The Art of Drug Synthesis

The Art of Drug Synthesis illustrates how chemistry, biology, pharmacokinetics, and a host of other disciplines come together to produce successful medicines. The authors have compiled a collection of 21 representative categories of drugs, from which they have selected as examples many of the best-selling drugs on the market today. An introduction to each drug is provided, as well as background to the biology, pharmacology, pharmacokinetics, and drug metabolism, followed by a detailed account of the drug synthesis. Edited by prominent scientists working in drug discovery for Pfizer Meets the needs of a growing community of researchers in pharmaceutical R&D Provides a useful guide for practicing pharmaceutical scientists as well as a text for medicinal chemistry students An excellent follow-up to the very successful first book by these editors, Contemporary Drug Synthesis, but with all new therapeutic categories and drugs discussed.

Douglas S. Johnson, PHD, is a Research Chemist at Pfizer Global Research and Development.

Jie Jack Li, PHD, is a Research Chemist at Pfizer Global Research and Development.

Foreword
Preface
Contributors
The Role of Medicinal Chemistry in Drug Discovery
Introduction
Hurdles in the Drug Discovery Process
The Tools of Medicinal Chemistry
In Silico Modeling
Structure-Based Drug Design (SBDD)
The Role of Synthetic Chemistry in Drug Discovery
References
Process Research: How Much? How Soon?
Introduction
Considerations for Successful Scale-up to Tox Batches and Phase I Material
Considerations for Phase 2 Material and Beyond
Reagent Selection
Solvent Selection
Unit Operations
Developing Simple, Effective, Efficient Work-ups and Isolations
The Importance of Physical States
Route Design and Process Optimization to Minimize COG
Summary
References
Cancer and Infectious Diseases
Aromatase Inhibitors for Breast Cancer: Exemestane (Aromasin), Anastrozole (Arimidex), and Letrozole (Femara)
Introduction
Synthesis of Exemestane
Synthesis of Anastrozole
Synthesis of Letrozole
References
Quinolone Antibiotics: Levofloxacin (Levaquin), Moxifloxacin (Avelox), Gemifloxacin (Factive), and Garenoxacin (T-3811) (
Introduction
Mechanism of Action
Modes of Resistance
Structure-Activity Relationship (SAR) and Structure-Toxicity Relationship (STR)
Pharmacokinetics
Synthetic Approaches
Levofloxacin
Moxifloxacin
Gemifloxacin
Garenoxacin (T-3811): A Promising Clinical Candidate
References
Triazole Antifungals: Itraconazole (Sporanox), Fluconazole (Diflucan), Voriconazole (Vfend), and Fosfluconazole (Prodif) (
Introduction
Synthesis of Itraconazole
Synthesis of Fluconazole
Synthesis of Voriconazole
Synthesis of Fosfluconazole
References
Non-Nucleoside HIV Reverse Transcriptase Inhibitors
Introduction
Synthesis of Nevirapine
Synthesis of Efavirenz
Synthesis of Delavirdine Mesylate
References
Neuraminidase Inhibitors for Influenza: Oseltamivir Phosphate (Tamiflu) And Zanamivir (Relenza)
Introduction
Relenza
Tamiflu
Synthesis of Oseltamivir Phosphate
Synthesis of Zanamivir
References
Cardiovascular and Metabolic Diseases
Peroxisome Proliferator-Activated Receptor (Ppar) Agonists for Type 2 Diabetes
Introduction
Insulin
Sulfonylurea Drugs
Meglitinides
Biguanides
Alpha-Glucosidase Inhibitors
Thiazolidinediones
Synthesis of Rosiglitazone
Synthesis of Pioglitazone
Synthesis of Muraglitazar
References
Angiotensin at 1 Antagonists for Hypertension
Introduction
Losartan Potassium
Introduction to Losartan Potassium
Synthesis of Losartan Potassium
Valsartan
Introduction to Valsartan
Synthesis of Valsartan
Irbesartan
Introduction to Irbesartan
Synthesis of Irbesartan
Candesartan Cilexetil
Introduction to Candesartan Cilexetil
Synthesis of Candesartan Cilexetil
Olmesartan Medoxomil
Introduction to Olmesartan Medoxomil
Synthesis of Olmesartan Medoxomil
Eprosartan Mesylate
Introduction to Eprosartan Mesylate
Synthesi
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The Art of Drug Synthesis

Summary

Author Biography

Table of Contents

Supplemental Materials