Contemporary Drug Synthesis
Wiley Series on Drug Synthesis

1. Edition July 2004
240 Pages, Hardcover
Wiley & Sons Ltd
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.
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
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..." (href="http://www.organische-chemie.ch/">www.organische-chemie.ch)
'...I warmly recommend this book to synthetic organic
chemists both in industry and in academia.' (Organic Process
Research and Development Journal, July 2007)