Retrosynthesis in the Manufacture of Generic Drugs

Retrosynthesis in the Manufacture of Generic Drugs PDF Author: Pedro Paulo Santos
Publisher: John Wiley & Sons
ISBN: 1119155533
Category : Science
Languages : en
Pages : 434

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Book Description
Offers a compendium of information on retrosynthesis and process chemistry, featuring innovative "reaction maps" showing synthetic routes of some widely used drugs This book illustrates how the retrosynthetic tool is applied in the Pharmaceutical Industry. It considers and evaluates the many viable synthetic routes that can be used by practicing industrialists, guiding readers through the various steps that lead to the "best" processes and the limits encountered if these are put into practice on an industrial scale of seven key Active Pharmaceutical Ingredient (API). It presents an evaluation of the potential each process has for implementation, before merging the two points of view—of retrosynthesis and process chemistry—in order to show how retrosynthetic analysis assists in selecting the most efficient route for an industrial synthesis of a particular compound whilst giving insight into the industrial process. The book also uses some key concepts used by process chemists to improve efficiency to indicate the best route to select. Each chapter in Retrosynthesis in the Manufacture of Generic Drugs Selected Case Studies is dedicated to one drug, with each containing information on: worldwide sales and patent status of the Active Pharmaceutical Ingredient (API); structure analysis and general retrosynthetic strategy of the API; first reported synthesis; critical analysis of the processes which have been developed and comparison of the synthetic routes; lessons learned; reaction conditions for Schemes A to X; chemical "highlights" on key reactions used during the synthesis; and references. Drugs covered include: Gabapentin, Clopidogrel, Citalopram and Escitalopram, Sitagliptin, Ezetimibe, Montelukast, and Oseltamivir. Show how the retrosynthetic tool is used by the Pharmaceutical Industry Fills a gap for a book where retrosynthetic analysis is systematically applied to active pharmaceutical ingredients (APIs) Features analyses and methodologies that aid readers in uncovering practical synthetic routes to other drug substances, whether they be NCEs (New Chemical Entities) or generic APIs (Active Pharmaceutical Ingredients) Presents information from both the patent and academic literature for those who wish to use as a basis for further study and thought Features the use of "reaction maps" which display several synthetic processes in the same scheme, and which allow easy comparisons of different routes that give the same molecule or intermediate. A selection of these maps are available to download from: https://www.wiley.com/go/santos/retrosynthesis Retrosynthesis in the Manufacture of Generic Drugs Selected Case Studies is an ideal book for researchers and advanced students in organic synthetic chemistry and process chemistry. It will also be of great benefit to practitioners in the pharmaceutical industry, particularly new starters, and those new to process chemistry.

Retrosynthesis in the Manufacture of Generic Drugs

Retrosynthesis in the Manufacture of Generic Drugs PDF Author: Pedro Paulo Santos
Publisher: John Wiley & Sons
ISBN: 1119155533
Category : Science
Languages : en
Pages : 434

Get Book

Book Description
Offers a compendium of information on retrosynthesis and process chemistry, featuring innovative "reaction maps" showing synthetic routes of some widely used drugs This book illustrates how the retrosynthetic tool is applied in the Pharmaceutical Industry. It considers and evaluates the many viable synthetic routes that can be used by practicing industrialists, guiding readers through the various steps that lead to the "best" processes and the limits encountered if these are put into practice on an industrial scale of seven key Active Pharmaceutical Ingredient (API). It presents an evaluation of the potential each process has for implementation, before merging the two points of view—of retrosynthesis and process chemistry—in order to show how retrosynthetic analysis assists in selecting the most efficient route for an industrial synthesis of a particular compound whilst giving insight into the industrial process. The book also uses some key concepts used by process chemists to improve efficiency to indicate the best route to select. Each chapter in Retrosynthesis in the Manufacture of Generic Drugs Selected Case Studies is dedicated to one drug, with each containing information on: worldwide sales and patent status of the Active Pharmaceutical Ingredient (API); structure analysis and general retrosynthetic strategy of the API; first reported synthesis; critical analysis of the processes which have been developed and comparison of the synthetic routes; lessons learned; reaction conditions for Schemes A to X; chemical "highlights" on key reactions used during the synthesis; and references. Drugs covered include: Gabapentin, Clopidogrel, Citalopram and Escitalopram, Sitagliptin, Ezetimibe, Montelukast, and Oseltamivir. Show how the retrosynthetic tool is used by the Pharmaceutical Industry Fills a gap for a book where retrosynthetic analysis is systematically applied to active pharmaceutical ingredients (APIs) Features analyses and methodologies that aid readers in uncovering practical synthetic routes to other drug substances, whether they be NCEs (New Chemical Entities) or generic APIs (Active Pharmaceutical Ingredients) Presents information from both the patent and academic literature for those who wish to use as a basis for further study and thought Features the use of "reaction maps" which display several synthetic processes in the same scheme, and which allow easy comparisons of different routes that give the same molecule or intermediate. A selection of these maps are available to download from: https://www.wiley.com/go/santos/retrosynthesis Retrosynthesis in the Manufacture of Generic Drugs Selected Case Studies is an ideal book for researchers and advanced students in organic synthetic chemistry and process chemistry. It will also be of great benefit to practitioners in the pharmaceutical industry, particularly new starters, and those new to process chemistry.

Synthesis of Essential Drugs

Synthesis of Essential Drugs PDF Author: Ruben Vardanyan
Publisher: Elsevier
ISBN: 9780080462127
Category : Medical
Languages : en
Pages : 634

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Book Description
Synthesis of Essential Drugs describes methods of synthesis, activity and implementation of diversity of all drug types and classes. With over 2300 references, mainly patent, for the methods of synthesis for over 700 drugs, along with the most widespread synonyms for these drugs, this book fills the gap that exists in the literature of drug synthesis. It provides the kind of information that will be of interest to those who work, or plan to begin work, in the areas of biologically active compounds and the synthesis of medicinal drugs. This book presents the synthesis of various groups of drugs in an order similar to that traditionally presented in a pharmacology curriculum. This was done with a very specific goal in mind – to harmonize the chemical aspects with the pharmacology curriculum in a manner useful to chemists. Practically every chapter begins with an accepted brief definition and description of a particular group of drugs, proposes their classification, and briefly explains the present model of their action. This is followed by a detailed discussion of methods for their synthesis. Of the thousands of drugs existing on the pharmaceutical market, the book mainly covers generic drugs that are included in the WHO’s Essential List of Drugs. For practically all of the 700+ drugs described in the book, references (around 2350) to the methods of their synthesis are given along with the most widespread synonyms. Synthesis of Essential Drugs is an excellent handbook for chemists, biochemists, medicinal chemists, pharmacists, pharmacologists, scientists, professionals, students, university libraries, researchers, medical doctors and students, and professionals working in medicinal chemistry. * Provides a brief description of methods of synthesis, activity and implementation of all drug types * Includes synonyms * Includes over 2300 references

Pharmaceutical Process Chemistry for Synthesis

Pharmaceutical Process Chemistry for Synthesis PDF Author: Peter J. Harrington
Publisher: John Wiley & Sons
ISBN: 0470922869
Category : Science
Languages : en
Pages : 815

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Book Description
There is a need to explain that generic versions of a drug may not be manufactured by the same process as brand-name drugs and that the different processes may have dramatically different environmental impacts. Two global forces are at odds today—the push for "greener" processes and the push for lower drug prices. This book brings this conflict into sharp focus by discussing in detail the published process chemistry for top-selling small molecule drugs. Providing insights about process route selection, choice of reagents, and reaction conditions, Pharmaceutical Process Chemistry for Synthesis guides process chemists in identifying best processes for manufacturing these blockbuster drugs as they lose patent protection. Further, it highlights the strategies and methodology that might be useful for expediting the process research and development of the blockbusters of the future. Written from a refreshingly objective perspective, this book is essential for process chemists who need to devise practical syntheses for increasingly complex drugs in a constantly decreasing time frame.

Drug Synthesis Book Set

Drug Synthesis Book Set PDF Author: Jie Jack Li
Publisher: John Wiley & Sons
ISBN: 9781119185659
Category : Science
Languages : en
Pages : 0

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Book Description
This set presents the authoritative and acclaimed Drug Synthesis books edited by Jie Jack Li and Douglas Johnson: Contemporary Drug Synthesis, The Art of Drug Synthesis, Modern Drug Synthesis, and Innovative Drug Synthesis. This book set will be enormously useful to pharmaceutical industry labs, research scientists in lead optimization and process development, and graduate students and courses in organic chemistry, synthetic organic chemistry, heterocyclic chemistry, medicinal chemistry, and drug synthesis courses.

Fundamentals of Medicinal Chemistry

Fundamentals of Medicinal Chemistry PDF Author: Gareth Thomas
Publisher: John Wiley & Sons
ISBN: 0470871695
Category : Science
Languages : en
Pages : 302

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Book Description
Provides a concise introduction to the chemistry of therapeutically active compounds, written in a readable and accessible style. The title begins by reviewing the structures and nomenclature of the more common classes of naturally occurring compounds found in biological organisms. An overview of medicinal chemistry is followed by chapters covering the discovery and design of drugs, pharmacokinetics and drug metabolism, The book concludes with a chapter on organic synthesis, followed by a brief look at drug development from the research stage through to marketing the final product. The text assumes little in the way of prior biological knowledge. relevant biology is included through biological topics, examples and the Appendices. Incorporates summary sections, examples, applications and problems Each chapter contains an additional summary section and solutions to the questions are provided at the end of the text Invaluable for undergraduates studying within the chemical, pharmaceutical and life sciences.

Artificial Intelligence in Drug Discovery

Artificial Intelligence in Drug Discovery PDF Author: Nathan Brown
Publisher: Royal Society of Chemistry
ISBN: 1839160543
Category : Computers
Languages : en
Pages : 425

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Book Description
Following significant advances in deep learning and related areas interest in artificial intelligence (AI) has rapidly grown. In particular, the application of AI in drug discovery provides an opportunity to tackle challenges that previously have been difficult to solve, such as predicting properties, designing molecules and optimising synthetic routes. Artificial Intelligence in Drug Discovery aims to introduce the reader to AI and machine learning tools and techniques, and to outline specific challenges including designing new molecular structures, synthesis planning and simulation. Providing a wealth of information from leading experts in the field this book is ideal for students, postgraduates and established researchers in both industry and academia.

Biotransformations

Biotransformations PDF Author: K. Faber
Publisher: Springer Science & Business Media
ISBN: 3540697918
Category : Science
Languages : en
Pages : 224

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Book Description
Whereas the hydrolases such as proteases, esterases and lipases are sufficiently well researched to be applied in every standard laboratory, other types of enzymes are still waiting to be discovered with respect to their applicability in organic-chemistry transformations on a preparative scale. This latter point is stressed here, with the focus on the newcomer-enzymes'which show great synthetic potential.

De novo Molecular Design

De novo Molecular Design PDF Author: Gisbert Schneider
Publisher: Wiley-VCH
ISBN: 9783527334612
Category : Medical
Languages : en
Pages : 0

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Book Description
Systematically examining current methods and strategies, this ready reference covers a wide range of molecular structures, from organic-chemical drugs to peptides, Proteins and nucleic acids, in line with emerging new drug classes derived from biomacromolecules. A leader in the field and one of the pioneers of this young discipline has assembled here the most prominent experts from across the world to provide first-hand knowledge. While most of their methods and examples come from the area of pharmaceutical discovery and development, the approaches are equally applicable for chemical probes and diagnostics, pesticides, and any other molecule designed to interact with a biological system. Numerous images and screenshots illustrate the many examples and method descriptions. With its broad and balanced coverage, this will be the firststop resource not only for medicinal chemists, biochemists and biotechnologists, but equally for bioinformaticians and molecular designers for many years to come. From the content: * Reaction-driven de novo design * Adaptive methods in molecular design * Design of ligands against multitarget profiles * Free energy methods in ligand design * Fragment-based de novo design * Automated design of focused and target family-oriented compound libraries * Molecular de novo design by nature-inspired computing * 3D QSAR approaches to de novo drug design * Bioisosteres in de novo design * De novo design of peptides, proteins and nucleic acid structures, including RNA aptamers and many more.

Classics in Total Synthesis

Classics in Total Synthesis PDF Author: K. C. Nicolaou
Publisher: John Wiley & Sons
ISBN: 3527292314
Category : Science
Languages : en
Pages : 826

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Book Description
K.C. Nicolaou - Winner of the Nemitsas Prize 2014 in Chemistry This book is a must for every synthetic chemist. With didactic skill and clarity, K. C. Nicolaou and E. Sorensen present the most remarkable and ingenious total syntheses from outstanding synthetic organic chemists. To make the complex strategies more accessible, especially to the novice, each total synthesis is analyzed retrosynthetically. The authors then carefully explain each synthetic step and give hints on alternative methods and potential pitfalls. Numerous references to useful reviews and the original literature make this book an indispensable source of further information. Special emphasis is placed on the skillful use of graphics and schemes: Retrosynthetic analyses, reaction sequences, and stereochemically crucial steps are presented in boxed sections within the text. For easy reference, key intermediates are also shown in the margins. Graduate students and researchers alike will find this book a gold mine of useful information essential for their daily work. Every synthetic organic chemist will want to have a copy on his or her desk.

Comprehensive Organic Chemistry Experiments for the Laboratory Classroom

Comprehensive Organic Chemistry Experiments for the Laboratory Classroom PDF Author: Carlos A. M. Afonso
Publisher: Royal Society of Chemistry
ISBN: 1849739633
Category : Science
Languages : en
Pages : 976

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Book Description
This expansive and practical textbook contains organic chemistry experiments for teaching in the laboratory at the undergraduate level covering a range of functional group transformations and key organic reactions.The editorial team have collected contributions from around the world and standardized them for publication. Each experiment will explore a modern chemistry scenario, such as: sustainable chemistry; application in the pharmaceutical industry; catalysis and material sciences, to name a few. All the experiments will be complemented with a set of questions to challenge the students and a section for the instructors, concerning the results obtained and advice on getting the best outcome from the experiment. A section covering practical aspects with tips and advice for the instructors, together with the results obtained in the laboratory by students, has been compiled for each experiment. Targeted at professors and lecturers in chemistry, this useful text will provide up to date experiments putting the science into context for the students.