Strategies for Organic Drug Synthesis and Design

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.

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.