Fundamentals of Early Clinical Drug Development

Contributors.
Preface.
1. Reflections on Process Research II (Edward J. J.Grabowski).
2. Development and Scale-Up of a Heterocyclic Cross-Coupling forthe Synthesis of5-[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 KeyFragment for the Formal Total Synthesis of the Anti-tumor AgentCryptophycin 52 (James Aikins, Tony Y. Zhang, Milton Zmijewski,and Barbara Briggs).
4. Efforts Toward a Commercially Viable Route and Process to theSynthesis of HIV PI GW640385X (John C. Roberts, Roman Davis,Brian D. Doan, Thomas C. Lovelace, Daniel E. Patterson, FrankRoschangar, Barry Sickles, Jennifer F. Toczko, and JuYang).
5. Development of an Asymmetric Synthesis of ABT-100 (AlbertW. 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 (RexJennings, William S. Kissel, Tung V. Le, Edward Lenoir, ThomasMulhern, and Robert Wade).
7. Responsibilities of the Process Chemist: Beyond SyntheticOrganic Chemistry (Stéphane Caron).
8. Outsourcing--The Challenge of Science, Speed, andQuality (Simone Andler-Burzlaff, Jason Bertola, and Roger E.Marti).
9. Automation and the Changing Face of Process Research in thePharmaceutical 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 (JosephH. Childers, Jr.)
11. Synthesis and Application of Radioisotopes in PharmaceuticalResearch 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 PharmaceuticalIngredients (David J. am Ende and Peter R. Rose).
14. Challenges in Early Formulation: Turning Drug Substance intoDrug Product (Mark H. Kleinman and Beeah Lee).
15. Intellectual Property and Early Development (Maria I.Shchuka).
Index.