Designed to provide a comprehensive, step-by-step approach to organic process research and development in the pharmaceutical, fine chemical, and agricultural chemical industries, this book describes the steps taken, following synthesis and evaluation, to bring key compounds to market in a cost-effective manner. It describes hands-on, step-by-step, approaches to solving process development problems, including route, reagent, and solvent selection; optimising catalytic reactions; chiral syntheses; and "green chemistry." Second Edition highlights: • Reflects the current thinking in chemical process R&D for small molecules • Retains similar structure and orientation to the first edition. • Contains approx. 85% new material • Primarily new examples (work-up and prospective considerations for pilot plant and manufacturing scale-up) • Some new/expanded topics (e.g. green chemistry, genotoxins, enzymatic processes) • Replaces the first edition, although the first edition contains useful older examples that readers may refer to Provides insights into generating rugged, practical, cost-effective processes for the chemical preparation of "small molecules" Breaks down process optimization into route, reagent and solvent selection, development of reaction conditions, workup, crystallizations and more Presents guidelines for implementing and troubleshooting processes
Handbook of Synthetic Organic Chemistry, Second Edition updates and expands the author’s popular 2007 work, Synthetic Organic Chemist’s Companion. This new handbook provides valuable, practical guidance; incorporates corrections, and includes coverage on important topics, such as lyophylization, crystallization, precipitation, HPLC detectors, gases, and microwave reactions. The book maintains the useful organization of the author’s earlier work, beginning with a basic overview and walking through every practical step of the process of organic synthesis, from reagents, solvents, and temperature control, to documentation, implementation, purification, and analytical methods for the product. From planning and setting up reactions, to recording them, the book provides insight and valuable guidance into every step of the process. Practical guidance for planning, working up, documenting, analyzing, and improving reactions in synthetic organic chemistry
A hands-on guide to assist in the planning and execution of synthetic reactions in the laboratory Despite the maturity of organic chemistry, it can still be very challenging to identify optimal methods for synthetic transformations that perform as well in real-world manufacturing processes as they do in the laboratory. This detailed and accessible guide attempts to address this vexing issue and deliver proven methodologies practicing synthetic chemists will find valuable for identifying reaction conditions that work reliably over the broadest possible range of substrates. Practical Synthetic Organic Chemistry: Provides a practical guide to strategically planning and executing chemical syntheses for the bench chemist in industry Discusses information that is not common knowledge beyond the boundaries of process chemistry groups, such as the synthetic routes of selected contemporary pharmaceutical drugs and practical solvents, as well as green chemistry concepts Highlights key reactions, including substitutions, additions, eliminations, rearrangements, oxidations, and reductions Addresses basic principles, mechanisms, advantages and disadvantages of the methodology, and techniques for achieving laboratory success Incorporating such an extraordinary wealth of information on organic chemistry and its related fields into one complete volume distinguishes Practical Synthetic Organic Chemistry as an incomparable desktop reference for professionals—and an invaluable study aid for students.
This text discusses the functions of Process R&D (research and development), which involves the method of transforming a research synthetic procedure into a plant process and the key aspects of a synthesis that must be considered when scaling up a process. Topics consist of: basic principles of chemical development; techniques for the minimization of by-product impurities; criteria for cost-effective synthesis of enantiopure compounds by resolutions; asymmetric synthesis, and "chiral pool" strategy; synthesis for labeling substances with hydrogen or carbon isotopes; and last, licensing.
This book deals with various unique elements in the drug development process within chemical engineering science and pharmaceutical R&D. The book is intended to be used as a professional reference and potentially as a text book reference in pharmaceutical engineering and pharmaceutical sciences. Many of the experimental methods related to pharmaceutical process development are learned on the job. This book is intended to provide many of those important concepts that R&D Engineers and manufacturing Engineers should know and be familiar if they are going to be successful in the Pharmaceutical Industry. These include basic analytics for quantitation of reaction components– often skipped in ChE Reaction Engineering and kinetics books. In addition Chemical Engineering in the Pharmaceutical Industry introduces contemporary methods of data analysis for kinetic modeling and extends these concepts into Quality by Design strategies for regulatory filings. For the current professionals, in-silico process modeling tools that streamline experimental screening approaches is also new and presented here. Continuous flow processing, although mainstream for ChE, is unique in this context given the range of scales and the complex economics associated with transforming existing batch-plant capacity. The book will be split into four distinct yet related parts. These parts will address the fundamentals of analytical techniques for engineers, thermodynamic modeling, and finally provides an appendix with common engineering tools and examples of their applications.
The Practice of Medicinal Chemistry, Fourth Edition provides a practical and comprehensive overview of the daily issues facing pharmaceutical researchers and chemists. In addition to its thorough treatment of basic medicinal chemistry principles, this updated edition has been revised to provide new and expanded coverage of the latest technologies and approaches in drug discovery. With topics like high content screening, scoring, docking, binding free energy calculations, polypharmacology, QSAR, chemical collections and databases, and much more, this book is the go-to reference for all academic and pharmaceutical researchers who need a complete understanding of medicinal chemistry and its application to drug discovery and development. Includes updated and expanded material on systems biology, chemogenomics, computer-aided drug design, and other important recent advances in the field Incorporates extensive color figures, case studies, and practical examples to help users gain a further understanding of key concepts Provides high-quality content in a comprehensive manner, including contributions from international chapter authors to illustrate the global nature of medicinal chemistry and drug development research An image bank is available for instructors at www.textbooks.elsevier.com
The vast majority of drugs are organic molecular entities. A clear understanding of the organic chemistry of drug degradation is essential to maintaining the stability, efficacy, and safety of a drug product throughout its shelf-life. During analytical method development, stability testing, and pharmaceutical manufacturing troubleshooting activities, one of the frequently occurring and usually challenging events would be the identification of drug degradants and understanding of drug degradation mechanisms and pathways. This book is written by a veteran of the pharmaceutical industry who has first-hand experience in drug design and development, drug degradation mechanism studies, analytical development, and manufacturing process troubleshooting and improvement. The author discusses various degradation pathways with an emphasis on the mechanisms of the underlying organic chemistry, which should aid greatly in the efforts of degradant identification, formulation development, analytical development, and manufacturing process improvement. Organic reactions that are significant in drug degradation will first be reviewed and then illustrated by examples of drug degradation reported in the literature. The author brings the book to a close with a final chapter dedicated to the strategy for rapid elucidation of drug degradants with regard to the current regulatory requirements and guidelines. One chapter that should be given special attention is Chapter 3, Oxidative Degradation. Oxidative degradation is one of the most common degradation pathways but perhaps the most complex one. This chapter employs more than sixty drug degradation case studies with in-depth discussion in regard to their unique degradation pathways. With the increasing regulatory requirements on the quality and safety of pharmaceutical products, in particular with regard to drug impurities and degradants, the book will be an invaluable resource for pharmaceutical and analytical scientists who engage in formulation development, analytical development, stability studies, degradant identification, and support of manufacturing process improvement. In addition, it will also be helpful to scientists engaged in drug discovery and development as well as in drug metabolism studies.
A reactions oriented course is a staple of most graduate organic programs, and synthesis is taught either as a part of that course or as a special topic. Ideally, the incoming student is an organic major, who has a good working knowledge of basic reactions, stereochemistry and conformational principles. In fact, however, many (often most) of the students in a first year graduate level organic course have deficiencies in their undergraduate work, are not organic majors and are not synthetically inclined. To save students much time catching up this text provides a reliable and readily available source for background material that will enable all graduate students to reach the same high level of proficiency in organic chemistry. Produced over many years with extensive feedback from students taking an organic chemistry course this book provides a reaction based approach. The first two chapters provide an introduction to functional groups; these are followed by chapters reviewing basic organic transformations (e.g. oxidation, reduction). The book then looks at carbon-carbon bond formation reactions and ways to ‘disconnect’ a bigger molecule into simpler building blocks. Most chapters include an extensive list of questions to test the reader’s understanding. There is also a new chapter outlining full retrosynthetic analyses of complex molecules which highlights common problems made by scientists. The book is intended for graduate and postgraduate students, scientific researchers in chemistry New publisher, new edition; extensively updated and corrected Over 950 new references with more than 6100 references in total Over 600 new reactions and figures replaced or updated Over 300 new homework problems from the current literature to provide nearly 800 problems to test reader understanding of the key principles
An integrated and insightful look at successful drug synthesis in today's drug discovery market The pharmaceutical industry is unquestionably vibrant today, with drug synthesis making a vital contribution. Whether in the early developmental stages of identifying and optimizing a lead, or the latter stages of process development and cost-effective scale-up, the ability to design elegant and economical synthetic routes is often a major factor in the eventual viability and commercial success of a drug. Contemporary Drug Synthesis examines how leading researchers and manufacturers have integrated chemistry, biology, pharmacokinetics, and a host of other disciplines in the creation and development of leading drugs. Authored by four of the pharmaceutical industry's most respected scientists, this timely volume: Focuses on the processes that resulted in high-profile drugs including Lipitor, Celebrex, Viagra, Gleevec, Nexium, Claritin, and over a dozen others Provides an in-depth introduction to each drug, followed by a detailed account of its synthesis Organizes the drugs into fourteen therapeutic areas for clarity and ease of use Process chemists provide an essential bridge between chemistry and the marketplace, creating scientifically practical drug processes while never losing sight of the commercial viability of those processes. Contemporary Drug Synthesis meets the needs of a growing community of researchers in pharmaceutical research and development, and is both a useful guide for practicing pharmaceutical scientists and an excellent text for medicinal and organic chemistry students.
Workbook developed from the Workshop Chemistry Project which explored, developed and applied the concept of peer-led team learning in problem-solving workshops in introductory chemistry courses.
"Nuclear Magnetic Resonance (NMR) Spectroscopy remains the foremost analytical technique for the structure elucidation of organic molecules and an indispensable tool for the synthetic, medicinal and natural product chemist. New techniques continue to emerge and the application of NMR methods continues to expand. High-Resolution NMR Techniques in Organic Chemistry is designed for use in academic and industrial NMR facilities, as a text for graduate-level NMR courses, and as an accessible reference for the chemist's or spectroscopist's desk." --Book Jacket.
Green chemistry is a new way of looking at organic synthesis and the design of drug molecules, offering important environmental and economic advantages over traditional synthetic processes. Pharmaceutical companies are increasingly turning to the principles of green chemistry in an effort to reduce waste, reduce costs and develop environmentally benign processes. Green Techniques for Organic Synthesis and Medicinal Chemistry presents an overview of the established and emerging techniques in green organic chemistry, highlighting their applications in medicinal chemistry. The book is divided into four parts: Introduction: Introduces the reader to the toxicology of organic chemicals,their environmental impact, and the concept of green chemistry. Green Catalysis: Covers a variety of green catalytic techniques including organocatalysis, supported catalysis, biocatalysis, fluorous catalysis, and catalytic direct C-H bond activation reactions. Green Synthetic Techniques: Presents a series of new techniques, assessing the green chemistry aspects and limitations (i.e. cost, equipment, expertise). Techniques include reactions in alternative solvents, atom economic multicomponent reactions, microwave and ultrasonic reactions, solid-supported synthesis, fluorous and ionic liquid-based recycling techniques, and flow reactors. Green Techniques in Pharmaceutical Industry: Covers applications of green chemistry concepts and special techniques for medicinal chemistry, including synthesis, analysis, separation, formulation, , and drug delivery. Process and business case studies are included to illustrate the applications in the pharmaceutical industry. Green Techniques for Organic Synthesis and Medicinal Chemistry is an essential resource on green chemistry technologies for academic researchers, R&D professionals and students working in organic chemistry and medicinal chemistry.
Bioconjugate Techniques, 3rd Edition, is the essential guide to the modification and cross linking of biomolecules for use in research, diagnostics, and therapeutics. It provides highly detailed information on the chemistry, reagent systems, and practical applications for creating labeled or conjugate molecules. It also describes dozens of reactions, with details on hundreds of commercially available reagents and the use of these reagents for modifying or crosslinking peptides and proteins, sugars and polysaccharides, nucleic acids and oligonucleotides, lipids, and synthetic polymers. Offers a one-stop source for proven methods and protocols for synthesizing bioconjugates in the lab Provides step-by-step presentation makes the book an ideal source for researchers who are less familiar with the synthesis of bioconjugates Features full color illustrations Includes a more extensive introduction into the vast field of bioconjugation and one of the most thorough overviews of immobilization chemistry ever presented
Experimental Organic Chemistry: Laboratory Manual is designed as a primer to initiate students in Organic Chemistry laboratory work. Organic Chemistry is an eminently experimental science that is based on a well-established theoretical framework where the basic aspects are well established but at the same time are under constant development. Therefore, it is essential for future professionals to develop a strong background in the laboratory as soon as possible, forming good habits from the outset and developing the necessary skills to address the challenges of the experimental work. This book is divided into three parts. In the first, safety issues in laboratories are addressed, offering tips for keeping laboratory notebooks. In the second, the material, the main basic laboratory procedures, preparation of samples for different spectroscopic techniques, Microscale, Green Chemistry, and qualitative organic analysis are described. The third part consists of a collection of 84 experiments, divided into 5 modules and arranged according to complexity. The last two chapters are devoted to the practices at Microscale Synthesis and Green Chemistry, seeking alternatives to traditional Organic Chemistry. Organizes lab course coverage in a logical and useful way Features a valuable chapter on Green Chemistry Experiments Includes 84 experiments arranged according to increasing complexity
This book brings together the chemical strategies used in the optimisation of organic reactions and processes, and highlights the practical and technological options available. This book offers: an encyclopedic treatment of organic chemistry from an industrial, process research and development, and manufacturing point of view plenty of examples to illustrate the scope and limitation of the strategies a comprehensive index organised by topic, reaction type, and reagent an extensive literature survey. This is an essential and comprehensive guide for experienced practitioners of chemical process research and development, fresh recruits to chemical industry R&D divisions, and academics who are interested in interacting with the chemical industry, optimising their synthetic strategies, and enriching the field of atom economy.
Future Directions in Biocatalysis, Second Edition, presents the future direction and latest research on how to utilize enzymes, i.e., natural catalysts, to make medicines and other necessities for humans. It emphasizes the most important and unique research on biocatalysis instead of simply detailing the ABC’s on the topic. This book is an indispensable tool for new researchers in the field to help identify specific needs, start new projects that address current environmental concerns, and develop techniques based on green technology. It provides invaluable hints and clues for conducting new research on enzymes, with final sections outlining future directions in biocatalysis further expanding the science into new applications. Gives future directions in the area of biocatalysis research Presents research topics based on their uniqueness, originality, and novelty Includes many explanatory figures to demonstrate concepts to both organic chemists and biochemists Shows that there is no boundary between organic chemistry and biochemistry
Process Intensification: Engineering for Efficiency, Sustainability and Flexibility is the first book to provide a practical working guide to understanding process intensification (PI) and developing successful PI solutions and applications in chemical process, civil, environmental, energy, pharmaceutical, biological, and biochemical systems. Process intensification is a chemical and process design approach that leads to substantially smaller, cleaner, safer, and more energy efficient process technology. It improves process flexibility, product quality, speed to market and inherent safety, with a reduced environmental footprint. This book represents a valuable resource for engineers working with leading-edge process technologies, and those involved research and development of chemical, process, environmental, pharmaceutical, and bioscience systems. No other reference covers both the technology and application of PI, addressing fundamentals, industry applications, and including a development and implementation guide Covers hot and high growth topics, including emission prevention, sustainable design, and pinch analysis World-class authors: Colin Ramshaw pioneered PI at ICI and is widely credited as the father of the technology
The second edition of Comprehensive Organic Synthesis—winner of the 2015 PROSE Award for Multivolume Reference/Science from the Association of American Publishers—builds upon the highly respected first edition in drawing together the new common themes that underlie the many disparate areas of organic chemistry. These themes support effective and efficient synthetic strategies, thus providing a comprehensive overview of this important discipline. Fully revised and updated, this new set forms an essential reference work for all those seeking information on the solution of synthetic problems, whether they are experienced practitioners or chemists whose major interests lie outside organic synthesis. In addition, synthetic chemists requiring the essential facts in new areas, as well as students completely new to the field, will find Comprehensive Organic Synthesis, Second Edition an invaluable source, providing an authoritative overview of core concepts. Winner of the 2015 PROSE Award for Multivolume Reference/Science from the Association of American Publishers Contains more than170 articles across nine volumes, including detailed analysis of core topics such as bonds, oxidation, and reduction Includes more than10,000 schemes and images Fully revised and updated; important growth areas—including combinatorial chemistry, new technological, industrial, and green chemistry developments—are covered extensively
In this textbook, designed to be used with classic texts of organic chemistry at the undergraduate level, or standing alone for more advanced students, the two experts, M. M. Green and H. A. Wittcoff bring together the principles and the practice. Written for students, while also giving much information that may be used to enhance teaching of the subject, the book's ten concise chapters combine important commercial and practical processes with the principles of organic chemistry. The result is a source of otherwise barely accessible information. In addition, personal anecdotes from the authors' vast experience make this a fascinating and indispensable textbook for everyone wishing to enhance an appreciation of this subject. Reviews: "This book is a joy to read (and re-read)." —James A. Moore, Rensselaer Polytechnic Institute "This very interesting book is going to find a unique place in the repertoire of organic textbooks." —James Canary, New York University "Simply put, this book is a gem. The chemistry described is rigorous but the warm, humorous, and conversational writing style makes the book a joy to read." —Dasan M. Thamattoor, Colby College "I have never come across such an enticing mix of stories of discovery with basic chemistry!" —Roald Hoffmann, Cornell University "This is a highly original book filling an obvious need." —Herbert Morawetz, Polytechnic University "This book is a delightful contribution to the field of organic chemistry that offers a useful pedagogical approach." —Pedro Cintas, Facultad de Ciencias-UEX Badajoz, Spain "What an excellent read! The book, intended for organic chemistry students, is in the style of the first books on organic chemistry by Isaac Asimov which impressed me as a teenager in the 1960´s. It makes the discovery of new chemicals and processes seem exciting, and emphasises the importance of academic understanding in the development of the chemical industry. (...) The book is full of interesting anecdotes, often related to serendiptious discoveries. But, as Louis Pasteur said, "Chance favours the prepared mind". (...) One interesting story on the cracking of petroleum and the subsequent build up of coke deposits relates to a father who was so obsessed with the subject that he called his son Carbon; Carbon then named his own daughters Methyl and Ethyl. In my opinion, any father who saddles his children with such names might be regarded as a well known arsenic heterocycle! In conclusion, all organic chemists should read this book for pleasure, not just to learn new knowledge. I hope the authors can be persuaded to write a second volume which covers the fine chemicals industry." —Organic Process Research & Development, Dr. Trevor Laird "This is a unique, fascinating book that bridges organic chemistry principles with chemical industrial applications. The story telling style make the reading/learning experience extremely enjoyable." —Qiao-Sheng Hu, College of Staten Island, City University of New York