edited by Kumar G. Gadamasetti
Providing guidance for chemists and other scientists entering pharmaceutical
discovery and development, this up-to-the-minute reference presents contributions
from an international group of nearly 50 renowned researchers—offering a
solid grounding in synthetic and physical organic chemistry, and clarifying
the roles of various specialties in the development of new drugs.
Features:
- highlights new strategies for aggressive drug development programs
- provides 12 case studies on agents such as inhibitors and antagonists
- illustrates "green chemistry" and environmentally sound means of synthesizing new medicinal compounds
- describes asymmetric synthesis, enantioselectivity, and phase transfer catalysis
- explores crystallization and specifications for purity and rigorous new uses of physical/analytical chemistry in refining drugs
- reviews the trend toward drugs with wider varieties of heterocyclic functionality, chirality, and greater complex structural features
- explicates safety methods and design of experiments
- analyzes time-to-market schedules and consequences of acceleration of the development process in the pharmaceutical industry
- clarifies the misinterpretation of process chemistry as mere scale-up work
- examines the role of automation in contemporary experimental methodology
- and more!
Contains over 1000 references, tables, and illustrations.
Contents
- Strategy
Process Research and Development Strategy for Accelerated Projects
- Case Studies
A Practical Synthesis of Ifetroban Sodium
Synthesis of 5-Lipoxygenase Inhibitors
Chemistry of Vitamin D: A Challenging Field for Process Research
A Highly Optimized and Concise Large Scale Synthesis of a Purine Bronchodilator
Ontazolast: The Evolution of a Process
Dilevalol Hydrochloride: Development of a Commercial Process
Design and Development of Practical Syntheses of LY228729, a Potent 5HT1a Receptor Agonist
Process Research and Development of CGS 19755, an NMDA Antagonist
Route Evaluation for the Production of (R)-Levoprotiline
The Process Research and Development of DuPont Merck’s Cyclic Urea Diols, A New Class of HIV Protease Inhibitors
Practical Enantio- and Diastereo-selective Processes for Azetidinones
Synthesis of the Common Lactone Moiety of HMG-CoA Reductase Inhibitors
- Enzymatic Intervention and Phase Transfer Catalysis
Chemistry, Biocatalysis and Engineering: An Interdisciplinary Approach to the
Manufacture of the Benzodiazepine Drug Candidate LY 300164
Benefits and Challenges of Applying Phase-Transfer Catalysis Technology in the Pharmaceutical Industry
- Asymmetric Synthesis and Enantioselectivity
Enantioselective Synthesis: The Optimum Process
Practical Catalysts for Asymmetric Synthesis: Ligands from Natural Sugars for
Rh-Catalyzed Asymmetric Synthesis of D- and L- Amino Acids
Chiral (Salen)Mn(III) Complexes in Asymmetric Epoxidations: Practical Synthesis of
cis-Aminoindanol and Its Application to Enantiopure Drug Synthesis
- Drug Substance Final Form and Process Safety
Chemical Development of the Drug Substance Solid Form
The Basic Principles of Thermal Process Safety: Towards a
Better Communication Between Safety Experts and Process Chemists
- Design of Experiments and Automation
Using Factorial Experiments in the Development of Process Chemistry
Laboratory Automation in Chemical Development
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Index