1st Edition

Process Chemistry in the Pharmaceutical Industry

Edited By Kumar Gadamasetti Copyright 1999

    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.

    Featuring over 1000 references, tables, and illustrations, Process Chemistry in the Pharmaceutical Industry is sure to find its way to the bookshelves of organic, physical, analytical, process, and medicinal chemists and biochemists; pharmacists; and upper-level undergraduate and graduate students in these disciplines.


    Process Chemistry in the Pharmaceutical Industry: An Overview, Kumar G. Gadamasetti


    Process Research and Development Strategy for Accelerated Projects, Christopher M. Cimarusti

    Case Studies

    A Practical Synthesis of Ifetroban Sodium, Richard H. Mueller
    Synthesis of 5-Lipoxygenase Inhibitors, Ivan Lantos and Richard Matsuoka
    Chemistry of Vitamin D: A Challenging Field for Process Research, Masami Okabe
    A Highly Optimized and Concise Large Scale Synthesis of a Purine Bronchodilator, Hans-Jürgen Federsel and Edib Jakupovic
    Ontazolast: The Evolution of a Process, Vittorio Farina, Karl Grozinger, Hermann Müller-Bötticher and Gregory P. Roth
    Dilevalol Hydrochloride: Development of a Commercial Process, Derek Walker
    Design and Development of Practical Syntheses of LY228729, a Potent 5HT1a Receptor Agonist, Michael J. Martinelli and David L. Varie
    Process Research and Development of CGS 19755, an NMDA Antagonist, Peter Giannousis, John Carlson and Marius Leimer
    Route Evaluation for the Production of (R)-Levoprotiline, H. U. Blaser, R. Gamboni, B. Pugin, G. Rihs, G. Sedelmeier, E. Schaub, E. Schmidt, B. Schmitz, F. Spindler and Hj. Wetter
    The Process Research and Development of DuPont Merck’s Cyclic Urea Diols, A New Class of HIV Protease Inhibitors, Pat N. Confalone and Robert E. Waltermire
    Practical Enantio- and Diastereo-selective Processes for Azetidinones, T. K. Thiruvengadam, Anantha R. Sudhakar, and Guangzhong Wu
    Synthesis of the Common Lactone Moiety of HMG-CoA Reductase Inhibitors, Ian M. McFarlane, Christopher G. Newton and Philippe Pitchen

    Enzymatic Intervention and Phase Transfer Catalysis

    Chemistry, Biocatalysis and Engineering: An Interdisciplinary Approach to the Manufacture of the Benzodiazepine Drug Candidate LY 300164, Benjamin A. Anderson, Marvin M. Hansen, Jeffrey T. Vicenzi and Milton J. Zmijewski
    Benefits and Challenges of Applying Phase-Transfer Catalysis Technology in the Pharmaceutical Industry, Marc E. Halpern

    Asymmetric Synthesis and Enantioselectivity

    Enantioselective Synthesis: The Optimum Process, John J. Partridge and Brian L. Bray
    Practical Catalysts for Asymmetric Synthesis: Ligands from Natural Sugars for Rh-Catalyzed Asymmetric Synthesis of D- and L- Amino Acids, Timothy A. Ayers and T. V. Rajan Babu
    Chiral (Salen)Mn(III) Complexes in Asymmetric Epoxidations: Practical Synthesis of cis-Aminoindanol and Its Application to Enantiopure Drug Synthesis, Chris H. Senanayake and Eric N. Jacobsen

    Drug Substance Final Form and Process Safety

    Chemical Development of the Drug Substance Solid Form, Michael D. Thompson and Jean-René Authelin
    The Basic Principles of Thermal Process Safety: Towards a Better Communication Between Safety Experts and Process Chemists, Wilfried Hoffmann

    Design of Experiments and Automation

    Using Factorial Experiments in the Development of Process Chemistry, Daniel R. Pilipauskas
    Laboratory Automation in Chemical Development, Martin R. Owen and Sheila H. Dewitt


    Kumar Gadamasetti

    ”...the book successfully achieves its goal of presenting the basic principles and challenges associated with the discovery and scale-up of a commercial manufacturing process of a new drug.”
    Journal of Medicinal Chemistry

    ”...gives a thorough overview of the challenges facing the modern development chemists in the pharmaceutical industry. It can be recommended to any graduates or postgraduates considering a career in this fascinating field, and even old hands will find much stimulating chemistry in the case studies. “
    Organic Process Research & Development

    ”...provides a good overview for those wanting an introduction to the science conducted in a process research group. For experienced process chemists, frequent descriptions of creative solutions to difficult problems makes the book worth reading.”
    Journal of the American Chemical Society

    ”...recommended without reservation. It is suitable not only for the process chemist but also for those involved in preparative work in research in teaching, and for advanced students. It should find a place in every chemical library.”
    Angewandte Chemie

    ”...presents pharmaceutical synthesis at its best in a very concise and educational way. The wealth of references and illustrations, and the carefully compiled subject index guarantees fast access to further information....the lively style in which chapters are written keeps the reader interested along the way.”
    European Journal of Pharmaceutics and Biopharmaceutics, 2000