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Standard medicinal chemistry courses and texts are organized by classes of drugs with an emphasis on descriptions of their biological and pharmacological effects. This book represents a new approach based on physical organic chemical principles and reaction mechanisms that allow the reader to extrapolate to many related classes of drug molecules. The Second Edition reflects the significant changes in the drug industry over the past decade, and includes chapter problems and other elements that make the book more useful for course instruction. New edition includes new chapter problems and exercises to help students learn, plus extensive references and illustrations Clearly presents an organic chemist's perspective of how drugs are designed and function, incorporating the extensive changes in the drug industry over the past ten years Well-respected author has published over 200 articles, earned 21 patents, and invented a drug that is under consideration for commercialization
Contrary to all other books in the field of organic synthesis, this volume combines Corey's methodology, which is based on the concept of synthon and retrosynthetic analysis, with Evans' methodology based on the `Lapworth model' of alternating polarities. Using this approach, the formation of carbon-carbon bonds and the manipulation of functional groups are treated together, whereas the stereochemical aspects are considered separately. Emphasis is laid on the importance of rigid structures, whether in the starting materials, the synthetic intermediates or the transition states, as a means of controlling the stereochemistry of the organic compounds. Enclosed with the book is a copy of a miniprogram (CHAOS) for an IBM PC, or fully compatible computers, which is an interactive program, affording the beginner a fast and easy way of learning, exploring and looking for new synthetic schemes of molecules of moderate complexity. As a textbook on organic synthesis, this volume will be of immense value at university level.
The second revised edition of an accessible A-level chemistry text, containing additional worked examples and exercises, and covering new topics such as AIDS research, High Temperature Superconductivity and the greenhouse effect.
The first edition of this book was welcomed with great enthusiasm by teachers and students. It therefore seemed opportune to publish a second, revised, updated and extended edition. Unfortunately, Professor F�lix Serratosa died before he could complete this task. Some new material has been added, the more significant changes being: 1) The book has been restructured into two well-differentiated sections: Part A, dealing with conventional organic synthesis, and Part B, devoted exclusively to computer-assisted organic synthesis and based on the former Chapter 11 and Appendices 2, 3 and 4 of the first edition. As decided in advance, Part B was to be the sole responsibility of Dr. Josep Xicart, who prepared the first versions of the CHAOS (Computerisation and Heuristics Applied to Organic Synthesis) program under the direction of Professor Serratosa. 2) In Chapter 1, emphasis is placed on new objectives and targets, as well as on the role that organic synthesis should play in the future in new areas of supramolecular chemistry and bioorganic chemistry. 3) A more extended discussion on synthetic methods and strategies based on radical carbon-carbon bond-forming reactions has been included (Chapter 7). 4) Some new examples to illustrate the heuristic principles have been incorporated (Chapter 4). 5) The chapter on alicyclic stereoselection has been split into two chapters (9 and 10). Chapter 10, which is exclusively devoted to Sharpless''s asymmetric epoxidation and dihyroxylation, has been written de novo. The most recent advances in catalytic stereoselective aldol are incorporated in Chapter 9. 6) In Chapter 11, which is new, the aim is to firstly, present a panoramic view of the most important methods for preparation of optically pure compounds in industrial scale (chirotechnology) and secondly, to give a brief insight into the new biological synthetic methodologies, such as the use of enzymes and catalytic monoclonal antibodies or abzymes, which are becoming more and more important and familiar to the synthetic organic chemist. 7) The chapter dealing with examples of retrosynthetic analysis and the corresponding total synthesis has been enlarged and includes new syntheses of natural products (Chapter 13). 8) The former Chapter 11 and Appendices 2, 3 and 4 devoted to computer assisted organic synthesis have been rewritten and constitute now Part B of the book. The following changes have been introduced: i) CHAOS version 3.0 for Macintosh and version 1.0 for PC Windows� substitute CHAOS version 2.0 for IBM PC and compatibles, ii) The corresponding Instruction Manuals and Disconnection Tables of these new versions are included, iii) two 3� inch diskettes with the new versions of CHAOS and CHAOSDBASE replace the diskette of version 2.0, iv) a new Appendix (Appendix B-1) with a brief introduction to Ugi''s Theory of Constitutional Chemistry and to the programs EROS and IGOR has also been added. 9) The main improvements in CHAOS version 3.0 for Macintosh are: i) The unique numbering or canonical matrices, ii) new disconnections, which are more selective, iii) besides RINGS and SYNTHETICALLY SIGNIFICANT RINGS, the new version gives, if required, the PRIMARY RINGS. Other new options are SELECT and RESIZE in the menu EDIT, by which one can select part of a synthetic sequence or resize the molecule drawing, iv) the possibility to introduce new disconnections from inside the program CHAOS itself and work (if desired) with one''s own chemistry, through CHAOSBASE. The aim of this program is to create DATABASES of new DISCONNECTIONS. Such DATABASES can be opened from the program CHAOS in such a manner that it allows to disconnect molecules according to the DISCONNECTIONS defined in the DATABASE (instead of disconnecting according to predefined ones implemented in CHAOS). 10) Mistakes and errors detected in the first edition have been corrected.
An instructor-oriented resource providing information on implementing clickers in organic chemistry courses. Part I gives instructors information on how to choose and manage a CRS system, develop effective questions, and integrate the questions into their courses. Part II contains 140 class-tested, lecture-ready questions. Most questions include histograms that show actual student response, generated in large classes with 200-300 students over multiple semesters. Each question also includes insights and suggestions for implementation.
Students see chemistry in action in this thorough but accessible informational text that is aligned to science core curriculum. It includes crosscutting concepts and covers carbon bonding, chains, and rings; alcohol and acids; other organic compounds, such as esters, aldehydes, ketones, ethers, amines, and halides; and polymers. Fact boxes about key terms, events, people, discoveries, and technologies, along with sidebars that give everyday examples of chemical applications help make the subject fun for readers. The volume also contains information about the life of German chemist Friedrich Wöhler, one of the fathers of organic chemistry.
Medicinal chemistry is a complex topic. Written in an easy to follow and conversational style, Basic Concepts in Medicinal Chemistry focuses on the fundamental concepts that govern the discipline of medicinal chemistry as well as how and why these concepts are essential to therapeutic decisions. The book emphasizes functional group analysis and the basics of drug structure evaluation. In a systematic fashion, learn how to identify and evaluate the functional groups that comprise the structure of a drug molecule and their influences on solubility, absorption, acid/base character, binding interactions, and stereochemical orientation. Relevant Phase I and Phase II metabolic transformations are also discussed for each functional group. Key features include: • Discussions on the roles and characteristics of organic functional groups, including the identification of acidic and basic functional groups. • How to solve problems involving pH, pKa, and ionization; salts and solubility; drug binding interactions; stereochemistry; and drug metabolism. • Numerous examples and expanded discussions for complex concepts. • Therapeutic examples that link the importance of medicinal chemistry to pharmacy and healthcare practice. • An overview of structure activity relationships (SARs) and concepts that govern drug design. • Review questions and practice problems at the end of each chapter that allow readers to test their understanding, with the answers provided in an appendix. Whether you are just starting your education toward a career in a healthcare field or need to brush up on your organic chemistry concepts, this book is here to help you navigate medicinal chemistry. About the Authors Marc W. Harrold, BS, Pharm, PhD, is Professor of Medicinal Chemistry at the Mylan School of Pharmacy, Duquesne University, Pittsburgh, PA. Professor Harrold is the 2011 winner of the Omicron Delta Kappa "Teacher of the Year" award at Duquesne University. He is also the two-time winner of the "TOPS" (Teacher of the Pharmacy School) award at the Mylan School of Pharmacy. Robin M. Zavod, PhD, is Associate Professor for Pharmaceutical Sciences at the Chicago College of Pharmacy, Midwestern University, Downers Grove, IL, where she was awarded the 2012 Outstanding Faculty of the Year award. Professor Zavod also serves on the adjunct faculty for Elmhurst College and the Illinois Institute of Technology. She currently serves as Editor-in-Chief of the journal Currents in Pharmacy Teaching and Learning.
Provides the background, tools, and models required to understand organic synthesis and plan chemical reactions more efficiently Knowledge of physical chemistry is essential for achieving successful chemical reactions in organic chemistry. Chemists must be competent in a range of areas to understand organic synthesis. Organic Chemistry provides the methods, models, and tools necessary to fully comprehend organic reactions. Written by two internationally recognized experts in the field, this much-needed textbook fills a gap in current literature on physical organic chemistry. Rigorous yet straightforward chapters first examine chemical equilibria, thermodynamics, reaction rates and mechanisms, and molecular orbital theory, providing readers with a strong foundation in physical organic chemistry. Subsequent chapters demonstrate various reactions involving organic, organometallic, and biochemical reactants and catalysts. Throughout the text, numerous questions and exercises, over 800 in total, help readers strengthen their comprehension of the subject and highlight key points of learning. The companion Organic Chemistry Workbook contains complete references and answers to every question in this text. A much-needed resource for students and working chemists alike, this text: -Presents models that establish if a reaction is possible, estimate how long it will take, and determine its properties -Describes reactions with broad practical value in synthesis and biology, such as C-C-coupling reactions, pericyclic reactions, and catalytic reactions -Enables readers to plan chemical reactions more efficiently -Features clear illustrations, figures, and tables -With a Foreword by Nobel Prize Laureate Robert H. Grubbs Organic Chemistry: Theory, Reactivity, and Mechanisms in Modern Synthesis is an ideal textbook for students and instructors of chemistry, and a valuable work of reference for organic chemists, physical chemists, and chemical engineers.