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Contemporary Drug Synthesis



Contemporary Drug Synthesis

Jie Jack Li, Douglas S. Johnson, Drago R. Sliskovic, Bruce D. Roth

ISBN: 978-0-471-68673-6 December 2004 240 Pages

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An integrated and insightful look at successful drug synthesis in today's drug discovery market

The pharmaceutical industry is unquestionably vibrant today, with drug synthesis making a vital contribution. Whether in the early developmental stages of identifying and optimizing a lead, or the latter stages of process development and cost-effective scale-up, the ability to design elegant and economical synthetic routes is often a major factor in the eventual viability and commercial success of a drug.

Contemporary Drug Synthesis examines how leading researchers and manufacturers have integrated chemistry, biology, pharmacokinetics, and a host of other disciplines in the creation and development of leading drugs.

Authored by four of the pharmaceutical industry's most respected scientists, this timely volume:

  • Focuses on the processes that resulted in high-profile drugs including Lipitor, Celebrex, Viagra, Gleevec, Nexium, Claritin, and over a dozen others
  • Provides an in-depth introduction to each drug, followed by a detailed account of its synthesis
  • Organizes the drugs into fourteen therapeutic areas for clarity and ease of use
Process chemists provide an essential bridge between chemistry and the marketplace, creating scientifically practical drug processes while never losing sight of the commercial viability of those processes. Contemporary Drug Synthesis meets the needs of a growing community of researchers in pharmaceutical research and development, and is both a useful guide for practicing pharmaceutical scientists and an excellent text for medicinal and organic chemistry students.
Preface v

Trade Names and Their Corresponding USANs xi

Acronyms and Abbreviations xiii

Chapter 1. Antithrombotics: Ticlopidine (Ticlid) and Clopidogrel (Plavix) 1

Chapter 2. Anti-inflammatory Cyclooxygenase-2 Selective Inhibitors: Celecoxib (Celebrex) and Rofecoxib (Vioxx) 11

Chapter 3. H+/K+ -ATPase Inhibitors: Esomeprazole (Nexium) 21

Chapter 4. Protein-tyrosine Kinase Inhibitors: Imatnib (Gleevec) and Gefitinib (Iressa) 29

Chapter 5. Non-sedating Antihistamines 39

Chapter 6. Cosmeceuticals: Istretinoin (Accutane), Tazarotene (Tazorac), Minoxidil (Rogaine), and Finasteride (Propecia) 55

Chapter 7. Antibacterials: Ciprofloxacin (Cipro) and Linezolid (Zyvox) 75

Chapter 8. Atypical Antupsychotics 89

Chapter 9. Atovastatin Calcium (Lipitor) 113

Chapter 10. Antidepressants 125

Chapter 11. Anti-obesity: Orlistat (Xenical) 149

Chapter 12. Triptans for Migrane 161

Chapter 13. PDE 5 Inhibitors for Erectile Dysfunction: Sildenafil (Viagra), Vardenafil (Levitra), and Tadalafil (Cialis) 189

Chapter 14. Antiasthmatics 201

Index 214

“…the authors have made an excellent selection of drugs and the coverage of the synthetic chemistry employed in their production is exemplary…” (Chemistry & Industry, 5th September 2005)

"…a clear and easy to use reference for anyone working in drug discovery and development." (E-STREAMS, January 2005)

"...a very useful book...for...pharmaceutical industry scientists...[and] the larger medicinal and organic chemistry community..." (Journal of Medicinal Chemistry, November 18, 2004)

"…an outstanding primer on methods for chemical drug synthesis…the test is most useful, well written, and serves as a useful read for those interested in drug synthesis." (American Journal of Therapeutics, September/October 2004)

“…highly interesting…keeps to the facts…” (

‘…I warmly recommend this book to synthetic organic chemists both in industry and in academia.' (Organic Process Research and Development Journal, July 2007)