publisher

Presents a selection of syntheses from the five-volume series , chosen to illustrate the strategy and organic transformation used to prepare various structural classes investigated as drugs. Focus is on agents that have been granted nonproprietary names, and drugs have been selected mainly for illustrative value of the chemistry used for synthesis. Discusses biological rationales for drug classes and actions of individual agents, and offers capsule presentations of basic principles of drug action. Includes reaction flow charts detailing routes used to prepare some 600 compounds, plus a reaction index. For those working in organic, medicinal, and pharmaceutical chemistry. Annotation c. by Book News, Inc., Portland, Or.

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