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Cover image for Fundamentals of early clinical drug development : from synthesis design to formulation
Title:
Fundamentals of early clinical drug development : from synthesis design to formulation
Publication Information:
Hoboken, NJ : Wiley-Interscience, 2006
ISBN:
9780471692782

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30000010108218 RM301.27 F86 2006 Open Access Book Book
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Summary

Summary

An informative look at the intricacies of today's drug development process



Once a discovery organization has identified a potential new drug candidate, it is the daunting task of synthetic organic chemists to identify the chemical process suitable for preparation of this compound in a highly regulated environment. Only through a multi-layered chemical process that takes into account such factors as safety, environmental considerations, freedom to operate and cost-effectiveness can researchers begin to refine the drug in terms of quality and yield.

This book covers both recent advances in the design and synthesis of new drugs, as well as the myriad other issues facing a new drug candidate as it moves through the development process. Utilizing recent case studies, the authors provide valuable insights into the complexities of the process, from designing new synthetic methodologies and applying new automated techniques for finding optimal reaction conditions to selecting the final drug form and formulation.

Both novice and active researchers will appreciate the inclusion of chapters on such diverse topics as:
* Cross-coupling methods
* Asymmetric synthesis
* Automation
* Chemical Engineering
* Application of radioisotopes
* Final form selection
* Formulations
* Intellectual property


A wealth of real-world examples and contributions from leading process scientists, engineers, and related professionals make this book a valuable addition to the scientific literature.


Author Notes

AHMED F. ABDEL-MAGID is a Senior Research Fellow in Chemical and Pharmaceutical Development at Johnson & Johnson Pharmaceutical Research & Development, L.L.C.

STÉPHANE CARON is a Director in Chemical Research and Development at Pfizer Global R&D.


Table of Contents

Edward J. J. GrabowskiJohn A. RaganJames Aikins and Tony Y. Zhang and Milton Zmijewski and Barbara BriggsJohn C. Roberts and Roman Davis and Brian D. Doan and Thomas C. Lovelace and Daniel E. Patterson and Frank Roschangar and Barry Sickles and Jennifer F. Toczko and Ju YangAlbert W. Kruger and Michael J. Rozema and Bridget D. Rohde and Bhadra Shelat and Lakshmi Bhagavatula and James J. Tien and Weijiang Zhang and Rodger F. HenryRex Jennings and William S. Kissel and Tung V. Le and Edward Lenoir and Thomas Mulhern and Robert WadeStephane CaronSimone Andler-Burzlaff and Jason Bertola and Roger E. MartiEdward J. Delaney and Merrill L. Davies and Brent D. Karcher and Victor W. Rosso and A. Erik Rubin and John J. VenitJoseph H. Childers, Jr.Larry E. Weaner and David C. HoerrGeorge J. QuallichDavid J. am Ende and Peter R. RoseMark H. Kleinman and Beeah LeeMaria I. Shchuka
Contributorsp. vii
Prefacep. xi
1 Reflections on Process Research IIp. 1
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-indolep. 21
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 52p. 37
4 Efforts Toward a Commercially Viable Route and Process to the Synthesis of HIV PI GW640385Xp. 53
5 Development of an Asymmetric Synthesis of ABT-100p. 73
6 Asymmetric Hydrogenation: A New Route to Pregabalinp. 85
7 Responsibilities of the Process Chemist: Beyond Synthetic Organic Chemistryp. 101
8 Outsourcing-The Challenge of Science, Speed, and Qualityp. 113
9 Automation and the Changing Face of Process Research in the Pharmaceutical Industryp. 129
10 Large-Scale Synthesis: An Engineering Perspectivep. 163
11 Synthesis and Application of Radioisotopes in Pharmaceutical Research and Developmentp. 189
12 Selection of the Drug Form in Exploratory Developmentp. 215
13 Strategies to Achieve Particle Size of Active Pharmaceutical Ingredientsp. 247
14 Challenges in Early Formulation: Turning Drug Substance into Drug Productp. 269
15 Intellectual Property and Early Developmentp. 295
Indexp. 319
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