Fundamentals of Early Clinical Drug Development: From Synthesis Design to Formulation

Preface.

1. Reflections on Process Research II (Edward J. J. Grabowski).

2. Development and Scale-Up of a Heterocyclic Cross-Coupling for the Synthesis of 5-[2-(3-Methyl-3H-imidazol-4-yl)-thieno[3,2-b]pyridine-7-yl] amino-2-methyl-1H-indole (John A. Ragan).

3. Large-Scale Enantioselective Preparation of 2E,7E, 5S,6R,5-Hydroxy-6-methyl-8-phenyl-octa-2,7-dienoic Acid, a Key Fragment for the Formal Total Synthesis of the Anti-tumor Agent Cryptophycin 52 (James Aikins, Tony Y. Zhang, Milton Zmijewski, and Barbara Briggs).

4. Efforts Toward a Commercially Viable Route and Process to the Synthesis of HIV PI GW640385X (John C. Roberts, Roman Davis, Brian D. Doan, Thomas C. Lovelace, Daniel E. Patterson, Frank Roschangar, Barry Sickles, Jennifer F. Toczko, and Ju Yang).

5. Development of an Asymmetric Synthesis of ABT-100 (Albert W. Kruger, Michael J. Rozema, Bridget D. Rohde, Bhadra Shelat, Lakshmi Bhagavatula, James J. Tien, Weijiang Zhang, and Rodger F. Henry)

6. Asymmetric Hydrogenation: A New Route to Pregabalin (Rex Jennings, William S. Kissel, Tung V. Le, Edward Lenoir, Thomas Mulhern, and Robert Wade).

7. Responsibilities of the Process Chemist: Beyond Synthetic Organic Chemistry (Stéphane Caron).

8. Outsourcing—The Challenge of Science, Speed, and Quality (Simone Andler-Burzlaff, Jason Bertola, and Roger E. Marti).

9. Automation and the Changing Face of Process Research in the Pharmaceutical Industry (Edward J. Delaney, Merrill L. Davies, Brent D. Karcher, Victor W. Rosso, A. Erik Rubin, and John J. Venit)

10. Large-Scale Synthesis: An Engineering Perspective (Joseph H. Childers, Jr.)

11. Synthesis and Application of Radioisotopes in Pharmaceutical Research and Development (Larry E. Weaner and David C. Hoerr).

12. Selection of the Drug Form in Exploratory Development (George J. Quallich).

13. Strategies to Achieve Particle Size of Active Pharmaceutical Ingredients (David J. am Ende and Peter R. Rose).

14. Challenges in Early Formulation: Turning Drug Substance into Drug Product (Mark H. Kleinman and Beeah Lee).

15. Intellectual Property and Early Development (Maria I. Shchuka).

Index.