Modern Drug Synthesis / Edition 1

Hardcover (Print)
Used and New from Other Sellers
Used and New from Other Sellers
from $92.22
Usually ships in 1-2 business days
(Save 26%)
Other sellers (Hardcover)
  • All (12) from $92.22   
  • New (9) from $98.13   
  • Used (3) from $92.22   

Overview

"The successor to tin- editors' two highly acclaimed works on drug synthesis, Contemporary Dntg Synthesis and The Art of Drag Synthesis, this book provides refoeused and extensive new coverage detailing how chemistry; biology, and pharmacokinetics integrate to spearhead successful medical findings. Modern Drug Synthesis carries on the mission of delivering the most up-to-date developments unfolding in this rapidly evolving field by placing a stronger emphasis on medicinal chemistry and pharmacology, in addition to drug synthesis." Modern Drug synthesis shows that whether durg synthesis is in early development or the process stage, the ability to design elegant and economical synthetic routes is often a major factor making a drug a commenrcial winner. Easy to follow and stacked with valuable information on the present and future direction of medicinal chemistry. Modern Drug Syntheis is the one guide that paints a clear and complete picture of this complex subject.

Read More Show Less

Editorial Reviews

From the Publisher
"All chapters are very well written, and the used schemes and tables are conveniently arranged. The information and explanations given are strengthened by well-chosen examples and so the reader can easily follow the discussion. The comprehensive referenced literature placed at the end of each chapter enables further reading, and a detailed keyword index in combination with a logically structured Table of Content allows fast access to the topic of interest." (ChemMedChem, 2010)
Read More Show Less

Product Details

  • ISBN-13: 9780470525838
  • Publisher: Wiley, John & Sons, Incorporated
  • Publication date: 8/9/2010
  • Series: Wiley Series on Drug Synthesis Series
  • Edition number: 1
  • Pages: 376
  • Product dimensions: 7.20 (w) x 10.00 (h) x 0.90 (d)

Meet the Author

JIE JACK LI is a chemist at Bristol-Myers Squibb Company in Wallingford, Connecticut. He is the coauthor of various books, including Palladium in Heterocyclic Chemistry, Name Reactions: A Collection of Detailed Reaction Mechanisms and Synthetic Applications, Name Reactions in Heterocyclic Chemistry, Contemporary Drug Synthesis, The Art of Drug Synthesis, Name Reactions for Functional Group Transformations, Name Reactions for Homologations, Parts 1 and 2, and Name Reactions for Carbocyclic Ring Formations.

DOUGLAS JOHNSON is a medicinal chemist and project leader at Pfizer in Groton, Connecticut. He is a coauthor on more than forty publications and patents, including the books The Art of Drug Synthesis and Contemporary Drug Synthesis.

Read More Show Less

Table of Contents

Preface

Contributors

I Infectious Diseases 1

Chapter 1 Raltegravir (Isentress): The First-in-Class HIV-1 Integrase Inhibitor Julianne A. Hunt Hunt, Julianne A. 3

1.1 Background 3

1.2 Pharmacology 5

1.3 Structure-Activity Relationship (SAR) 6

1.4 Pharmacokinetics and Drug Metabolism 8

1.5 Efficacy and Safety 9

1.6 Syntheses 10

1.7 References 13

Chapter 2 Maraviroc (Selzentry): The First-in-Class CCR5 Antagonist for the Treatment of HIV David Price Price, David 17

2.1 Background 17

2.2 Structure-Activity Relationship (SAR) 19

2.3 Pharmacokinetics and Safety 21

2.4 Syntheses 22

2.5 References 27

Chapter 3 Darunavir (Prezista): A HIV-1 Protease Inhibitor for Treatment of Multidrug Resistant HIV Cuthbert D. Martyr Martyr, Cuthbert D. 29

3.1 Background 29

3.2 Pharmacology 32

3.3 Structure-Activity Relationship (SAR) 32

3.4 Pharmacokinetics and Drug Metabolism 33

3.5 Efficacy and Safety 33

3.6 Syntheses 34

3.7 References 42

II Cancer

Chapter 4 Decitabine (Dacogen): A DNA Methyltransferase Inhibitor for Cancer Jennifer A. Van Camp Van Camp, Jennifer A. 47

4.1 Background 47

4.2 Pharmacology 49

4.3 Structure-Activity Relationship (SAR) 49

4.4 Pharmacokinetics and Drug Metabolism 50

4.5 Efficacy and Safety 50

4.6 Syntheses 51

4.7 References 54

Chapter 5 Capecitabine (Xeloda): An Oral Chemotherapy Agent R. Jason Herr Herr, R. Jason 57

5.1 Background 57

5.2 Pharmacology 60

5.3 Structure-Activity Relationship (SAR) 62

5.4 Pharmacokinetics and Efficacy 63

5.5 Syntheses 64

5.6 References 70

Chapter 6 Sorafenib (Nexavar): A Multikinase Inhibitor for Advanced Renal Cell Carcinoma and Unresectable Hepatocellular Carcinoma Yazhong Huang Huang, Yazhong 73

6.1 Background 73

6.2 Pharmacology 75

6.3 Structure-Activity Relationship (SAR) 77

6.4 Pharmacokinetics and Drug Metabolism 78

6.5 Efficacy and Safety 78

6.6 Syntheses 79

6.7 References 84

Chapter 7 Sunitinib (Sutent): An Angiogenesis Inhibitor Martin Pettersson Pettersson, Martin 87

7.1 Background 87

7.2 Discovery and Development 89

7.3 Syntheses 91

7.3.1 Discovery Route 91

7.3.2 Process Route 92

7.4 References 97

Chapter 8 Bortezomib (Velcade): A First-in-Class Proteasome Inhibitor David S. Millan Millan, David S. 99

8.1 Background 99

8.2 Pharmacology 101

8.3 Structure-Activity Relationship (SAR) 102

8.4 Pharmacokinetics and Drug Metabolism 104

8.5 Efficacy and Safety 104

8.6 Syntheses 105

8.7 References 109

Chapter 9 Pazopanib (Votrient): A VEGFR Tyrosine Kinase Inhibitor for Cancer Jie Jack Li Jie, Jack Li 111

9.1 Background 111

9.2 Pharmacology 113

9.3 Structure-Activity Relationship (SAR) 114

9.4 Pharmacokinetics and Drug Metabolism 117

9.5 Efficacy and Safety 118

9.6 Syntheses 118

9.7 Other VEGFR Inhibitors in Development: Vandetanib and Cediranib 120

9.8 References 121

III Cardiovascular and Metabolic Diseases 123

Chapter 10 Sitagliptin (Januvia): A Treatment for Type 2 Diabetes Joseph D. Armstrong III Armstrong, Joseph D., III 125

10.1 Background 125

10.2 Pharmacology 126

10.3 Structure-Activity Relationship (SAR) 127

10.4 Pharmacokinetics and Drug Metabolism 128

10.5 Efficacy and Safety 129

10.6 Syntheses 130

10.7 References 138

Chapter 11 Aliskiren (Tekturna), The First-in-Class Renin Inhibitor for Hypertension Victor J. Cee Cee, Victor J. 141

11.1 Background 141

11.2 Pharmacology 144

11.3 Structure-Activity Relationship (SAR) 145

11.4 Pharmacokinetics and Drug Metabolism 146

11.5 Efficacy and Safety 147

11.6 Syntheses 148

11.7 References 156

Chapter 12 Vernakalant (Kynapid): An Investigational Drug for the Treatment of Atrial Fibrillation David L. Gray Gray, David L. 159

12.1 Background 159

12.2 Pharmacology 163

12.3 Structure-Activity Relationship (SAR) 163

12.4 Pharmacokinetics and Drug Metabolism 164

12.5 Efficacy and Safety 165

12.6 Syntheses 166

12.7 References 171

Chapter 13 Conivaptan (Vaprisol), Vasopressin Via and V2 Antagonist for Hyponatremia Brian A. Lanman Lanman, Brian A. 175

13.1 Background 175

13.2 Pharmacology 177

13.3 Structure-Activity Relationship (SAR) 179

13.4 Pharmacokinetics and Drug Metabolism 181

13.5 Efficacy and Safety 182

13.6 Syntheses 183

13.7 References 189

Chapter 14 Rivaroxaban (Xarelto): A Factor Xa Inhibitor for the Treatment of Thrombotic Events Jason Crawford Crawford, Jason 191

14.1 Background 191

14.2 Pharmacology 193

14.3 Structure-Activity Relationship (SAR) 194

14.4 Pharmacokinetics and Drug Metabolism 196

14.5 Efficacy and Safety 197

14.6 Syntheses 198

14.7 Compounds in Development: Apixaban and Otamixaban 203

14.8 References 204

Chapter 15 Endothelin Antagonists for the Treatment of Pulmonary Arterial Hypertension David J. Edmonds Edmonds, David J. 207

15.1 Background 208

15.2 Treatment of PAH 209

15.3 Endothelin Antagonists 211

15.4 Synthesis of Bosentan 215

15.5 Synthesis of Sitaxsentan 217

15.6 Synthesis of Ambrisentan 219

15.7 Conclusion 221

15.8 References 221

IV Central Nervous System Diseases 225

Chapter 16 Varenicline (Chantix), An α4β2 Nicotinic Receptor Partial Agonist for Smoking Cessation Robert A. Singer Singer, Robert A. 227

16.1 Background 227

16.2 Discovery Chemistry Program 229

16.3 Pharmacology 231

16.4 Pharmacokinetics and Drug Metabolism 231

16.5 Efficacy and Safety 232

16.6 Syntheses 232

16.7 References 244

Chapter 17 Donepezil, Rivastigmine, and Galantamine: Cholinesterase Inhibitors for Alzheimer Disease Kapil Karki Karki, Kapil 249

17.1 Background 250

17.2 Pharmacology 251

17.3 Structure-Activity Relationship (SAR) 253

17.4 Pharmacokinetics and Drug Metabolism 256

17.5 Efficacy and Safety 258

17.6 Synthesis of Donepezil 259

17.7 Synthesis of Rivastigmine 262

17.8 Synthesis of Galantamine 265

17.9 References 271

Chapter 18 Aprepitant (Emend): A NKi Receptor Antagonist for the Treatment of Postchemotherapy Emesis John A. Lowe III Lowe, John A., III 275

18.1 Background 275

18.2 In Vitro Pharmacology and Structure-Activity Relationships 279

18.3 In Vivo Pharmacology 281

18.4 Pharmacokinetics and Drug Metabolism 282

18.5 Efficacy and Safety 282

18.6 Syntheses 283

18.7 References 289

Chapter 19 Armodafinil (Nuvigil): A Psychostimulant for the Treatment of Narcolepsy Jason Crawford Crawford, Jason 291

19.1 Background 291

19.2 Pharmacology 293

19.3 Pharmacokinetics and Drug Metabolism 294

19.4 Efficacy and Safety 295

19.5 Synthesis 296

19.6 References 303

V Miscellaneous 307

Chapter 20 Raloxifene (Evista): A Selective Estrogen Receptor Modulator (SERM) Marta Pineiro-Nunez Pineiro-Nunez, Marta 309

20.1 Background 309

20.2 Mechanism of Action 313

20.3 Pharmacokinetics and Drag Metabolism 313

20.4 Efficacy and Safety 314

20.5 Syntheses 315

20.6 References 325

Chapter 21 Latanoprost (Xalatan): A Prostanoid FP Agonist for Glaucoma Kevin E. Henegar Henegar, Kevin E. 329

21.1 Background 329

21.2 Syntheses 331

21.3 References 337

Index 339

Read More Show Less

Customer Reviews

Be the first to write a review
( 0 )
Rating Distribution

5 Star

(0)

4 Star

(0)

3 Star

(0)

2 Star

(0)

1 Star

(0)

Your Rating:

Your Name: Create a Pen Name or

Barnes & Noble.com Review Rules

Our reader reviews allow you to share your comments on titles you liked, or didn't, with others. By submitting an online review, you are representing to Barnes & Noble.com that all information contained in your review is original and accurate in all respects, and that the submission of such content by you and the posting of such content by Barnes & Noble.com does not and will not violate the rights of any third party. Please follow the rules below to help ensure that your review can be posted.

Reviews by Our Customers Under the Age of 13

We highly value and respect everyone's opinion concerning the titles we offer. However, we cannot allow persons under the age of 13 to have accounts at BN.com or to post customer reviews. Please see our Terms of Use for more details.

What to exclude from your review:

Please do not write about reviews, commentary, or information posted on the product page. If you see any errors in the information on the product page, please send us an email.

Reviews should not contain any of the following:

  • - HTML tags, profanity, obscenities, vulgarities, or comments that defame anyone
  • - Time-sensitive information such as tour dates, signings, lectures, etc.
  • - Single-word reviews. Other people will read your review to discover why you liked or didn't like the title. Be descriptive.
  • - Comments focusing on the author or that may ruin the ending for others
  • - Phone numbers, addresses, URLs
  • - Pricing and availability information or alternative ordering information
  • - Advertisements or commercial solicitation

Reminder:

  • - By submitting a review, you grant to Barnes & Noble.com and its sublicensees the royalty-free, perpetual, irrevocable right and license to use the review in accordance with the Barnes & Noble.com Terms of Use.
  • - Barnes & Noble.com reserves the right not to post any review -- particularly those that do not follow the terms and conditions of these Rules. Barnes & Noble.com also reserves the right to remove any review at any time without notice.
  • - See Terms of Use for other conditions and disclaimers.
Search for Products You'd Like to Recommend

Recommend other products that relate to your review. Just search for them below and share!

Create a Pen Name

Your Pen Name is your unique identity on BN.com. It will appear on the reviews you write and other website activities. Your Pen Name cannot be edited, changed or deleted once submitted.

 
Your Pen Name can be any combination of alphanumeric characters (plus - and _), and must be at least two characters long.

Continue Anonymously

    If you find inappropriate content, please report it to Barnes & Noble
    Why is this product inappropriate?
    Comments (optional)